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Tytuł:
Simultaneous Imaging and Therapy Using Epitope-Specific Anti-Epidermal Growth Factor Receptor (EGFR) Antibody Conjugates.
Autorzy:
Tikum, Anjong Florence (AUTHOR)
Nambisan, Anand Krishnan (AUTHOR)
Ketchemen, Jessica Pougoue (AUTHOR)
Babeker, Hanan (AUTHOR)
Khan, Musharraf N. (AUTHOR)
Torlakovic, Emina E. (AUTHOR)
Fonge, Humphrey (AUTHOR)
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Źródło:
Pharmaceutics. Sep2022, Vol. 14 Issue 9, pN.PAG-N.PAG. 17p.
Czasopismo naukowe
Tytuł:
Kinetic profiling and functional characterization of 8-phenylxanthine derivatives as A 2B adenosine receptor antagonists.
Autorzy:
Vlachodimou A; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, the Netherlands.
de Vries H; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, the Netherlands.
Pasoli M; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, the Netherlands.
Goudswaard M; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, the Netherlands.
Kim SA; Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, 9000 Rockville Pike, Bethesda, MD 20892, USA.
Kim YC; Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, 9000 Rockville Pike, Bethesda, MD 20892, USA.
Scortichini M; Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, 9000 Rockville Pike, Bethesda, MD 20892, USA.
Marshall M; Department of Internal Medicine and Molecular Physiology & Biological Physics, University of Virginia Health Science Center, Charlottesville, VA 22908, USA.
Linden J; Department of Internal Medicine and Molecular Physiology & Biological Physics, University of Virginia Health Science Center, Charlottesville, VA 22908, USA.
Heitman LH; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, the Netherlands; Oncode Institute, Leiden, the Netherlands.
Jacobson KA; Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, 9000 Rockville Pike, Bethesda, MD 20892, USA. Electronic address: .
IJzerman AP; Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, the Netherlands. Electronic address: .
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Źródło:
Biochemical pharmacology [Biochem Pharmacol] 2022 Jun; Vol. 200, pp. 115027. Date of Electronic Publication: 2022 Apr 06.
Typ publikacji:
Journal Article; Research Support, N.I.H., Intramural
MeSH Terms:
Purinergic P1 Receptor Antagonists*
Xanthines*/pharmacology
Adenosine A2 Receptor Antagonists/pharmacology ; Kinetics ; Radioligand Assay ; Receptor, Adenosine A2B/metabolism ; Receptors, Purinergic P1/metabolism
Czasopismo naukowe
Tytuł:
In Vitro, In Vivo and In Silico Characterization of a Novel Kappa-Opioid Receptor Antagonist.
Autorzy:
Puls, Kristina (AUTHOR)
Olivé-Marti, Aina-Leonor (AUTHOR)
Pach, Szymon (AUTHOR)
Pinter, Birgit (AUTHOR)
Erli, Filippo (AUTHOR)
Wolber, Gerhard (AUTHOR)
Spetea, Mariana (AUTHOR)
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Źródło:
Pharmaceuticals (14248247). Jun2022, Vol. 15 Issue 6, p680-N.PAG. 21p.
Czasopismo naukowe
Tytuł:
Effects of Rare Phytocannabinoids on the Endocannabinoid System of Human Keratinocytes.
Autorzy:
Di Meo, Camilla (AUTHOR)
Tortolani, Daniel (AUTHOR)
Standoli, Sara (AUTHOR)
Angelucci, Clotilde Beatrice (AUTHOR)
Fanti, Federico (AUTHOR)
Leuti, Alessandro (AUTHOR)
Sergi, Manuel (AUTHOR)
Kadhim, Salam (AUTHOR)
Hsu, Eric (AUTHOR)
Rapino, Cinzia (AUTHOR)
Maccarrone, Mauro (AUTHOR)
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Źródło:
International Journal of Molecular Sciences. May2022, Vol. 23 Issue 10, p5430-5430. 19p.
