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Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.
Imbriglio, Jason E; Shen, Dong-Ming; Liang, Rui; Marby, Ken; You, Ming; Youm, Hye Won; Feng, Zhe; London, Clare; Xiong, Yusheng; Tata, Jim; Verras, Andreas; Garcia-Calvo, Margarita; Song, Xuelei; Addona, George H; McLaren, Dave G; He, Timothy; Murphy, Beth; Metzger, Dan E; Salituro, Gino; Deckman, Diana; Chen, Qing; Jin, Xiaoling; Stout, Steven J; Wang, Sheng-Ping; Wilsie, Larissa; Palyha, Oksana; Han, Seongah; Hubbard, Brian K; Previs, Stephen F; Pinto, Shirly; Taggart, Andrew.
Afiliação
  • Imbriglio JE; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Shen DM; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Liang R; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Marby K; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • You M; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Youm HW; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Feng Z; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • London C; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Xiong Y; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Tata J; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Verras A; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Garcia-Calvo M; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Song X; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Addona GH; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • McLaren DG; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • He T; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Murphy B; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Metzger DE; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Salituro G; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Deckman D; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Chen Q; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Jin X; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Stout SJ; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Wang SP; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Wilsie L; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Palyha O; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Han S; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Hubbard BK; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Previs SF; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Pinto S; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
  • Taggart A; Department of Discovery Chemistry, ‡Chemistry Modeling, and Informatics, §In Vitro Pharmacology, ∥In Vivo Pharmacology, ⊥Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Basic Pharmaceutical Sciences, and ○Atherosclerosis, Merck & Co., Inc. , 2000 Galloping Hill Road, Kenilworth,
J Med Chem ; 58(23): 9345-53, 2015 Dec 10.
Article em En | MEDLINE | ID: mdl-26561979
ABSTRACT
DGAT2 plays a critical role in hepatic triglyceride production, and data suggests that inhibition of DGAT2 could prove to be beneficial in treating a number of disease states. This article documents the discovery and optimization of a selective small molecule inhibitor of DGAT2 as well as pharmacological proof of biology in a mouse model of triglyceride production.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Triglicerídeos / Inibidores Enzimáticos / Diacilglicerol O-Aciltransferase / Isoquinolinas Limite: Animals / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2015 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Triglicerídeos / Inibidores Enzimáticos / Diacilglicerol O-Aciltransferase / Isoquinolinas Limite: Animals / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2015 Tipo de documento: Article