Informacja

Drogi użytkowniku, aplikacja do prawidłowego działania wymaga obsługi JavaScript. Proszę włącz obsługę JavaScript w Twojej przeglądarce.

Przeglądasz jako GOŚĆ

Wyszukujesz frazę ""Drug Inverse Agonism"" wg kryterium: Temat


Tytuł :
Molecular Dynamics Simulations Based on 1-Phenyl-4-Benzoyl-1-Hydro-Triazole ERRα Inverse Agonists.
Autorzy :
Gao Z; School of Chemistry and Chemical Engineering, Qilu University of Technology (Shandong Academy of Sciences), 3501 Da Xue Road, Jinan 250353, China.
Du Y; School of Chemistry and Chemical Engineering, Qilu University of Technology (Shandong Academy of Sciences), 3501 Da Xue Road, Jinan 250353, China.
Sheng X; College of Chemistry, Chemical Engineering and Materials Science, Shandong Normal University, 88 Wen Hua Dong Road, Jinan 250014, China.
Shen J; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China.
Pokaż więcej
Źródło :
International journal of molecular sciences [Int J Mol Sci] 2021 Apr 02; Vol. 22 (7). Date of Electronic Publication: 2021 Apr 02.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Inverse Agonism*
Receptors, Estrogen/*antagonists & inhibitors
Molecular Dynamics Simulation
Czasopismo naukowe
Tytuł :
Pimavanserin, a 5HT 2A receptor inverse agonist, rapidly suppresses Aβ production and related pathology in a mouse model of Alzheimer's disease.
Autorzy :
Yuede CM; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Wallace CE; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Davis TA; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Gardiner WD; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Hettinger JC; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Edwards HM; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Hendrix RD; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Doherty BM; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Yuede KM; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Burstein ES; ACADIA Pharmaceuticals Inc, San Diego, CA, USA.
Cirrito JR; Department of Neurology, Washington University School of Medicine, St. Louis, MO, USA.; Knight Alzheimer's Disease Research Center, Washington University School of Medicine, St. Louis, MO, USA.; Hope Center for Neurological Disorders, Washington University School of Medicine, St. Louis, MO, USA.
Pokaż więcej
Źródło :
Journal of neurochemistry [J Neurochem] 2021 Mar; Vol. 156 (5), pp. 658-673. Date of Electronic Publication: 2021 Jan 10.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
MeSH Terms :
Drug Inverse Agonism*
Alzheimer Disease/*metabolism
Amyloid beta-Peptides/*antagonists & inhibitors
Piperidines/*therapeutic use
Receptor, Serotonin, 5-HT2A/*metabolism
Serotonin 5-HT2 Receptor Agonists/*therapeutic use
Urea/*analogs & derivatives
Alzheimer Disease/drug therapy ; Alzheimer Disease/genetics ; Alzheimer Disease/pathology ; Amyloid beta-Peptides/biosynthesis ; Animals ; Female ; Male ; Maze Learning/drug effects ; Maze Learning/physiology ; Mice ; Mice, Inbred C3H ; Mice, Transgenic ; Piperidines/pharmacology ; Serotonin 5-HT2 Receptor Agonists/pharmacology ; Serotonin 5-HT2 Receptor Antagonists/pharmacology ; Serotonin 5-HT2 Receptor Antagonists/therapeutic use ; Urea/pharmacology ; Urea/therapeutic use
Czasopismo naukowe
Tytuł :
Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors.
Autorzy :
Chen Z; Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China; Shenzhen Pingle Orthopaedic Hospital (Shenzhen Pingshan Traditional Chinese Medicine Hospital), Shenzhen, 518118, China.
Chen H; Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Zhang Z; Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Ding P; Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Yan X; Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Li Y; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, China.
Zhang S; Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Gu Q; Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
Zhou H; Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China. Electronic address: .
Xu J; Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, China. Electronic address: .
Pokaż więcej
Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2020 Nov 15; Vol. 206, pp. 112793. Date of Electronic Publication: 2020 Sep 06.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Drug Inverse Agonism*
Hypolipidemic Agents/*pharmacology
Lipogenesis/*drug effects
Liver X Receptors/*agonists
Spiro Compounds/*chemistry
Spiro Compounds/*pharmacology
3T3-L1 Cells ; Animals ; Hep G2 Cells ; Humans ; Liver X Receptors/chemistry ; Liver X Receptors/metabolism ; Mice ; Molecular Dynamics Simulation ; Protein Conformation
Czasopismo naukowe
Tytuł :
An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
Autorzy :
Kim J; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea; College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu, 41566, South Korea.
