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Tytuł :
Identification and characterization of a wolfberry carboxypeptidase inhibitor from Lycium barbarum.
Autorzy :
Huang J; School of Biological Sciences, Nanyang Technological University, Singapore 637551, Singapore. Electronic address: .
Wong KH; School of Biological Sciences, Nanyang Technological University, Singapore 637551, Singapore. Electronic address: .
Tan WL; School of Biological Sciences, Nanyang Technological University, Singapore 637551, Singapore. Electronic address: .
Tay SV; School of Biological Sciences, Nanyang Technological University, Singapore 637551, Singapore. Electronic address: .
Wang S; China R&D and Scientific Affair, Shanghai Discovery Center, Janssen Research & Development, Johnson & Johnson, Shanghai 200030, China. Electronic address: .
Tam JP; School of Biological Sciences, Nanyang Technological University, Singapore 637551, Singapore. Electronic address: .
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Źródło :
Food chemistry [Food Chem] 2021 Jul 30; Vol. 351, pp. 129338. Date of Electronic Publication: 2021 Feb 19.
Typ publikacji :
Journal Article
MeSH Terms :
Carboxypeptidases/*antagonists & inhibitors
Enzyme Inhibitors/*pharmacology
Lycium/*chemistry
Peptides/*pharmacology
Cysteine ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/metabolism ; Lycium/metabolism ; Peptides/chemistry ; Peptides/metabolism ; Proteomics
Czasopismo naukowe
Tytuł :
Inactivation Mechanism of Neuronal Nitric Oxide Synthase by ( S )-2-Amino-5-(2-(methylthio)acetimidamido)pentanoic Acid: Chemical Conversion of the Inactivator in the Active Site.
Autorzy :
Yan L; School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China.
Wang Y; School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China.
Zhang S; School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China.
Li X; School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China.
Wei J; School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China.
Wang Z; Institute of Ageing Research, School of Medicine, Hangzhou Normal University, Hangzhou, Zhejiang 311121, China.
Liu Y; School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China.
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Źródło :
Inorganic chemistry [Inorg Chem] 2021 Jul 05; Vol. 60 (13), pp. 9345-9358. Date of Electronic Publication: 2021 Jun 17.
Typ publikacji :
Journal Article
MeSH Terms :
Enzyme Inhibitors/*pharmacology
Nitric Oxide Synthase Type I/*antagonists & inhibitors
Pentanoic Acids/*pharmacology
Crystallography, X-Ray ; Density Functional Theory ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Humans ; Molecular Conformation ; Molecular Dynamics Simulation ; Nitric Oxide Synthase Type I/metabolism ; Pentanoic Acids/chemical synthesis ; Pentanoic Acids/chemistry
Czasopismo naukowe
Tytuł :
Combination of Heme Oxygenase-1 Inhibition and Sigma Receptor Modulation for Anticancer Activity.
Autorzy :
Romeo G; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
Ciaffaglione V; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
Amata E; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
Dichiara M; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
Calabrese L; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
Vanella L; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
Sorrenti V; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
Grosso S; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
D'Amico AG; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
D'Agata V; Department of Biomedical and Biotechnological Sciences, University of Catania, 95100 Catania, Italy.
Intagliata S; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
Salerno L; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
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Źródło :
Molecules (Basel, Switzerland) [Molecules] 2021 Jun 24; Vol. 26 (13). Date of Electronic Publication: 2021 Jun 24.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents*/chemistry
Antineoplastic Agents*/pharmacology
Enzyme Inhibitors*/chemistry
Enzyme Inhibitors*/pharmacology
Neoplasms*/drug therapy
Neoplasms*/metabolism
Neoplasms*/pathology
Heme Oxygenase-1/*antagonists & inhibitors
Neoplasm Proteins/*antagonists & inhibitors
Receptors, sigma/*antagonists & inhibitors
Animals ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Heme Oxygenase-1/metabolism ; Humans ; Neoplasm Proteins/metabolism ; Rats ; Receptors, sigma/metabolism
Czasopismo naukowe
Tytuł :
Exploring the potential of novel xanthine oxidase inhibitory peptide (ACECD) derived from Skipjack tuna hydrolysates using affinity-ultrafiltration coupled with HPLC-MALDI-TOF/TOF-MS.
Autorzy :
Zhong H; Ningbo Research Institute, Zhejiang University, Ningbo 315100, China; College of Biosystems Engineering and Food Science, Zhejiang University, Hangzhou 310058, China.
Abdullah; College of Biosystems Engineering and Food Science, Zhejiang University, Hangzhou 310058, China.
Zhang Y; Ningbo Research Institute, Zhejiang University, Ningbo 315100, China; College of Biosystems Engineering and Food Science, Zhejiang University, Hangzhou 310058, China.
Deng L; College of Biological Science and Technology, Hubei Minzu University, Enshi 445000, China.
Zhao M; Ningbo Research Institute, Zhejiang University, Ningbo 315100, China; College of Biosystems Engineering and Food Science, Zhejiang University, Hangzhou 310058, China.
Tang J; Ningbo Research Institute, Zhejiang University, Ningbo 315100, China; College of Biosystems Engineering and Food Science, Zhejiang University, Hangzhou 310058, China.
Zhang H; Ningbo Research Institute, Zhejiang University, Ningbo 315100, China; College of Biosystems Engineering and Food Science, Zhejiang University, Hangzhou 310058, China.
Feng F; Ningbo Research Institute, Zhejiang University, Ningbo 315100, China; College of Biosystems Engineering and Food Science, Zhejiang University, Hangzhou 310058, China. Electronic address: .