Czasopismo naukowe
Tytuł:
Evaluation of the PSMA-Binding Ligand Pb-NG001 in Multicellular Tumour Spheroid and Mouse Models of Prostate Cancer.
Autorzy:
Stenberg VY; Department of Radiation Biology, Institute for Cancer Research, The Norwegian Radium Hospital, Oslo University Hospital, 0379 Oslo, Norway.; Department of Research and Development, Nucligen AS, 0379 Oslo, Norway.; Institute for Clinical Medicine, University of Oslo, 0318 Oslo, Norway.
Larsen RH; Department of Research and Development, Nucligen AS, 0379 Oslo, Norway.
Ma LW; Department of Radiation Biology, Institute for Cancer Research, The Norwegian Radium Hospital, Oslo University Hospital, 0379 Oslo, Norway.
Peng Q; Department of Pathology, The Norwegian Radium Hospital, Oslo University Hospital, 0379 Oslo, Norway.
Juzenas P; Department of Pathology, The Norwegian Radium Hospital, Oslo University Hospital, 0379 Oslo, Norway.
Bruland ØS; Institute for Clinical Medicine, University of Oslo, 0318 Oslo, Norway.; Department of Oncology, The Norwegian Radium Hospital, Oslo University Hospital, 0379 Oslo, Norway.
Juzeniene A; Department of Radiation Biology, Institute for Cancer Research, The Norwegian Radium Hospital, Oslo University Hospital, 0379 Oslo, Norway.
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Źródło:
International journal of molecular sciences [Int J Mol Sci] 2021 May 01; Vol. 22 (9). Date of Electronic Publication: 2021 May 01.
Typ publikacji:
Journal Article
MeSH Terms:
Radioligand Assay*
Prostatic Neoplasms, Castration-Resistant/*radiotherapy
Radiopharmaceuticals/*pharmacology
Spheroids, Cellular/*radiation effects
Animals ; Cell Line, Tumor ; Disease Models, Animal ; Heterografts ; Humans ; Lead/pharmacology ; Ligands ; Male ; Mice ; Neoplasm Metastasis ; Prostatic Neoplasms, Castration-Resistant/pathology ; Radioisotopes/pharmacology ; Spheroids, Cellular/pathology ; Tissue Distribution/radiation effects
Czasopismo naukowe
Tytuł:
Exploration of Diazaspiro Cores as Piperazine Bioisosteres in the Development of σ2 Receptor Ligands.
Autorzy:
Xu K; Department of Radiology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.
Hsieh CJ; Department of Radiology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.
Lee JY; Department of Radiology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.
Riad A; Department of Radiology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.
Izzo NJ; Cognition Therapeutics Inc., Pittsburgh, PA 15203, USA.
Look G; Cognition Therapeutics Inc., Pittsburgh, PA 15203, USA.
Catalano S; Cognition Therapeutics Inc., Pittsburgh, PA 15203, USA.
Mach RH; Department of Radiology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.
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Źródło:
International journal of molecular sciences [Int J Mol Sci] 2022 Jul 27; Vol. 23 (15). Date of Electronic Publication: 2022 Jul 27.
Typ publikacji:
Journal Article
MeSH Terms:
Receptors, sigma*/metabolism
Ligands ; Piperazine ; Radioligand Assay ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł:
New class of benzothiophene morpholine analogues with high selectivity and affinity were designed and evaluated for anti-drug addiction.
Autorzy:
Cai J; School of Chemistry and Chemical Engineering, Southeast University, Nanjing, Jiangsu, China.
Wang Y; School of Chemistry and Chemical Engineering, Southeast University, Nanjing, Jiangsu, China.
Chen X; School of Chemistry and Chemical Engineering, Southeast University, Nanjing, Jiangsu, China.
Ji M; School of Biological Science and Medical Engineering, Southeast University, Nanjing, China.
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Źródło:
Chemical biology & drug design [Chem Biol Drug Des] 2022 Apr; Vol. 99 (4), pp. 634-649. Date of Electronic Publication: 2022 Feb 25.