Hwang H; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
Yoon H; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
Lee JE; Department of Biomaterials Science, College of Natural Resources and Life Science/Life and Industry Convergence Research Institute, Pusan National University, Pusan, South Korea.
Oh JM; Department of Nuclear Medicine, School of Medicine, Kyungpook National University Hospital, Daegu, South Korea.
An H; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
Ji HD; Department of Nuclear Medicine, School of Medicine, Kyungpook National University Hospital, Daegu, South Korea.
Lee S; Leading-edge Research Center for Drug Discovery and Development for Diabetes and Metabolic Disease, Kyungpook National University Hospital, Daegu, 41404, South Korea.
Cha E; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
Ma MJ; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
Kim DS; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
Lee SJ; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
Kadayat TM; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
Song J; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
Lee SW; Department of Nuclear Medicine, School of Medicine, Kyungpook National University Hospital, Daegu, South Korea.
Jeon JH; Leading-edge Research Center for Drug Discovery and Development for Diabetes and Metabolic Disease, Kyungpook National University Hospital, Daegu, 41404, South Korea; Department of Internal Medicine, School of Medicine, Kyungpook National University, Daegu, 41944, South Korea.
Park KG; Department of Internal Medicine, School of Medicine, Kyungpook National University, Daegu, 41944, South Korea.
Lee IK; Leading-edge Research Center for Drug Discovery and Development for Diabetes and Metabolic Disease, Kyungpook National University Hospital, Daegu, 41404, South Korea; Department of Internal Medicine, School of Medicine, Kyungpook National University, Daegu, 41944, South Korea.
Jeon YH; Laboratory Animal Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea. Electronic address: .
Chin J; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea. Electronic address: .
Cho SJ; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea; Leading-edge Research Center for Drug Discovery and Development for Diabetes and Metabolic Disease, Kyungpook National University Hospital, Daegu, 41404, South Korea. Electronic address: .
Pokaż więcej
Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2020 Nov 01; Vol. 205, pp. 112501. Date of Electronic Publication: 2020 Jul 14.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Inverse Agonism*
Antineoplastic Agents/*pharmacokinetics
Antineoplastic Agents/*pharmacology
Iodine Radioisotopes/*therapeutic use
Receptors, Estrogen/*antagonists & inhibitors
Thyroid Neoplasms/*drug therapy
Administration, Oral ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/therapeutic use ; Biological Availability ; Cell Line, Tumor ; Humans ; Molecular Docking Simulation ; Protein Conformation ; Receptors, Estrogen/chemistry ; Receptors, Estrogen/metabolism ; Thyroid Neoplasms/pathology ; Thyroid Neoplasms/radiotherapy
Czasopismo naukowe
Tytuł :
A Systematic Review of Inverse Agonism at Adrenoceptor Subtypes.
Autorzy :
Michel MC; Department of Pharmacology, Johannes Gutenberg University, 55131 Mainz, Germany.
Michel-Reher MB; Department of Pharmacology, Johannes Gutenberg University, 55131 Mainz, Germany.
Hein P; TherapeutAix UG, 52066 Aachen, Germany.
Pokaż więcej
Źródło :
Cells [Cells] 2020 Aug 19; Vol. 9 (9). Date of Electronic Publication: 2020 Aug 19.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't; Systematic Review
MeSH Terms :
Drug Inverse Agonism*
Drug Development/*methods
Receptors, Adrenergic, beta-2/*therapeutic use
Humans
Czasopismo naukowe
Tytuł :
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A 2A Receptor.
Autorzy :
Amelia T; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.; School of Pharmacy, Bandung Institute of Technology, Jalan Ganesha 10, 40132 Bandung, Indonesia.
van Veldhoven JPD; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Falsini M; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Liu R; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Heitman LH; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
van Westen GJP; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Segala E; Sosei Heptares, Steinmetz Building, Granta Park, Cambridge CB21 6DG, United Kingdom.
Verdon G; Sosei Heptares, Steinmetz Building, Granta Park, Cambridge CB21 6DG, United Kingdom.
Cheng RKY; Sosei Heptares, Steinmetz Building, Granta Park, Cambridge CB21 6DG, United Kingdom.