Wang J; Ningbo Research Institute, Zhejiang University, Ningbo 315100, China; College of Biosystems Engineering and Food Science, Zhejiang University, Hangzhou 310058, China. Electronic address: .
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Źródło :
Food chemistry [Food Chem] 2021 Jun 15; Vol. 347, pp. 129068. Date of Electronic Publication: 2021 Jan 12.
Typ publikacji :
Journal Article
MeSH Terms :
Enzyme Inhibitors/*chemistry
Peptides/*chemistry
Tuna/*metabolism
Xanthine Oxidase/*antagonists & inhibitors
Amino Acid Sequence ; Animals ; Antioxidants/chemistry ; Binding Sites ; Chromatography, High Pressure Liquid ; Enzyme Inhibitors/isolation & purification ; Enzyme Inhibitors/metabolism ; Molecular Docking Simulation ; Peptides/isolation & purification ; Peptides/metabolism ; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization ; Ultrafiltration ; Xanthine Oxidase/metabolism
Czasopismo naukowe
Tytuł :
Inhibitors of bacterial H 2 S biogenesis targeting antibiotic resistance and tolerance.
Autorzy :
Shatalin K; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Nuthanakanti A; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Kaushik A; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Shishov D; Gero LLC, Moscow, Russia.
Peselis A; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Shamovsky I; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Pani B; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Lechpammer M; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Vasilyev N; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Shatalina E; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Rebatchouk D; Ellyris LLC, Union, NJ 07083, USA.
Mironov A; Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Center for Precision Genome Editing and Genetic Technologies for Biomedicine, Moscow 119991, Russia.
Fedichev P; Gero LLC, Moscow, Russia.
Serganov A; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA.
Nudler E; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA. .; Howard Hughes Medical Institute, New York University School of Medicine, New York, NY 10016, USA.
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Źródło :
Science (New York, N.Y.) [Science] 2021 Jun 11; Vol. 372 (6547), pp. 1169-1175.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Anti-Bacterial Agents/*pharmacology
Cystathionine gamma-Lyase/*antagonists & inhibitors
Enzyme Inhibitors/*pharmacology
Hydrogen Sulfide/*metabolism
Pseudomonas aeruginosa/*drug effects
Staphylococcus aureus/*drug effects
Animals ; Anti-Bacterial Agents/chemistry ; Anti-Bacterial Agents/metabolism ; Biofilms ; Crystallography, X-Ray ; Cystathionine gamma-Lyase/chemistry ; Cystathionine gamma-Lyase/genetics ; Cystathionine gamma-Lyase/metabolism ; Drug Discovery ; Drug Resistance, Bacterial ; Drug Synergism ; Drug Tolerance ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/metabolism ; Mice ; Microbial Sensitivity Tests ; Models, Molecular ; Molecular Docking Simulation ; Molecular Structure ; Pseudomonas Infections/drug therapy ; Pseudomonas Infections/microbiology ; Pseudomonas aeruginosa/enzymology ; Pseudomonas aeruginosa/genetics ; Pseudomonas aeruginosa/growth & development ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/metabolism ; Small Molecule Libraries/pharmacology ; Staphylococcal Infections/drug therapy ; Staphylococcal Infections/microbiology ; Staphylococcus aureus/enzymology ; Staphylococcus aureus/genetics ; Staphylococcus aureus/growth & development
Czasopismo naukowe
Tytuł :
Small-Molecule Inhibitors Targeting Proteasome-Associated Deubiquitinases.
Autorzy :
Moon S; Department of New Biology, Daegu Gyeongbuk Institute of Science and Technology (DGIST), Daegu 42988, Korea.; Protein Dynamics-Based Proteotoxicity Control Lab, Basic Research Lab, Daegu Gyeongbuk Institute of Science and Technology (DGIST), Daegu 42988, Korea.; Center for Cell Fate Reprogramming & Control, Daegu Gyeongbuk Institute of Science and Technology (DGIST), Daegu 42988, Korea.
Muniyappan S; Department of New Biology, Daegu Gyeongbuk Institute of Science and Technology (DGIST), Daegu 42988, Korea.
Lee SB; Protein Dynamics-Based Proteotoxicity Control Lab, Basic Research Lab, Daegu Gyeongbuk Institute of Science and Technology (DGIST), Daegu 42988, Korea.; Department of Brain & Cognitive Sciences, Daegu Gyeongbuk Institute of Science and Technology (DGIST), Daegu 42988, Korea.
Lee BH; Department of New Biology, Daegu Gyeongbuk Institute of Science and Technology (DGIST), Daegu 42988, Korea.; Protein Dynamics-Based Proteotoxicity Control Lab, Basic Research Lab, Daegu Gyeongbuk Institute of Science and Technology (DGIST), Daegu 42988, Korea.; Center for Cell Fate Reprogramming & Control, Daegu Gyeongbuk Institute of Science and Technology (DGIST), Daegu 42988, Korea.
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Źródło :
International journal of molecular sciences [Int J Mol Sci] 2021 Jun 09; Vol. 22 (12). Date of Electronic Publication: 2021 Jun 09.