Typ publikacji:
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms:
Receptors, Dopamine D3*/chemistry
Substance-Related Disorders*
Animals ; Ligands ; Mice ; Morpholines/pharmacology ; Radioligand Assay ; Structure-Activity Relationship ; Thiophenes
Czasopismo naukowe
Tytuł:
Development of Bicyclo[3.1.0]hexane-Based A 3 Receptor Ligands: Closing the Gaps in the Structure-Affinity Relationships.
Autorzy:
Lemmerhirt JP; European Institute for Molecular Imaging (EIMI), University of Münster, Waldeyerstr. 15, 48149 Münster, Germany.
Isaak A; European Institute for Molecular Imaging (EIMI), University of Münster, Waldeyerstr. 15, 48149 Münster, Germany.
Liu R; Leiden Academic Centre for Drug Research (LACDR), Division of Medicinal Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Kock M; European Institute for Molecular Imaging (EIMI), University of Münster, Waldeyerstr. 15, 48149 Münster, Germany.
Daniliuc CG; Organisch-Chemisches Institut, University of Münster, Corrensstraße 40, 48149 Münster, Germany.
Jacobson KA; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.
Heitman LH; Leiden Academic Centre for Drug Research (LACDR), Division of Medicinal Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Junker A; European Institute for Molecular Imaging (EIMI), University of Münster, Waldeyerstr. 15, 48149 Münster, Germany.
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Źródło:
Molecules (Basel, Switzerland) [Molecules] 2022 Mar 31; Vol. 27 (7). Date of Electronic Publication: 2022 Mar 31.
Typ publikacji:
Journal Article
MeSH Terms:
Hexanes*
Receptor, Adenosine A3*/chemistry
Animals ; CHO Cells ; Cricetinae ; Ligands ; Nucleosides/chemistry ; Radioligand Assay ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł:
Could Fibroblast Activation Protein (FAP)-Specific Radioligands Be Considered as Pan-Tumor Agents?
Autorzy:
Roustaei H; Nuclear Medicine Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
Kiamanesh Z; Nuclear Medicine Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
Askari E; Nuclear Medicine Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
Sadeghi R; Nuclear Medicine Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
Aryana K; Nuclear Medicine Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
Treglia G; Ente Ospedaliero Cantonale, Bellinzona, Switzerland.; Faculty of Biomedical Sciences, Universitá della Svizzera italiana, Lugano, Switzerland.; Faculty of Biology and Medicine, University of Lausanne, Lausanne, Switzerland.
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Źródło:
Contrast media & molecular imaging [Contrast Media Mol Imaging] 2022 Feb 22; Vol. 2022, pp. 3948873. Date of Electronic Publication: 2022 Feb 22 (Print Publication: 2022).
Typ publikacji:
Journal Article; Meta-Analysis; Systematic Review
MeSH Terms:
Endopeptidases*
Membrane Proteins*
Positron Emission Tomography Computed Tomography*
Fluorodeoxyglucose F18 ; Gallium Radioisotopes ; Humans ; Ligands ; Radioligand Assay
Czasopismo naukowe
Tytuł:
Synthesis and Characterization of a Specific Iodine-125-Labeled TRPC5 Radioligand.
Autorzy:
Yu Y; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
Liang Q; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
Du L; Department of Anesthesiology, Center for the Study of Itch, Washington University School of Medicine, St. Louis, MO 63110, USA.
Jiang H; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
Gu J; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
Hu H; Department of Anesthesiology, Center for the Study of Itch, Washington University School of Medicine, St. Louis, MO 63110, USA.
Tu Z; Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
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Źródło:
ChemMedChem [ChemMedChem] 2020 Oct 05; Vol. 15 (19), pp. 1854-1860. Date of Electronic Publication: 2020 Sep 02.