Cooke RM; Sosei Heptares, Steinmetz Building, Granta Park, Cambridge CB21 6DG, United Kingdom.
van der Es D; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
IJzerman AP; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 Apr 08; Vol. 64 (7), pp. 3827-3842. Date of Electronic Publication: 2021 Mar 25.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Adenosine A2 Receptor Agonists/*metabolism
Aminopyridines/*metabolism
Pyrimidines/*metabolism
Receptor, Adenosine A2A/*metabolism
Aminopyridines/chemical synthesis ; Animals ; Binding Sites ; CHO Cells ; Cricetulus ; Crystallography, X-Ray ; Drug Inverse Agonism ; Drug Partial Agonism ; HEK293 Cells ; Humans ; Ligands ; Molecular Docking Simulation ; Protein Binding ; Pyrimidines/chemical synthesis ; Small Molecule Libraries/metabolism
Czasopismo naukowe
Tytuł :
Biased agonism at histamine H 1 receptor: Desensitization, internalization and MAPK activation triggered by antihistamines.
Autorzy :
Burghi V; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Buenos Aires, Argentina; Instituto de Investigaciones Farmacológicas (ININFA, UBA, CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Echeverría EB; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Buenos Aires, Argentina; Instituto de Investigaciones Farmacológicas (ININFA, UBA, CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Zappia CD; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Buenos Aires, Argentina; Instituto de Investigaciones Farmacológicas (ININFA, UBA, CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Díaz Nebreda A; Laboratorio de Patología y Farmacología Molecular, Instituto de Biología y Medicina Experimental (IByME-CONICET), Buenos Aires, Argentina.
Ripoll S; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Buenos Aires, Argentina; Instituto de Investigaciones Farmacológicas (ININFA, UBA, CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Gómez N; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Buenos Aires, Argentina; Instituto de Investigaciones Farmacológicas (ININFA, UBA, CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Shayo C; Laboratorio de Patología y Farmacología Molecular, Instituto de Biología y Medicina Experimental (IByME-CONICET), Buenos Aires, Argentina.
Davio CA; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Buenos Aires, Argentina; Instituto de Investigaciones Farmacológicas (ININFA, UBA, CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Monczor F; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Buenos Aires, Argentina; Instituto de Investigaciones Farmacológicas (ININFA, UBA, CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Fernández NC; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Buenos Aires, Argentina; Instituto de Investigaciones Farmacológicas (ININFA, UBA, CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina. Electronic address: .
Pokaż więcej
Źródło :
European journal of pharmacology [Eur J Pharmacol] 2021 Apr 05; Vol. 896, pp. 173913. Date of Electronic Publication: 2021 Jan 26.
Typ publikacji :
Comparative Study; Journal Article
MeSH Terms :
Extracellular Signal-Regulated MAP Kinases/*metabolism
Histamine Agonists/*pharmacology
Histamine H1 Antagonists/*pharmacology
Receptors, Histamine H1/*drug effects
A549 Cells ; Calcium Signaling/drug effects ; Cyclooxygenase 2/genetics ; Cyclooxygenase 2/metabolism ; Drug Inverse Agonism ; Enzyme Activation ; G-Protein-Coupled Receptor Kinase 2/genetics ; G-Protein-Coupled Receptor Kinase 2/metabolism ; GTP-Binding Protein alpha Subunits, Gq-G11/metabolism ; Humans ; Inflammation Mediators/metabolism ; Inositol 1,4,5-Trisphosphate/metabolism ; Interleukin-8/genetics ; Interleukin-8/metabolism ; Ligands ; Phosphorylation ; Protein Transport ; Receptors, Histamine H1/metabolism ; Type C Phospholipases/metabolism
Czasopismo naukowe
Tytuł :
Endocrine effects of the novel ghrelin receptor inverse agonist PF-5190457: Results from a placebo-controlled human laboratory alcohol co-administration study in heavy drinkers.
Autorzy :
Lee MR; Section on Clinical Psychoneuroendocrinology and Neuropsychopharmacology, National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research and National Institute on Drug Abuse Intramural Research Program, National Institutes of Health, Bethesda, MD, USA.
Farokhnia M; Section on Clinical Psychoneuroendocrinology and Neuropsychopharmacology, National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research and National Institute on Drug Abuse Intramural Research Program, National Institutes of Health, Bethesda, MD, USA; Center on Compulsive Behaviors, National Institutes of Health, Bethesda, MD, USA.
Cobbina E; Clinical Pharmacokinetics Research Laboratory, Department of Biomedical & Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI, USA.
Saravanakumar A; Clinical Pharmacokinetics Research Laboratory, Department of Biomedical & Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI, USA.
Li X; Biostatistics and Clinical Epidemiology Service, Clinical Center, National Institutes of Health, Bethesda, MD, USA.