Typ publikacji :
Journal Article; Review
MeSH Terms :
Enzyme Inhibitors*/chemistry
Enzyme Inhibitors*/therapeutic use
Neoplasm Proteins*/antagonists & inhibitors
Neoplasm Proteins*/metabolism
Neoplasms*/drug therapy
Neoplasms*/enzymology
Neoplasms*/pathology
Pyrroles*/chemistry
Pyrroles*/therapeutic use
Pyrrolidines*/chemistry
Pyrrolidines*/therapeutic use
Ubiquitin Thiolesterase*/antagonists & inhibitors
Ubiquitin Thiolesterase*/metabolism
Proteasome Endopeptidase Complex/*metabolism
Proteolysis/*drug effects
Humans
Czasopismo naukowe
Tytuł :
The diterpene Manool extracted from Salvia tingitana lowers free radical production in retinal rod outer segments by inhibiting the extramitochondrial F 1 F o ATP synthase.
Autorzy :
Ravera S; Dipartimento di Medicina Sperimentale, Università di Genova, Genova, Italy.
Esposito A; Centro di Biologia Integrata (CIBIO), Università di Trento, Trento, Italy.
Degan P; UOC Mutagenesi, IRCCS Policlinico San Martino -IST (Istituto Nazionale per la Ricerca sul Cancro), Genova, Italy.
Caicci F; Dipartimento di Biologia, Università di Padova, Padova, Italy.
Manni L; Dipartimento di Biologia, Università di Padova, Padova, Italy.
Liguori A; Dipartimento di Farmacia (DIFAR), Università di Genova, Genova, Italy.
Bisio A; Dipartimento di Farmacia (DIFAR), Università di Genova, Genova, Italy.
Iobbi V; Dipartimento di Farmacia (DIFAR), Università di Genova, Genova, Italy.
Schito A; Dipartimento di Scienze Chirurgiche e Diagnostiche Integrate (DISC), Sezione di Microbiologia, Università di Genova, Genova, Italy.
Traverso CE; Clinica Oculistica, (DINOGMI) Università di Genova, Genova, Italy.
Panfoli I; Dipartimento di Farmacia (DIFAR), Università di Genova, Genova, Italy.
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Źródło :
Cell biochemistry and function [Cell Biochem Funct] 2021 Jun; Vol. 39 (4), pp. 528-535. Date of Electronic Publication: 2021 Jan 20.
Typ publikacji :
Journal Article
MeSH Terms :
Antioxidants/*pharmacology
Diterpenes/*pharmacology
Enzyme Inhibitors/*pharmacology
Proton-Translocating ATPases/*antagonists & inhibitors
Retinal Photoreceptor Cell Outer Segment/*drug effects
Salvia/*chemistry
Animals ; Antioxidants/chemistry ; Antioxidants/isolation & purification ; Cattle ; Diterpenes/chemistry ; Diterpenes/isolation & purification ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/isolation & purification ; Free Radicals/antagonists & inhibitors ; Free Radicals/metabolism ; Models, Molecular ; Oxidative Stress/drug effects ; Proton-Translocating ATPases/genetics ; Proton-Translocating ATPases/metabolism ; Retinal Photoreceptor Cell Outer Segment/metabolism
Czasopismo naukowe
Tytuł :
ACE inhibitor-related angioedema in a COVID-19 patient-a plausible contribution of the viral infection?
Autorzy :
Kuzemczak M; Peter Munk Cardiac Centre, Division of Cardiology, Toronto General Hospital, University Health Network, 585 University Avenue, Toronto, Ontario, M5G 2C4, Canada. .; Chair of Emergency Medicine, Department of Medical Rescue, Poznan University of Medical Sciences, Poznań, Poland. .; Department of Invasive Cardiology, Central Clinical Hospital of the Ministry of Interior and Administration, Warsaw, Poland. .
Kavvouras C; Peter Munk Cardiac Centre, Division of Cardiology, Toronto General Hospital, University Health Network, 585 University Avenue, Toronto, Ontario, M5G 2C4, Canada.
Alkhalil M; Peter Munk Cardiac Centre, Division of Cardiology, Toronto General Hospital, University Health Network, 585 University Avenue, Toronto, Ontario, M5G 2C4, Canada.
Osten M; Peter Munk Cardiac Centre, Division of Cardiology, Toronto General Hospital, University Health Network, 585 University Avenue, Toronto, Ontario, M5G 2C4, Canada.
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Źródło :
European journal of clinical pharmacology [Eur J Clin Pharmacol] 2021 Jun; Vol. 77 (6), pp. 933-934. Date of Electronic Publication: 2021 Jan 03.
Typ publikacji :
Case Reports; Letter
MeSH Terms :
Angioedema*/chemically induced
Angioedema*/physiopathology
Angioedema*/therapy
Angioedema*/virology
Angiotensin-Converting Enzyme Inhibitors*/administration & dosage
Angiotensin-Converting Enzyme Inhibitors*/adverse effects
COVID-19*/complications
COVID-19*/diagnosis
COVID-19*/physiopathology
Myocardial Infarction*/complications
Myocardial Infarction*/diagnosis
Myocardial Infarction*/drug therapy
Myocardial Infarction*/physiopathology
Ramipril*/administration & dosage
Ramipril*/adverse effects
COVID-19 Nucleic Acid Testing ; Cardiovascular Agents/administration & dosage ; Coronary Angiography/methods ; Drug Substitution/methods ; Humans ; Male ; Middle Aged ; Patient Care Management ; Platelet Aggregation Inhibitors/administration & dosage ; SARS-CoV-2 ; Treatment Outcome
Raport
Tytuł :
The PFKFB3 Inhibitor AZ67 Inhibits Angiogenesis Independently of Glycolysis Inhibition.
Autorzy :
Emini Veseli B; Laboratory of Physiopharmacology, University of Antwerp, 2610 Antwerp, Belgium.; Aberdeen Cardiovascular and Diabetes Centre, Institute of Medical Sciences, University of Aberdeen, Aberdeen AB25 2ZD, UK.