Typ publikacji:
Journal Article; Research Support, N.I.H., Extramural
MeSH Terms:
Radioligand Assay*
Radiopharmaceuticals/*pharmacology
TRPC Cation Channels/*antagonists & inhibitors
Animals ; Brain/metabolism ; Calcium/analysis ; Calcium/metabolism ; Cells, Cultured ; Dose-Response Relationship, Drug ; HEK293 Cells ; Humans ; Iodine Radioisotopes ; Molecular Structure ; Positron-Emission Tomography ; Radiopharmaceuticals/chemical synthesis ; Radiopharmaceuticals/chemistry ; Rats ; TRPC Cation Channels/chemistry ; TRPC Cation Channels/metabolism
Czasopismo naukowe
Tytuł:
Heterobivalent Ligand for the Adenosine A 2A -Dopamine D 2 Receptor Heteromer.
Autorzy:
Pulido D; Biomedical Research Networking Center in Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), 08034 Barcelona, Spain.; Department of Surfactants and Nanobiotechnology, Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), 08034 Barcelona, Spain.
Casadó-Anguera V; Department of Biochemistry and Molecular Biomedicine, Faculty of Biology, Institute of Biomedicine of the University of Barcelona (IBUB), University of Barcelona, 08028 Barcelona, Spain.
Gómez-Autet M; Laboratori de Medicina Computacional, Unitat de Bioestadística, Facultat de Medicina, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain.
Llopart N; Department of Biochemistry and Molecular Biomedicine, Faculty of Biology, Institute of Biomedicine of the University of Barcelona (IBUB), University of Barcelona, 08028 Barcelona, Spain.
Moreno E; Department of Biochemistry and Molecular Biomedicine, Faculty of Biology, Institute of Biomedicine of the University of Barcelona (IBUB), University of Barcelona, 08028 Barcelona, Spain.
Casajuana-Martin N; Laboratori de Medicina Computacional, Unitat de Bioestadística, Facultat de Medicina, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain.
Ferré S; Integrative Neurobiology Section, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, Baltimore, Maryland 21224, United States.
Pardo L; Laboratori de Medicina Computacional, Unitat de Bioestadística, Facultat de Medicina, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain.
Casadó V; Department of Biochemistry and Molecular Biomedicine, Faculty of Biology, Institute of Biomedicine of the University of Barcelona (IBUB), University of Barcelona, 08028 Barcelona, Spain.
Royo M; Biomedical Research Networking Center in Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), 08034 Barcelona, Spain.; Department of Surfactants and Nanobiotechnology, Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), 08034 Barcelona, Spain.
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Źródło:
Journal of medicinal chemistry [J Med Chem] 2022 Jan 13; Vol. 65 (1), pp. 616-632. Date of Electronic Publication: 2022 Jan 04.
Typ publikacji:
Journal Article; Research Support, N.I.H., Intramural; Research Support, Non-U.S. Gov't
MeSH Terms:
Receptor, Adenosine A2A/*drug effects
Receptors, Dopamine D2/*drug effects
Animals ; Binding Sites ; CHO Cells ; Cricetinae ; Cricetulus ; Drug Design ; Humans ; Ligands ; Molecular Dynamics Simulation ; Radioligand Assay
Czasopismo naukowe
Tytuł:
Comparative characterization of β-adrenoceptors in the bladder, heart, and lungs of rats: Alterations in spontaneously hypertensive rats.
Autorzy:
Yamada S; Center for Pharma-Food Research (CPFR), Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan. Electronic address: .
Niiya R; Laboratory of Biopharmacy, Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
Ito Y; Center for Pharma-Food Research (CPFR), Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
Kato Y; Kagawa School of Pharmaceutical Sciences, Tokushima Bunri University, 1314-1, Shido, Sanuki, Kagawa 769-2193, Japan.
Onoue S; Laboratory of Biopharmacy, Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
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Źródło:
Journal of pharmacological sciences [J Pharmacol Sci] 2022 Jan; Vol. 148 (1), pp. 51-55. Date of Electronic Publication: 2021 Oct 09.