Battista JT; Section on Clinical Psychoneuroendocrinology and Neuropsychopharmacology, National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research and National Institute on Drug Abuse Intramural Research Program, National Institutes of Health, Bethesda, MD, USA.
Farinelli LA; Section on Clinical Psychoneuroendocrinology and Neuropsychopharmacology, National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research and National Institute on Drug Abuse Intramural Research Program, National Institutes of Health, Bethesda, MD, USA.
Akhlaghi F; Clinical Pharmacokinetics Research Laboratory, Department of Biomedical & Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI, USA.
Leggio L; Section on Clinical Psychoneuroendocrinology and Neuropsychopharmacology, National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research and National Institute on Drug Abuse Intramural Research Program, National Institutes of Health, Bethesda, MD, USA; Center on Compulsive Behaviors, National Institutes of Health, Bethesda, MD, USA; Medication Development Program, National Institute on Drug Abuse Intramural Research Program, National Institutes of Health, Baltimore, MD, USA; Center for Alcohol and Addiction Studies, Department of Behavioral and Social Sciences, Brown University, Providence, RI, USA. Electronic address: .
Pokaż więcej
Źródło :
Neuropharmacology [Neuropharmacology] 2020 Jun 15; Vol. 170, pp. 107788. Date of Electronic Publication: 2019 Sep 23.
Typ publikacji :
Clinical Trial, Phase I; Journal Article; Research Support, N.I.H., Extramural; Research Support, N.I.H., Intramural
MeSH Terms :
Drug Inverse Agonism*
Alcoholic Intoxication/*blood
Azetidines/*administration & dosage
Ethanol/*administration & dosage
Ghrelin/*blood
Receptors, Ghrelin/*agonists
Spiro Compounds/*administration & dosage
Adult ; Alcoholic Intoxication/drug therapy ; Dose-Response Relationship, Drug ; Female ; Hormones/blood ; Humans ; Islet Amyloid Polypeptide/blood ; Leptin/blood ; Male ; Prolactin/blood ; Single-Blind Method
Czasopismo naukowe
Tytuł :
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.
Autorzy :
Fischer O; Department of Chemistry and Pharmacy, Pharmaceutical Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.
Hofmann J; Department of Chemistry and Pharmacy, Pharmaceutical Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.
Rampp H; Department of Chemistry and Pharmacy, Pharmaceutical Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.
Kaindl J; Department of Chemistry and Pharmacy, Pharmaceutical Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.
Pratsch G; Department of Chemistry and Pharmacy, Pharmaceutical Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.
Bartuschat A; Department of Chemistry and Pharmacy, Pharmaceutical Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.
Taudte RV; Institute of Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander-Universität Erlangen-Nürnberg, Fahrstr. 17, 91054 Erlangen, Germany.
Fromm MF; Institute of Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander-Universität Erlangen-Nürnberg, Fahrstr. 17, 91054 Erlangen, Germany.
Hübner H; Department of Chemistry and Pharmacy, Pharmaceutical Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.
Gmeiner P; Department of Chemistry and Pharmacy, Pharmaceutical Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.
Heinrich MR; Department of Chemistry and Pharmacy, Pharmaceutical Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Apr 23; Vol. 63 (8), pp. 4349-4369. Date of Electronic Publication: 2020 Apr 09.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Drug Inverse Agonism*
Aminobiphenyl Compounds/*chemistry
Halogens/*chemistry
Muscarinic Agonists/*chemistry
Muscarinic Antagonists/*chemistry
Receptor, Muscarinic M3/*agonists
Receptor, Muscarinic M3/*antagonists & inhibitors
Aminobiphenyl Compounds/pharmacology ; Animals ; Caco-2 Cells ; HEK293 Cells ; Halogens/pharmacology ; Humans ; Male ; Molecular Docking Simulation/methods ; Muscarinic Agonists/metabolism ; Muscarinic Agonists/pharmacology ; Muscarinic Antagonists/pharmacology ; Protein Binding/physiology ; Protein Structure, Secondary ; Rats ; Rats, Sprague-Dawley ; Receptor, Muscarinic M3/metabolism
Czasopismo naukowe
Tytuł :
CB1 Receptor-Dependent and Independent Induction of Lipolysis in Primary Rat Adipocytes by the Inverse Agonist Rimonabant (SR141716A).
Autorzy :
Müller GA; Institute for Diabetes and Obesity (IDO), Helmholtz Diabetes Center (HDC), Helmholtz Zentrum München, German Research Center for Environmental Health (GmbH), 85764 Oberschleissheim, Germany.; German Center for Diabetes Research (DZD), 85764 Oberschleissheim, Germany.; Ludwig-Maximilians-University Munich, Department Biology I, Genetics, 82152 Planegg-Martinsried, Germany.