Van Wielendaele P; Laboratory of Medical Biochemistry, University of Antwerp, 2610 Antwerp, Belgium.
Delibegovic M; Aberdeen Cardiovascular and Diabetes Centre, Institute of Medical Sciences, University of Aberdeen, Aberdeen AB25 2ZD, UK.
Martinet W; Laboratory of Physiopharmacology, University of Antwerp, 2610 Antwerp, Belgium.
De Meyer GRY; Laboratory of Physiopharmacology, University of Antwerp, 2610 Antwerp, Belgium.
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Źródło :
International journal of molecular sciences [Int J Mol Sci] 2021 May 31; Vol. 22 (11). Date of Electronic Publication: 2021 May 31.
Typ publikacji :
Journal Article
MeSH Terms :
Enzyme Inhibitors*/metabolism
Enzyme Inhibitors*/pharmacology
Phosphofructokinase-2*/antagonists & inhibitors
Phosphofructokinase-2*/metabolism
Cell Proliferation/*drug effects
Glycolysis/*drug effects
Neovascularization, Physiologic/*drug effects
Animals ; Cell Line ; Endothelial Cells ; Humans ; Mice ; Mice, Inbred C57BL ; Protein Binding
Czasopismo naukowe
Tytuł :
Identification of post-digestion angiotensin-I converting enzyme (ACE) inhibitory peptides from soybean protein Isolate: Their production conditions and in silico molecular docking with ACE.
Autorzy :
Xu Z; School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China; Guangdong Huapeptide Biotechnology Co., Ltd., Zhaoqing 526238, China.
Wu C; School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China; Department of Food Science and Engineering, Jinan University, Guangzhou 510632, China.
Sun-Waterhouse D; School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China.
Zhao T; School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China.
Waterhouse GIN; School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China.
Zhao M; School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China; Department of Food Science and Engineering, Jinan University, Guangzhou 510632, China; Guangdong Huapeptide Biotechnology Co., Ltd., Zhaoqing 526238, China.
Su G; School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China; Department of Food Science and Engineering, Jinan University, Guangzhou 510632, China. Electronic address: .
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Źródło :
Food chemistry [Food Chem] 2021 May 30; Vol. 345, pp. 128855. Date of Electronic Publication: 2020 Dec 10.
Typ publikacji :
Journal Article
MeSH Terms :
Computer Simulation*
Digestion*
Molecular Docking Simulation*
Angiotensin-Converting Enzyme Inhibitors/*analysis
Peptides/*analysis
Peptidyl-Dipeptidase A/*metabolism
Soybean Proteins/*chemistry
Angiotensin-Converting Enzyme Inhibitors/metabolism ; Angiotensin-Converting Enzyme Inhibitors/pharmacology ; Animals ; Hydrophobic and Hydrophilic Interactions ; Peptides/metabolism ; Peptides/pharmacology ; Peptidyl-Dipeptidase A/chemistry ; Protein Conformation
Czasopismo naukowe
Tytuł :
Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model.
Autorzy :
De Fusco C; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Schimpl M; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Börjesson U; Discovery Sciences, R&D, AstraZeneca, Gothenburg SE-431 83, Sweden.
Cheung T; Oncology R&D, AstraZeneca, Boston, Massachusetts 02451, United States.
Collie I; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Evans L; Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Narasimhan P; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Stubbs C; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Vazquez-Chantada M; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Wagner DJ; Oncology R&D, AstraZeneca, Boston, Massachusetts 02451, United States.
Grondine M; Oncology R&D, AstraZeneca, Boston, Massachusetts 02451, United States.
Sanders MG; Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Tentarelli S; Oncology R&D, AstraZeneca, Boston, Massachusetts 02451, United States.
Underwood E; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Argyrou A; Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Smith JM; Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Lynch JT; Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Chiarparin E; Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Robb G; Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Bagal SK; Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
Scott JS; Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 May 27; Vol. 64 (10), pp. 6814-6826. Date of Electronic Publication: 2021 Apr 26.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Enzyme Inhibitors/*chemistry
Methionine Adenosyltransferase/*antagonists & inhibitors
Allosteric Site ; Animals ; Cell Proliferation ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; Gene Knockout Techniques ; HCT116 Cells ; Half-Life ; Humans ; Methionine Adenosyltransferase/genetics ; Methionine Adenosyltransferase/metabolism ; Mice ; Molecular Dynamics Simulation ; Neoplasms/drug therapy ; Neoplasms/pathology ; Quinazolines/chemistry ; Quinazolines/metabolism ; Quinazolines/pharmacology ; Quinazolines/therapeutic use ; Rats ; S-Adenosylmethionine/metabolism ; Structure-Activity Relationship ; Transplantation, Heterologous
Czasopismo naukowe
Tytuł :
Glutaminyl Cyclase, Diseases, and Development of Glutaminyl Cyclase Inhibitors.
Autorzy :
Xu C; School of Pharmaceutical Sciences, Health Science Center, Shenzhen University, Shenzhen 518060, China.
Wang YN; School of Pharmaceutical Sciences, Health Science Center, Shenzhen University, Shenzhen 518060, China.