Typ publikacji:
Comparative Study; Journal Article
MeSH Terms:
Lung/*metabolism
Myocardium/*metabolism
Rats, Inbred SHR/*metabolism
Receptors, Adrenergic, beta/*metabolism
Urinary Bladder/*metabolism
Animals ; Radioligand Assay/methods ; Rats, Inbred WKY ; Rats, Sprague-Dawley ; Rats, Wistar ; Receptors, Adrenergic, beta-1/metabolism ; Receptors, Adrenergic, beta-3/metabolism
Czasopismo naukowe
Tytuł:
Indole-Containing Amidinohydrazones as Nonpeptide, Dual RXFP3/4 Agonists: Synthesis, Structure-Activity Relationship, and Molecular Modeling Studies.
Autorzy:
Guan D; Center for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Rahman MT; Center for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Gay EA; Center for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Vasukuttan V; Center for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Mathews KM; Center for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Decker AM; Center for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Williams AH; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536, United States.
Zhan CG; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536, United States.
Jin C; Center for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
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Źródło:
Journal of medicinal chemistry [J Med Chem] 2021 Dec 23; Vol. 64 (24), pp. 17866-17886. Date of Electronic Publication: 2021 Dec 02.
Typ publikacji:
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms:
Hydrazones/*pharmacology
Indoles/*chemistry
Receptors, G-Protein-Coupled/*agonists
Receptors, Peptide/*agonists
Humans ; Hydrazones/chemical synthesis ; Hydrazones/chemistry ; Models, Molecular ; Radioligand Assay ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł:
Histatin-1 is an endogenous ligand of the sigma-2 receptor.
Autorzy:
Son KN; Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, IL, USA.
Lee H; Department of Pharmaceutical Science and Biophysics Core at Research Resources Center, University of Illinois at Chicago, IL, USA.
Shah D; Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, IL, USA.
Kalmodia S; Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, IL, USA.
Miller RC; Department of Chemical & Biomolecular Engineering, University of Illinois at Urbana-Champaign, IL, USA.
Ali M; Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, IL, USA.
Balasubramaniam A; Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, IL, USA.
Cologna SM; Department of Chemistry, University of Illinois at Chicago, IL, USA.
Kong H; Department of Chemical & Biomolecular Engineering, University of Illinois at Urbana-Champaign, IL, USA.
Shukla D; Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, IL, USA.
Aakalu VK; Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, IL, USA.
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Źródło:
The FEBS journal [FEBS J] 2021 Dec; Vol. 288 (23), pp. 6815-6827. Date of Electronic Publication: 2021 Jul 23.
Typ publikacji:
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms:
Cell Membrane/*metabolism
Histatins/*metabolism
Radioligand Assay/*methods
Receptors, sigma/*metabolism
Amino Acid Sequence ; Cell Movement ; Cells, Cultured ; Epithelial Cells/metabolism ; Epithelium, Corneal/cytology ; HEK293 Cells ; HeLa Cells ; Histatins/genetics ; Humans ; Ligands ; Membrane Proteins/genetics ; Membrane Proteins/metabolism ; Microscopy, Confocal ; Protein Binding ; Receptors, sigma/genetics
Czasopismo naukowe
Tytuł:
Chiral Cyclic Aliphatic Linkers as Building Blocks for Selective Dopamine D 2 or D 3 Receptor Agonists.
Autorzy:
Battiti FO; Medicinal Chemistry Section, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse─Intramural Research Program, National Institutes of Health, 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Zaidi SA; Department of Quantitative and Computational Biology, USC Michelson Center, University of Southern California, Los Angeles, California 90089, United States.; Department of Chemistry, Bridge Institute, University of Southern California, Los Angeles, California 90089, United States.
Katritch V; Department of Chemistry, Bridge Institute, University of Southern California, Los Angeles, California 90089, United States.
Newman AH; Medicinal Chemistry Section, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse─Intramural Research Program, National Institutes of Health, 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Bonifazi A; Medicinal Chemistry Section, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse─Intramural Research Program, National Institutes of Health, 333 Cassell Drive, Baltimore, Maryland 21224, United States.