Herling AW; Sanofi Pharma Germany GmbH, Diabetes Research, 65926 Frankfurt am Main, Germany.
Wied S; Sanofi Pharma Germany GmbH, Diabetes Research, 65926 Frankfurt am Main, Germany.
Müller TD; Institute for Diabetes and Obesity (IDO), Helmholtz Diabetes Center (HDC), Helmholtz Zentrum München, German Research Center for Environmental Health (GmbH), 85764 Oberschleissheim, Germany.; German Center for Diabetes Research (DZD), 85764 Oberschleissheim, Germany.; Department of Pharmacology and Experimental Therapy, Institute of Experimental and Clinical Pharmacology and Toxicology, Eberhard Karls University Hospitals and Clinics, 72074 Tübingen, Germany.
Pokaż więcej
Źródło :
Molecules (Basel, Switzerland) [Molecules] 2020 Feb 18; Vol. 25 (4). Date of Electronic Publication: 2020 Feb 18.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Inverse Agonism*
Lipolysis*
Adipocytes/*metabolism
Receptor, Cannabinoid, CB1/*agonists
Receptor, Cannabinoid, CB1/*metabolism
Rimonabant/*pharmacology
Adipocytes/drug effects ; Animals ; Cell-Free System ; Cells, Cultured ; Cyclic AMP-Dependent Protein Kinases/metabolism ; Enzyme Activation/drug effects ; Lipid Droplets/metabolism ; Male ; Phosphorylation/drug effects ; Rats, Wistar ; Sterol Esterase/metabolism
Czasopismo naukowe
Tytuł :
Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Autorzy :
Yang MG; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Beaudoin-Bertrand M; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Xiao Z; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Marcoux D; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Weigelt CA; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Yip S; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Wu DR; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Ruzanov M; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Sack JS; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Wang J; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Yarde M; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Li S; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Shuster DJ; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Xie JH; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Sherry T; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Obermeier MT; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Fura A; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Stefanski K; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Cornelius G; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Khandelwal P; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Karmakar A; Department of Discovery Synthesis, Biocon Bristol-Myers Squibb Research Centre, Biocon Park, Bommasandra IV Phase, Jigani Link Road, Bengaluru 560099, India.
Basha M; Department of Discovery Synthesis, Biocon Bristol-Myers Squibb Research Centre, Biocon Park, Bommasandra IV Phase, Jigani Link Road, Bengaluru 560099, India.
Babu V; Department of Discovery Synthesis, Biocon Bristol-Myers Squibb Research Centre, Biocon Park, Bommasandra IV Phase, Jigani Link Road, Bengaluru 560099, India.
Gupta AK; Department of Discovery Synthesis, Biocon Bristol-Myers Squibb Research Centre, Biocon Park, Bommasandra IV Phase, Jigani Link Road, Bengaluru 560099, India.
Mathur A; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Salter-Cid L; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Denton R; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Zhao Q; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Dhar TGM; Research and Early Development, Bristol Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 Mar 11; Vol. 64 (5), pp. 2714-2724. Date of Electronic Publication: 2021 Feb 16.
Typ publikacji :
Journal Article
MeSH Terms :
Amides/*therapeutic use
Hydrocarbons, Cyclic/*therapeutic use
Nuclear Receptor Subfamily 1, Group F, Member 3/*antagonists & inhibitors
Psoriasis/*drug therapy
Amides/chemistry ; Amides/pharmacokinetics ; Animals ; Drug Inverse Agonism ; Female ; Humans ; Hydrocarbons, Cyclic/chemistry ; Hydrocarbons, Cyclic/pharmacokinetics ; Interleukin-23 ; Mice, Inbred C57BL ; Microsomes, Liver/metabolism ; Molecular Structure ; Psoriasis/chemically induced ; Rats ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Autorzy :
Marcoux D; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Duan JJ; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Shi Q; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Cherney RJ; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Srivastava AS; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Cornelius L; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Batt DG; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Liu Q; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Beaudoin-Bertrand M; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Weigelt CA; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Khandelwal P; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Vishwakrishnan S; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Selvakumar K; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Karmakar A; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Gupta AK; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Basha M; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Ramlingam S; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Manjunath N; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Vanteru S; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Karmakar S; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Maddala N; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Vetrichelvan M; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Gupta A; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India.