Wu H; School of Pharmaceutical Sciences, Health Science Center, Shenzhen University, Shenzhen 518060, China.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 May 27; Vol. 64 (10), pp. 6549-6565. Date of Electronic Publication: 2021 May 17.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't; Review
MeSH Terms :
Aminoacyltransferases/*antagonists & inhibitors
Enzyme Inhibitors/*chemistry
Aminoacyltransferases/metabolism ; Amyloid beta-Peptides/metabolism ; Biological Products/chemistry ; Biological Products/metabolism ; Biological Products/therapeutic use ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/therapeutic use ; Humans ; Imidazoles/chemistry ; Imidazoles/metabolism ; Imidazoles/therapeutic use ; Inflammation/drug therapy ; Inflammation/metabolism ; Inflammation/pathology ; Neurodegenerative Diseases/drug therapy ; Neurodegenerative Diseases/metabolism ; Neurodegenerative Diseases/pathology ; Pyrrolidonecarboxylic Acid/metabolism ; Up-Regulation
Czasopismo naukowe
Tytuł :
Design, Synthesis, and Biological Evaluation of Novel 6 H -Benzo[ c ]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors.
Autorzy :
Tang L; Institute of Chemical Industry of Forest Products, Chinese Academy of Forestry, Nanjing 210042, China.; School of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China.; School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China.
Jiang J; Institute of Chemical Industry of Forest Products, Chinese Academy of Forestry, Nanjing 210042, China.; School of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China.
Song G; School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China.
Wang Y; School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China.
Zhuang Z; School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China.
Tan Y; School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China.
Xia Y; School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China.
Huang X; School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China.
Feng X; School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China.
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Źródło :
International journal of molecular sciences [Int J Mol Sci] 2021 May 26; Vol. 22 (11). Date of Electronic Publication: 2021 May 26.
Typ publikacji :
Journal Article
MeSH Terms :
Benzopyrans*/chemical synthesis
Benzopyrans*/chemistry
Benzopyrans*/pharmacology
Drug Design*
Enzyme Inhibitors*/chemical synthesis
Enzyme Inhibitors*/chemistry
Enzyme Inhibitors*/pharmacology
Exonucleases/*antagonists & inhibitors
Cell Line ; Drug Evaluation ; Exonucleases/metabolism ; Humans ; Molecular Structure ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
In Vitro Identification and In Vivo Confirmation of Inhibitors for Sweet Potato Chlorotic Stunt Virus RNA Silencing Suppressor, a Viral RNase III.
Autorzy :
Wang L; Department of Agricultural Sciences, University of Helsinki, Helsinki, Finland .
Poque S; Department of Agricultural Sciences, University of Helsinki, Helsinki, Finland.
Laamanen K; Institute for Molecular Medicine Finland, University of Helsinki, Helsinki, Finland.
Saarela J; Institute for Molecular Medicine Finland, University of Helsinki, Helsinki, Finland.
Poso A; School of Pharmacy, University of Eastern Finland, Kuopio, Finland.; Department of Internal Medicine VIII, University Hospital Tübingen, Tübingen, Germany.
Laitinen T; School of Pharmacy, University of Eastern Finland, Kuopio, Finland.
Valkonen JPT; Department of Agricultural Sciences, University of Helsinki, Helsinki, Finland .
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Źródło :
Journal of virology [J Virol] 2021 May 24; Vol. 95 (12). Date of Electronic Publication: 2021 May 24 (Print Publication: 2021).
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Antiviral Agents/*pharmacology
Crinivirus/*drug effects
Enzyme Inhibitors/*pharmacology
Ipomoea batatas/*virology
Plant Diseases/*virology
Ribonuclease III/*antagonists & inhibitors
Small Molecule Libraries/*pharmacology
Antiviral Agents/chemistry ; Antiviral Agents/metabolism ; Crinivirus/enzymology ; Crinivirus/physiology ; Dose-Response Relationship, Drug ; Drug Evaluation, Preclinical ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/metabolism ; High-Throughput Screening Assays ; Molecular Docking Simulation ; Photosynthesis/drug effects ; RNA Interference ; Ribonuclease III/chemistry ; Ribonuclease III/metabolism ; Small Molecule Libraries/chemistry ; Viral Proteins/antagonists & inhibitors
SCR Organism :
Sweet potato chlorotic stunt virus
Czasopismo naukowe
Tytuł :
From the Design to the In Vivo Evaluation of Benzohomoadamantane-Derived Soluble Epoxide Hydrolase Inhibitors for the Treatment of Acute Pancreatitis.
Autorzy :
Codony S; Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Departament de Farmacologia, Toxicologia i Química Terapèutica, Facultat de Farmàcia i Ciències de l'Alimentació, and Institute of Biomedicine (IBUB), Universitat de Barcelona, Av. Joan XXIII, 27-31, Barcelona 08028, Spain.
Calvó-Tusell C; CompBioLab Group, Departament de Química and Institut de Química Computacional i Catàlisi (IQCC), Universitat de Girona, C/ Maria Aurèlia Capmany 69, Girona 17003, Spain.
Valverde E; Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Departament de Farmacologia, Toxicologia i Química Terapèutica, Facultat de Farmàcia i Ciències de l'Alimentació, and Institute of Biomedicine (IBUB), Universitat de Barcelona, Av. Joan XXIII, 27-31, Barcelona 08028, Spain.
Osuna S; CompBioLab Group, Departament de Química and Institut de Química Computacional i Catàlisi (IQCC), Universitat de Girona, C/ Maria Aurèlia Capmany 69, Girona 17003, Spain.; Institució Catalana de Recerca i Estudis Avançats (ICREA), Barcelona 08010, Spain.
Morisseau C; Department of Entomology and Nematology and Comprehensive Cancer Center, University of California Davis, One Shields Avenue, Davis 95616, California, United States.