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Źródło:
Journal of medicinal chemistry [J Med Chem] 2021 Nov 11; Vol. 64 (21), pp. 16088-16105. Date of Electronic Publication: 2021 Oct 26.
Typ publikacji:
Journal Article; Research Support, N.I.H., Intramural
MeSH Terms:
Dopamine Agonists/*pharmacology
Receptors, Dopamine D2/*drug effects
Receptors, Dopamine D3/*drug effects
Dopamine Agonists/chemistry ; HEK293 Cells ; Humans ; Ligands ; Molecular Docking Simulation ; Radioligand Assay ; Stereoisomerism
Czasopismo naukowe
Tytuł:
Pharmacological characterization of mutant huntingtin aggregate-directed PET imaging tracer candidates.
Autorzy:
Herrmann F; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Hessmann M; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Schaertl S; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Berg-Rosseburg K; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Brown CJ; Evotec (U.K.) Ltd., 114 Innovation Drive, Milton Park, Abingdon, OX14 4RZ, UK.
Bursow G; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Chiki A; Laboratory of Molecular and Chemical Biology of Neurodegeneration, Brain Mind Institute, Ecole Polytechnique Fédérale de Lausanne (EPFL), 1015, Lausanne, Switzerland.
Ebneth A; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Gehrmann M; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Hoeschen N; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Hotze M; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Jahn S; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Johnson PD; Evotec (U.K.) Ltd., 114 Innovation Drive, Milton Park, Abingdon, OX14 4RZ, UK.
Khetarpal V; CHDI Management/CHDI Foundation, 6080 Center Drive, Suite 700, Los Angeles, CA, 90045, USA.
Kiselyov A; CHDI Management/CHDI Foundation, 6080 Center Drive, Suite 700, Los Angeles, CA, 90045, USA.
Kottig K; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Ladewig S; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Lashuel H; Laboratory of Molecular and Chemical Biology of Neurodegeneration, Brain Mind Institute, Ecole Polytechnique Fédérale de Lausanne (EPFL), 1015, Lausanne, Switzerland.
Letschert S; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Mills MR; Evotec (U.K.) Ltd., 114 Innovation Drive, Milton Park, Abingdon, OX14 4RZ, UK.
Petersen K; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Prime ME; Evotec (U.K.) Ltd., 114 Innovation Drive, Milton Park, Abingdon, OX14 4RZ, UK.
Scheich C; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Schmiedel G; Evotec SE, Essener Bogen 7, 22419, Hamburg, Germany.
Wityak J; CHDI Management/CHDI Foundation, 6080 Center Drive, Suite 700, Los Angeles, CA, 90045, USA.
Liu L; CHDI Management/CHDI Foundation, 6080 Center Drive, Suite 700, Los Angeles, CA, 90045, USA.
Dominguez C; CHDI Management/CHDI Foundation, 6080 Center Drive, Suite 700, Los Angeles, CA, 90045, USA.
Muñoz-Sanjuán I; CHDI Management/CHDI Foundation, 6080 Center Drive, Suite 700, Los Angeles, CA, 90045, USA.
Bard JA; CHDI Management/CHDI Foundation, 6080 Center Drive, Suite 700, Los Angeles, CA, 90045, USA. .
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Źródło:
Scientific reports [Sci Rep] 2021 Sep 09; Vol. 11 (1), pp. 17977. Date of Electronic Publication: 2021 Sep 09.
Typ publikacji:
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms:
Huntingtin Protein/*metabolism
Huntington Disease/*metabolism
Positron-Emission Tomography/*methods
Protein Aggregates/*genetics
Protein Aggregation, Pathological/*diagnostic imaging
Radiopharmaceuticals/*metabolism
Alzheimer Disease/metabolism ; Alzheimer Disease/pathology ; Animals ; Autoradiography/methods ; Brain/metabolism ; Disease Models, Animal ; Humans ; Huntingtin Protein/genetics ; Huntington Disease/pathology ; Immunohistochemistry/methods ; Mice ; Mice, Transgenic ; Nitrogen Radioisotopes/metabolism ; Radioactive Tracers ; Radioligand Assay/methods ; Recombinant Proteins/metabolism
Czasopismo naukowe
Tytuł:
Identification and Characterization of Cannabidiol as an OX1R Antagonist by Computational and In Vitro Functional Validation.