Rampulla RA; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Mathur A; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Yip S; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Li P; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Wu DR; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Khan J; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Ruzanov M; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Sack JS; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Wang J; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Yarde M; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Cvijic ME; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Li S; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Shuster DJ; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Borowski V; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Xie JH; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
McIntyre KW; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Obermeier MT; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Fura A; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Stefanski K; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Cornelius G; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Hynes J Jr; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Tino JA; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Macor JE; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Salter-Cid L; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Denton R; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Zhao Q; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Carter PH; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Dhar TGM; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2019 Nov 14; Vol. 62 (21), pp. 9931-9946. Date of Electronic Publication: 2019 Oct 31.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Drug Inverse Agonism*
Nuclear Receptor Subfamily 1, Group F, Member 3/*agonists
Pyrrolidines/*pharmacology
Animals ; Humans ; Jurkat Cells ; Mice ; Models, Molecular ; Nuclear Receptor Subfamily 1, Group F, Member 3/chemistry ; Protein Conformation ; Pyrrolidines/chemistry ; Pyrrolidines/pharmacokinetics ; Structure-Activity Relationship ; Tissue Distribution
Czasopismo naukowe
Tytuł :
Development of Novel δ Opioid Receptor Inverse Agonists without a Basic Nitrogen Atom and Their Antitussive Effects in Mice.
Autorzy :
Higashi E; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
Hirayama S; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.; Medicinal Research Laboratories, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
Nikaido J; Department of Pathophysiology and Therapeutics , Hoshi University School of Pharmacy and Pharmaceutical Sciences , 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501 , Japan.
Shibasaki M; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
Kono T; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
Honjo A; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
Ikeda H; Department of Pathophysiology and Therapeutics , Hoshi University School of Pharmacy and Pharmaceutical Sciences , 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501 , Japan.
Kamei J; Department of Pathophysiology and Therapeutics , Hoshi University School of Pharmacy and Pharmaceutical Sciences , 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501 , Japan.; Global Research Center for Innovative Life Science , Hoshi University School of Pharmacy and Pharmaceutical Sciences , 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501 , Japan.
Fujii H; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.; Medicinal Research Laboratories, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
Pokaż więcej
Źródło :
ACS chemical neuroscience [ACS Chem Neurosci] 2019 Sep 18; Vol. 10 (9), pp. 3939-3945. Date of Electronic Publication: 2019 Aug 15.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Inverse Agonism*
Nitrogen*
Analgesics, Opioid/*therapeutic use
Antitussive Agents/*therapeutic use
Drug Development/*methods
Receptors, Opioid, delta/*agonists
Analgesics, Opioid/chemistry ; Analgesics, Opioid/metabolism ; Animals ; Antitussive Agents/chemistry ; Antitussive Agents/metabolism ; Citric Acid/toxicity ; Cough/chemically induced ; Cough/drug therapy ; Cough/metabolism ; Dose-Response Relationship, Drug ; Mice ; Receptors, Opioid, delta/metabolism
Czasopismo naukowe
Tytuł :
Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists.
Autorzy :
Amaudrut J; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Argiriadi MA; AbbVie, 381 Plantation Street, Worcester, MA 01605, USA.
Barth M; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Breinlinger EC; AbbVie, 381 Plantation Street, Worcester, MA 01605, USA.
Bressac D; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Broqua P; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Calderwood DJ; AbbVie, 100 Research Drive, Worcester, MA 01605, USA.
Chatar M; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Cusack KP; AbbVie, 381 Plantation Street, Worcester, MA 01605, USA.
Gauld SB; AbbVie, 1 North Waukegan Road, North Chicago, IL 60064, USA.
Jacquet S; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Kamath RV; AbbVie, 100 Research Drive, Worcester, MA 01605, USA.
Kort ME; AbbVie, 1 North Waukegan Road, North Chicago, IL 60064, USA.
Lepais V; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Luccarini JM; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Masson P; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Montalbetti C; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Mounier L; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Potin D; Inventiva, 50 rue de Dijon, 21121 Daix, France. Electronic address: .
Poupardin O; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Rouaud S; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Spitzer L; Inventiva, 50 rue de Dijon, 21121 Daix, France.
Wallace CD; AbbVie, 100 Research Drive, Worcester, MA 01605, USA.
Pokaż więcej
Źródło :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Jul 15; Vol. 29 (14), pp. 1799-1806. Date of Electronic Publication: 2019 May 09.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Inverse Agonism*
Nuclear Receptor Subfamily 1, Group F, Member 3/*chemistry
Quinolines/*chemistry
Animals ; Disease Models, Animal ; Humans ; Mice
Czasopismo naukowe
Tytuł :
Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H 3 receptor antagonists/inverse agonists containing triazole moiety.