Loza MI; Drug Screening Platform/Biofarma Research Group, CIMUS Research Center. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica, University of Santiago de Compostela (USC), Santiago de Compostela 15782, Spain.
Brea J; Drug Screening Platform/Biofarma Research Group, CIMUS Research Center. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica, University of Santiago de Compostela (USC), Santiago de Compostela 15782, Spain.
Pérez C; Institute of Medicinal Chemistry, Spanish National Research Council (CSIC), C/Juan de la Cierva 3, Madrid 28006, Spain.
Rodríguez-Franco MI; Institute of Medicinal Chemistry, Spanish National Research Council (CSIC), C/Juan de la Cierva 3, Madrid 28006, Spain.
Pizarro-Delgado J; Pharmacology Section. Department of Pharmacology, Toxicology and Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, and Institute of Biomedicine of the University of Barcelona (IBUB), University of Barcelona, Av. Joan XXIII, 27-31, Barcelona 08028, Spain.; Spanish Biomedical Research Center in Diabetes and Associated Metabolic Diseases (CIBERDEM)-Instituto de Salud Carlos III, Madrid 28029, Spain.; Pediatric Research Institute-Hospital Sant Joan de Déu, Esplugues de Llobregat 08950, Spain.
Corpas R; Institute of Biomedical Research of Barcelona (IIBB), CSIC and IDIBAPS, Barcelona 08036, Spain.; CIBER Epidemiology and Public Health (CIBERESP)-Instituto de Salud Carlos III, Madrid 28029, Spain.
Griñán-Ferré C; Pharmacology Section. Department of Pharmacology, Toxicology and Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, and Institut de Neurociències, University of Barcelona, Av. Joan XXIII, 27-31, Barcelona 08028, Spain.
Pallàs M; Pharmacology Section. Department of Pharmacology, Toxicology and Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, and Institut de Neurociències, University of Barcelona, Av. Joan XXIII, 27-31, Barcelona 08028, Spain.
Sanfeliu C; Institute of Biomedical Research of Barcelona (IIBB), CSIC and IDIBAPS, Barcelona 08036, Spain.; CIBER Epidemiology and Public Health (CIBERESP)-Instituto de Salud Carlos III, Madrid 28029, Spain.
Vázquez-Carrera M; Pharmacology Section. Department of Pharmacology, Toxicology and Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, and Institute of Biomedicine of the University of Barcelona (IBUB), University of Barcelona, Av. Joan XXIII, 27-31, Barcelona 08028, Spain.; Spanish Biomedical Research Center in Diabetes and Associated Metabolic Diseases (CIBERDEM)-Instituto de Salud Carlos III, Madrid 28029, Spain.; Pediatric Research Institute-Hospital Sant Joan de Déu, Esplugues de Llobregat 08950, Spain.
Hammock BD; Department of Entomology and Nematology and Comprehensive Cancer Center, University of California Davis, One Shields Avenue, Davis 95616, California, United States.
Feixas F; CompBioLab Group, Departament de Química and Institut de Química Computacional i Catàlisi (IQCC), Universitat de Girona, C/ Maria Aurèlia Capmany 69, Girona 17003, Spain.
Vázquez S; Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Departament de Farmacologia, Toxicologia i Química Terapèutica, Facultat de Farmàcia i Ciències de l'Alimentació, and Institute of Biomedicine (IBUB), Universitat de Barcelona, Av. Joan XXIII, 27-31, Barcelona 08028, Spain.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 May 13; Vol. 64 (9), pp. 5429-5446. Date of Electronic Publication: 2021 May 04.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
MeSH Terms :
Drug Design*
Adamantane/*chemistry
Enzyme Inhibitors/*chemistry
Epoxide Hydrolases/*antagonists & inhibitors
Acute Disease ; Adamantane/metabolism ; Adamantane/pharmacology ; Adamantane/therapeutic use ; Animals ; Binding Sites ; Catalytic Domain ; Cell Membrane Permeability/drug effects ; Drug Stability ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; Epoxide Hydrolases/metabolism ; Half-Life ; Humans ; Hydrophobic and Hydrophilic Interactions ; Male ; Mice ; Mice, Inbred C57BL ; Molecular Dynamics Simulation ; Pancreatitis/drug therapy ; Rats ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Development of Potent NEDD8-Activating Enzyme Inhibitors Bearing a Pyrimidotriazole Scaffold.
Autorzy :
Xiong C; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; Pharm-X Center, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.; University of Chinese Academy of Sciences, Beijing 100049, China.
Zhou L; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; University of Chinese Academy of Sciences, Beijing 100049, China.
Tan J; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; Pharm-X Center, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.; University of Chinese Academy of Sciences, Beijing 100049, China.
Song S; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; University of Chinese Academy of Sciences, Beijing 100049, China.
Bao X; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; University of Chinese Academy of Sciences, Beijing 100049, China.
Zhang N; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; University of Chinese Academy of Sciences, Beijing 100049, China.
Ding H; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; University of Chinese Academy of Sciences, Beijing 100049, China.
Zhao J; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; Pharm-X Center, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.; School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China.
He JX; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; University of Chinese Academy of Sciences, Beijing 100049, China.
Miao ZH; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; University of Chinese Academy of Sciences, Beijing 100049, China.