Autorzy:
Vitale RM; Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.
Iannotti FA; Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.; Endocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.
Schiano Moriello A; Endocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.; Epitech Group SpA, Saccolongo, 35100 Padova, Italy.
Tunisi L; Endocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.; Department of Veterinary Medicine and Animal Productions, University of Naples Federico II, 80131 Naples, Italy.
Piscitelli F; Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.; Endocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.
Savopoulos R; GW Research Ltd., Sovereign House, Vision Park, Histon, Cambridge CB24 9BZ, UK.
Cristino L; Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.; Endocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.
De Petrocellis L; Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.; Endocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.
Amodeo P; Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.
Gray R; GW Research Ltd., Sovereign House, Vision Park, Histon, Cambridge CB24 9BZ, UK.
Di Marzo V; Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.; Endocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli, Italy.; Canada Excellence Research Chair on the Microbiome-Endocannabinoidome Axis in Metabolic Health (CERC-MEND), Université Laval, Quebec City, QC G1V 4G5, Canada.
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Źródło:
Biomolecules [Biomolecules] 2021 Aug 01; Vol. 11 (8). Date of Electronic Publication: 2021 Aug 01.
Typ publikacji:
Journal Article; Research Support, Non-U.S. Gov't; Validation Study
MeSH Terms:
Anti-Anxiety Agents/*pharmacology
Anticonvulsants/*pharmacology
Cannabidiol/*pharmacology
Orexin Receptors/*chemistry
Orexins/*chemistry
Animals ; Anti-Anxiety Agents/chemistry ; Anti-Anxiety Agents/metabolism ; Anticonvulsants/chemistry ; Anticonvulsants/metabolism ; Binding Sites ; CHO Cells ; Calcium/metabolism ; Cannabidiol/chemistry ; Cannabidiol/metabolism ; Cricetulus ; Gene Expression ; Humans ; Kinetics ; Molecular Docking Simulation ; Molecular Imaging ; Orexin Receptor Antagonists ; Orexin Receptors/genetics ; Orexin Receptors/metabolism ; Orexins/metabolism ; Protein Binding ; Protein Conformation, alpha-Helical ; Protein Conformation, beta-Strand ; Protein Interaction Domains and Motifs ; Radioligand Assay ; Transgenes
Czasopismo naukowe
Tytuł:
A radioligand receptor binding assay for measuring of insulin secreted by MIN6 cells after stimulation with glucose, arginine, ornithine, dopamine, and serotonin.
Autorzy:
Asai, Seiya (AUTHOR)
Žáková, Lenka (AUTHOR)
Selicharová, Irena (AUTHOR)
Marek, Aleš (AUTHOR)
Jiráček, Jiří (AUTHOR)
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Źródło:
Analytical & Bioanalytical Chemistry. Jul2021, Vol. 413 Issue 17, p4531-4543. 13p.
Czasopismo naukowe
Tytuł:
Novel High Affinity Sigma-1 Receptor Ligands from Minimal Ensemble Docking-Based Virtual Screening.
Autorzy:
Dvorácskó S; Biological Research Centre, Institute of Biochemistry, Eötvös Loránd Research Network (ELKH), H-6726 Szeged, Hungary.
Lázár L; Institute of Pharmaceutical Chemistry, University of Szeged, H-6720 Szeged, Hungary.
Fülöp F; Institute of Pharmaceutical Chemistry, University of Szeged, H-6720 Szeged, Hungary.
Palkó M; Institute of Pharmaceutical Chemistry, University of Szeged, H-6720 Szeged, Hungary.