Autorzy :
Song M; Medical College, Jinggangshan University, Ji'an, China.
Yan R; Medical College, Jinggangshan University, Ji'an, China.
Zhang Y; Medical College, Jinggangshan University, Ji'an, China.
Guo D; Medical College, Jinggangshan University, Ji'an, China.
Zhou N; College of Life Sciences, Zhejiang University, Hangzhou, China.
Deng X; Medical College, Jinggangshan University, Ji'an, China.
Pokaż więcej
Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 1310-1321.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Anticonvulsants/*chemistry
Histamine H3 Antagonists/*chemistry
Triazoles/*chemistry
Animals ; Anticonvulsants/chemical synthesis ; Anticonvulsants/therapeutic use ; Dose-Response Relationship, Drug ; Drug Inverse Agonism ; Histamine H3 Antagonists/pharmacology ; Mice ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Screening of Focused Compound Library Targeting Liver X Receptors in Pancreatic Cancer Identified Ligands with Inverse Agonist and Degrader Activity.
Autorzy :
Karaboga H
Huang W; College of Pharmacy, Guangxi Medical University, Qingxiu District, Nanning, Guangxi, China.
Srivastava S
Widmann S
Addanki S
Gamage KT
Mazhar Z
Ebalunode JO
Briggs JM
Gustafsson JÅ
Filgueira CS; Department of Nanomedicine, Houston Methodist Research Institute, Houston, Texas 77030, United States.
Gilbertson SR
Lin CY
Pokaż więcej
Źródło :
ACS chemical biology [ACS Chem Biol] 2020 Nov 20; Vol. 15 (11), pp. 2916-2928. Date of Electronic Publication: 2020 Oct 19.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Antineoplastic Agents/*pharmacology
Carcinoma, Pancreatic Ductal/*drug therapy
Liver X Receptors/*metabolism
Pancreatic Neoplasms/*drug therapy
Small Molecule Libraries/*pharmacology
Antineoplastic Agents/chemistry ; Carcinoma, Pancreatic Ductal/metabolism ; Cell Line, Tumor ; Drug Inverse Agonism ; Humans ; Ligands ; Liver X Receptors/agonists ; Pancreatic Neoplasms/metabolism ; Proteolysis/drug effects ; Small Molecule Libraries/chemistry
Czasopismo naukowe
Tytuł :
Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold.
Autorzy :
Haj Salah KB; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Maingot M; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Blayo AL; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
M'Kadmi C; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Damian M; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Mary S; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Cantel S; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Neasta J; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Oiry C; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Péraldi-Roux S; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Fernandez G; Laboratory of Neurophysiology of the Multidisciplinary Institute of Cell, La Plata, Buenos Aires 1900, Argentina.
Romero GG; Laboratory of Neurophysiology of the Multidisciplinary Institute of Cell, La Plata, Buenos Aires 1900, Argentina.
Perello M; Laboratory of Neurophysiology of the Multidisciplinary Institute of Cell, La Plata, Buenos Aires 1900, Argentina.
Marie J; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Banères JL; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Fehrentz JA; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Denoyelle S; IBMM, Univ Montpellier, CNRS, ENSCM, Faculty of Pharmacy, 34000 Montpellier, France.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Oct 08; Vol. 63 (19), pp. 10796-10815. Date of Electronic Publication: 2020 Sep 21.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Receptors, Ghrelin/*agonists
Triazoles/*pharmacology
Animals ; Drug Inverse Agonism ; GTP-Binding Proteins/metabolism ; HEK293 Cells ; Humans ; Insulin Secretion/drug effects ; Islets of Langerhans/drug effects ; Islets of Langerhans/metabolism ; Ligands ; Rats ; Triazoles/chemistry
Czasopismo naukowe
Tytuł :
3-Substituted Quinolines as RORγt Inverse Agonists.
Autorzy :
Tanis VM; Discovery Product Development and Supply, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States. Electronic address: .
Venkatesan H; Discovery Product Development and Supply, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States. Electronic address: .
Cummings MD; Discovery Product Development and Supply, Janssen Research and Development, Welsh and McKean Roads, Spring House, PA 19477, United States. Electronic address: .
Albers M; Department of Research, Phenex Pharmaceuticals AG, Heidelberg, Germany.
Kent Barbay J; Discovery Product Development and Supply, Janssen Research and Development, Welsh and McKean Roads, Spring House, PA 19477, United States.
Herman K; Discovery Immunology, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States.