Zhang A; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.; Pharm-X Center, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.; University of Chinese Academy of Sciences, Beijing 100049, China.; Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.; State Key Laboratory of Esophageal Cancer Prevention and Treatment, Ministry of Education of China, Zhengzhou University, Zhengzhou 450001, China.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 May 13; Vol. 64 (9), pp. 6161-6178. Date of Electronic Publication: 2021 Apr 15.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Drug Design*
Enzyme Inhibitors/*chemistry
Enzyme Inhibitors/*pharmacology
Tirapazamine/*chemistry
Tirapazamine/*pharmacology
Ubiquitin-Activating Enzymes/*antagonists & inhibitors
Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacokinetics ; Antineoplastic Agents/pharmacology ; Antineoplastic Combined Chemotherapy Protocols ; Cell Line, Tumor ; Cisplatin ; Enzyme Inhibitors/pharmacokinetics ; Humans ; Ifosfamide ; Mitomycin ; Tirapazamine/pharmacokinetics ; Tissue Distribution ; Xenograft Model Antitumor Assays
SCR Protocol :
MIP protocol
Czasopismo naukowe
Tytuł :
Discovery of Orally Bioavailable Purine-Based Inhibitors of the Low-Molecular-Weight Protein Tyrosine Phosphatase.
Autorzy :
Stanford SM; Department of Medicine, University of California, San Diego, La Jolla, California 92037, United States.
Diaz MA; Department of Medicine, University of California, San Diego, La Jolla, California 92037, United States.
Ardecky RJ; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Zou J; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Roosild T; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Holmes ZJ; Department of Medicine, University of California, San Diego, La Jolla, California 92037, United States.
Nguyen TP; Department of Medicine, University of California, San Diego, La Jolla, California 92037, United States.
Hedrick MP; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Rodiles S; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Guan A; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Grotegut S; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Santelli E; Department of Medicine, University of California, San Diego, La Jolla, California 92037, United States.
Chung TDY; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Jackson MR; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Bottini N; Department of Medicine, University of California, San Diego, La Jolla, California 92037, United States.
Pinkerton AB; Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 May 13; Vol. 64 (9), pp. 5645-5653. Date of Electronic Publication: 2021 Apr 29.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
MeSH Terms :
Enzyme Inhibitors/*chemistry
Protein Tyrosine Phosphatases/*antagonists & inhibitors
Purines/*chemistry
Administration, Oral ; Animals ; Binding Sites ; Crystallography, X-Ray ; Diabetes Mellitus, Type 2/drug therapy ; Diabetes Mellitus, Type 2/etiology ; Disease Models, Animal ; Drug Evaluation, Preclinical ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; Half-Life ; Humans ; Insulin Resistance ; Kinetics ; Molecular Dynamics Simulation ; Obesity/complications ; Obesity/pathology ; Phosphorylation/drug effects ; Protein Tyrosine Phosphatases/metabolism ; Proto-Oncogene Proteins c-akt/metabolism ; Purines/metabolism ; Purines/pharmacology ; Purines/therapeutic use ; Signal Transduction/drug effects ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease.
Autorzy :
Stevaert A; Laboratory of Virology and Chemotherapy, Rega Institute, KU Leuven, 3000 Leuven, Belgium.
Krasniqi B; Molecular Design and Synthesis, Department of Chemistry, KU Leuven, 3001 Leuven, Belgium.
Van Loy B; Laboratory of Virology and Chemotherapy, Rega Institute, KU Leuven, 3000 Leuven, Belgium.
Nguyen T; Biochemistry, Molecular and Structural Biology, Department of Chemistry, KU Leuven, 3001 Leuven, Belgium.
Thomas J; Molecular Design and Synthesis, Department of Chemistry, KU Leuven, 3001 Leuven, Belgium.
Vandeput J; Laboratory of Virology and Chemotherapy, Rega Institute, KU Leuven, 3000 Leuven, Belgium.
Jochmans D; Laboratory of Virology and Chemotherapy, Rega Institute, KU Leuven, 3000 Leuven, Belgium.
Thiel V; Institute of Virology and Immunology (IVI), 3012 Bern and 3012 Bern, Switzerland.; Department of Infectious Diseases and Pathobiology, Vetsuisse Faculty, University of Bern, 3012 Bern, Switzerland.
Dijkman R; Institute of Virology and Immunology (IVI), 3012 Bern and 3012 Bern, Switzerland.; Department of Infectious Diseases and Pathobiology, Vetsuisse Faculty, University of Bern, 3012 Bern, Switzerland.; Institute for Infectious Diseases (IFIK), University of Bern, 3012 Bern, Switzerland.
Dehaen W; Molecular Design and Synthesis, Department of Chemistry, KU Leuven, 3001 Leuven, Belgium.
Voet A; Biochemistry, Molecular and Structural Biology, Department of Chemistry, KU Leuven, 3001 Leuven, Belgium.
Naesens L; Laboratory of Virology and Chemotherapy, Rega Institute, KU Leuven, 3000 Leuven, Belgium.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 May 13; Vol. 64 (9), pp. 5632-5644. Date of Electronic Publication: 2021 Apr 20.
Typ publikacji :
Journal Article
MeSH Terms :
Antiviral Agents/*pharmacology
Coronavirus 229E, Human/*drug effects
Coronavirus 229E, Human/*enzymology
Endoribonucleases/*antagonists & inhibitors
Enzyme Inhibitors/*pharmacology
Oleanolic Acid/*analogs & derivatives
Viral Nonstructural Proteins/*antagonists & inhibitors
Virus Replication/*drug effects
Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Cell Line ; Dose-Response Relationship, Drug ; Endoribonucleases/metabolism ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Humans ; Microbial Sensitivity Tests ; Models, Molecular ; Oleanolic Acid/chemical synthesis ; Oleanolic Acid/chemistry ; Oleanolic Acid/pharmacology ; Viral Nonstructural Proteins/metabolism
Czasopismo naukowe
Tytuł :
Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5- a ]pyridine Scaffold: SAR of the Biphenyl Moiety.