Zalán Z; Institute of Pharmaceutical Chemistry, University of Szeged, H-6720 Szeged, Hungary.
Penke B; Department of Medical Chemistry, University of Szeged, H-6720 Szeged, Hungary.
Fülöp L; Department of Medical Chemistry, University of Szeged, H-6720 Szeged, Hungary.
Tömböly C; Biological Research Centre, Institute of Biochemistry, Eötvös Loránd Research Network (ELKH), H-6726 Szeged, Hungary.
Bogár F; Department of Medical Chemistry, University of Szeged, H-6720 Szeged, Hungary.; MTA-SZTE Biomimetic Systems Research Group, Eötvös Loránd Research Network (ELKH), H-6720 Szeged, Hungary.
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Źródło:
International journal of molecular sciences [Int J Mol Sci] 2021 Jul 29; Vol. 22 (15). Date of Electronic Publication: 2021 Jul 29.
Typ publikacji:
Journal Article
MeSH Terms:
Isoxazoles/*chemistry
Molecular Docking Simulation/*methods
Pentazocine/*chemistry
Pyridines/*chemistry
Receptors, sigma/*chemistry
Binding Sites ; Hydrophobic and Hydrophilic Interactions ; Isoxazoles/analysis ; Isoxazoles/pharmacology ; Ligands ; Molecular Structure ; Pentazocine/analysis ; Pentazocine/pharmacology ; Protein Binding ; Pyridines/analysis ; Pyridines/pharmacology ; Radioligand Assay/methods ; Receptors, sigma/agonists ; Receptors, sigma/analysis ; Receptors, sigma/antagonists & inhibitors
Czasopismo naukowe
Tytuł:
Synthesis and Characterization of Azido Aryl Analogs of IBNtxA for Radio-Photoaffinity Labeling Opioid Receptors in Cell Lines and in Mouse Brain.
Autorzy:
Grinnell SG; Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center, New York, NY, USA. .; Neuroscience Graduate Program, Weill Cornell Graduate School of Medical Sciences, New York, NY, USA. .
Uprety R; Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center, New York, NY, USA.
Varadi A; Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center, New York, NY, USA.; Neuroscience Graduate Program, Weill Cornell Graduate School of Medical Sciences, New York, NY, USA.
Subrath J; Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center, New York, NY, USA.
Hunkele A; Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center, New York, NY, USA.
Pan YX; Department of Neurology, Memorial Sloan-Kettering Cancer Center, New York, NY, USA.; Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center, New York, NY, USA.
Pasternak GW; Department of Neurology, Memorial Sloan-Kettering Cancer Center, New York, NY, USA.; Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center, New York, NY, USA.; Neuroscience Graduate Program, Weill Cornell Graduate School of Medical Sciences, New York, NY, USA.; Pharmacology Graduate Program, Weill Cornell Graduate School of Medical Sciences, New York, NY, USA.
Majumdar S; Center for Clinical Pharmacology, St Louis College of Pharmacy and Washington University School of Medicine, St Louis, MO, USA. .
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Źródło:
Cellular and molecular neurobiology [Cell Mol Neurobiol] 2021 Jul; Vol. 41 (5), pp. 977-993. Date of Electronic Publication: 2020 May 18.
Typ publikacji:
Journal Article
MeSH Terms:
Analgesics, Opioid/*metabolism
Azides/*metabolism
Brain/*metabolism
Naltrexone/*analogs & derivatives
Photoaffinity Labels/*metabolism
Receptors, Opioid/*metabolism
Analgesics, Opioid/chemical synthesis ; Animals ; Azides/chemical synthesis ; Brain/drug effects ; CHO Cells ; Cell Line ; Cricetinae ; Cricetulus ; Dose-Response Relationship, Drug ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Naltrexone/chemical synthesis ; Naltrexone/metabolism ; Photoaffinity Labels/chemical synthesis ; Protein Binding/physiology ; Radioligand Assay/methods
Czasopismo naukowe

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