Kummer DA; Discovery Product Development and Supply, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States.
Milligan C; Discovery Product Development and Supply, Janssen Research and Development, Welsh and McKean Roads, Spring House, PA 19477, United States.
Nelen MI; Discovery Product Development and Supply, Janssen Research and Development, Welsh and McKean Roads, Spring House, PA 19477, United States.
Nishimura R; Discovery Product Development and Supply, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States.
Schlueter T; Department of Research, Phenex Pharmaceuticals AG, Heidelberg, Germany.
Scott B; Discovery Product Development and Supply, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States.
Spurlino J; Discovery Product Development and Supply, Janssen Research and Development, Welsh and McKean Roads, Spring House, PA 19477, United States.
Wolin R; Discovery Product Development and Supply, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States.
Woods C; Discovery Product Development and Supply, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States.
Xue X; Discovery Immunology, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States.
Edwards JP; Discovery Product Development and Supply, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States.
Fourie AM; Discovery Immunology, Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, United States.
Leonard K; Discovery Product Development and Supply, Janssen Research and Development, Welsh and McKean Roads, Spring House, PA 19477, United States.
Pokaż więcej
Źródło :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Jun 15; Vol. 29 (12), pp. 1463-1470. Date of Electronic Publication: 2019 Apr 12.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Inverse Agonism*
Quinolines/*agonists
Animals ; Humans ; Molecular Structure ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Discovery of N-indanyl benzamides as potent RORγt inverse agonists.
Autorzy :
Tian J; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, China.
Sun N; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, China.
Yu M; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, China.
Gu X; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, China.
Xie Q; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, China.
Shao L; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, China.
Liu J; Department of Biology and Pharmacology, Shanghai ChemPartner CO, LTD, 998 Halei Road, Shanghai, 201203, China.
Liu L; State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, 1111 Zhongshan North No. 1 Road, Shanghai, 200437, China. Electronic address: .
Wang Y; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, China. Electronic address: .
Pokaż więcej
Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2019 Apr 01; Vol. 167, pp. 37-48. Date of Electronic Publication: 2019 Feb 04.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Discovery*
Drug Inverse Agonism*
Benzamides/*pharmacology
Nuclear Receptor Subfamily 1, Group F, Member 3/*agonists
Animals ; Autoimmune Diseases/drug therapy ; Binding Sites ; Cell Differentiation/drug effects ; Fluorescence Resonance Energy Transfer ; Indans/chemistry ; Inhibitory Concentration 50 ; Mice ; Stereoisomerism ; Structure-Activity Relationship ; Th17 Cells/cytology
Czasopismo naukowe
Tytuł :
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
Autorzy :
Yukawa T; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Nara Y; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Kono M; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Sato A; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Oda T; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Takagi T; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Sato T; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Banno Y; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Taya N; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Imada T; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Shiokawa Z; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Negoro N; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Kawamoto T; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Koyama R; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Uchiyama N; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Skene R; Takeda California , 9625 Towne Centre Drive , San Diego , California 92121 , United States.
Hoffman I; Takeda California , 9625 Towne Centre Drive , San Diego , California 92121 , United States.
Chen CH; Takeda California , 9625 Towne Centre Drive , San Diego , California 92121 , United States.
Sang B; Takeda California , 9625 Towne Centre Drive , San Diego , California 92121 , United States.
Snell G; Takeda California , 9625 Towne Centre Drive , San Diego , California 92121 , United States.
Katsuyama R; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Yamamoto S; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Shirai J; Pharmaceutical Research Division , Takeda Pharmaceutical Company Limited , 26-1 Muraoka-Higashi 2-chome , Fujisawa , Kanagawa 251-8555 , Japan.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2019 Feb 14; Vol. 62 (3), pp. 1167-1179. Date of Electronic Publication: 2019 Feb 04.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Drug Design*
Drug Inverse Agonism*
Nuclear Receptor Subfamily 1, Group F, Member 3/*agonists
Animals ; High-Throughput Screening Assays ; Molecular Dynamics Simulation ; Structure-Activity Relationship ; Th17 Cells/drug effects
Czasopismo naukowe

Ta witryna wykorzystuje pliki cookies do przechowywania informacji na Twoim komputerze. Pliki cookies stosujemy w celu świadczenia usług na najwyższym poziomie, w tym w sposób dostosowany do indywidualnych potrzeb. Korzystanie z witryny bez zmiany ustawień dotyczących cookies oznacza, że będą one zamieszczane w Twoim komputerze. W każdym momencie możesz dokonać zmiany ustawień dotyczących cookies