Autorzy :
Sainas S; Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, Turin 10125, Italy.
Giorgis M; Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, Turin 10125, Italy.
Circosta P; Department of Clinical and Biological Sciences, University of Turin, Regione Gonzole 10, Orbassano, Turin 10043, Italy.; Molecular Biotechnology Center, University of Turin, Via Nizza 52, Turin 10126, Italy.
Gaidano V; Department of Clinical and Biological Sciences, University of Turin, Regione Gonzole 10, Orbassano, Turin 10043, Italy.; Division of Hematology, AO SS Antonio e Biagio e Cesare Arrigo, Via Venezia 16, Alessandria 15121, Italy.
Bonanni D; Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, Turin 10125, Italy.
Pippione AC; Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, Turin 10125, Italy.
Bagnati R; Department of Environmental Health Sciences, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri 2, Milano 20156, Italy.
Passoni A; Department of Environmental Health Sciences, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri 2, Milano 20156, Italy.
Qiu Y; Laboratory of Tumor Microenvironment, Candiolo Cancer Institute, FPO, IRCCS, Candiolo, Strada Provinciale, 142-KM 3.95, Candiolo, Turin 10060, Italy.; Higher Education Mega Center, Institutes for Life Sciences, South China University of Technology, Guangzhou 510641, China.
Cojocaru CF; Laboratory of Tumor Microenvironment, Candiolo Cancer Institute, FPO, IRCCS, Candiolo, Strada Provinciale, 142-KM 3.95, Candiolo, Turin 10060, Italy.
Canepa B; Gem Forlab srl, Via Ribes, 5, Colleretto Giacosa, Turin 10010, Italy.
Bona A; Gem Chimica srl, Via Maestri del Lavoro, 25, Busca, Cuneo 12022, Italy.
Rolando B; Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, Turin 10125, Italy.
Mishina M; Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, Turin 10125, Italy.
Ramondetti C; Department of Oncology, University of Turin, Via Michelangelo 27/B, Turin 10125, Italy.
Buccinnà B; Department of Oncology, University of Turin, Via Michelangelo 27/B, Turin 10125, Italy.
Piccinini M; Department of Oncology, University of Turin, Via Michelangelo 27/B, Turin 10125, Italy.
Houshmand M; Department of Clinical and Biological Sciences, University of Turin, Regione Gonzole 10, Orbassano, Turin 10043, Italy.; Molecular Biotechnology Center, University of Turin, Via Nizza 52, Turin 10126, Italy.
Cignetti A; Division of Hematology and Cell Therapy, AO Ordine Mauriziano, Largo Filippo Turati, 62, Turin 10128, Italy.
Giraudo E; Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, Turin 10125, Italy.; Laboratory of Tumor Microenvironment, Candiolo Cancer Institute, FPO, IRCCS, Candiolo, Strada Provinciale, 142-KM 3.95, Candiolo, Turin 10060, Italy.
Al-Karadaghi S; Department of Biochemistry and Structural Biology, Lund University, Naturvetarvägen 14, Box 124, Lund 221 00, Sweden.
Boschi D; Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, Turin 10125, Italy.
Saglio G; Department of Clinical and Biological Sciences, University of Turin, Regione Gonzole 10, Orbassano, Turin 10043, Italy.; Division of Hematology and Cell Therapy, AO Ordine Mauriziano, Largo Filippo Turati, 62, Turin 10128, Italy.
Lolli ML; Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, Turin 10125, Italy.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 May 13; Vol. 64 (9), pp. 5404-5428. Date of Electronic Publication: 2021 Apr 12.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Biphenyl Compounds/*chemistry
Enzyme Inhibitors/*chemistry
Oxidoreductases Acting on CH-CH Group Donors/*antagonists & inhibitors
Pyrazoles/*chemistry
Pyridines/*chemistry
Animals ; Apoptosis/drug effects ; Binding Sites ; Cell Differentiation/drug effects ; Cell Line, Tumor ; Drug Design ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; Female ; Half-Life ; Humans ; Leukemia, Myeloid, Acute/drug therapy ; Male ; Mice ; Mice, Inbred BALB C ; Microsomes, Liver/metabolism ; Molecular Docking Simulation ; Oxidoreductases Acting on CH-CH Group Donors/metabolism ; Pyrazoles/metabolism ; Pyrazoles/pharmacology ; Pyrazoles/therapeutic use ; Pyridines/metabolism ; Pyridines/pharmacology ; Pyridines/therapeutic use ; Rats ; Rats, Sprague-Dawley ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.
Autorzy :
Wu Z; Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
Bai Y; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China.
Jin J; Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
Jiang T; Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
Shen H; Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
Ju Q; Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
Zhu Q; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China; Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
Xu Y; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China; Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 May 05; Vol. 217, pp. 113357. Date of Electronic Publication: 2021 Mar 10.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Discovery*
Antineoplastic Agents/*pharmacology
Enzyme Inhibitors/*pharmacology
Phosphatidylinositol 3-Kinases/*metabolism
Poly(ADP-ribose) Polymerases/*metabolism
Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Humans ; Male ; Mammary Neoplasms, Experimental/drug therapy ; Mammary Neoplasms, Experimental/metabolism ; Mammary Neoplasms, Experimental/pathology ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Models, Molecular ; Molecular Structure ; Structure-Activity Relationship
Czasopismo naukowe

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