Literature DB >> 24900747

Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes.

Narihiro Toda1, Xiaolin Hao2, Yasuyuki Ogawa1, Kozo Oda1, Ming Yu2, Zice Fu2, Yi Chen2, Yongjae Kim2, Mike Lizarzaburu2, Sarah Lively2, Shauna Lawlis2, Michiko Murakoshi1, Futoshi Nara1, Nobuaki Watanabe1, Jeff D Reagan2, Hui Tian2, Angela Fu2, Alykhan Motani2, Qingxiang Liu2, Yi-Jyun Lin2, Run Zhuang2, Yumei Xiong2, Peter Fan2, Julio Medina2, Leping Li2, Masanori Izumi1, Ryo Okuyama1, Satoshi Shibuya1.   

Abstract

GPR142 is a G protein-coupled receptor that is predominantly expressed in pancreatic β-cells. GPR142 agonists stimulate insulin secretion in the presence of high glucose concentration, so that they could be novel insulin secretagogues with reduced or no risk of hypoglycemia. We report here the optimization of HTS hit compound 1 toward a proof of concept compound 33, which showed potent glucose lowering effects during an oral glucose tolerance test in mice and monkeys.

Entities:  

Keywords:  GPR142; agonist; diabetes; glucose lowering; insulin secretagogue

Year:  2013        PMID： 24900747      PMCID： PMC4027368          DOI： 10.1021/ml400186z

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  12 in total

1.  Novel metabolic bioactivation mechanism for a series of anti-inflammatory agents (2,5-diaminothiophene derivatives) mediated by cytochrome p450 enzymes.

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Journal:  Drug Metab Dispos       Date:  2010-06-07       Impact factor: 3.922

2.  Lipophilicity in drug discovery.

Authors:  Michael J Waring
Journal:  Expert Opin Drug Discov       Date:  2010-03       Impact factor: 6.098

3.  Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus.

Authors:  Mike Lizarzaburu; Simon Turcotte; Xiaohui Du; Jason Duquette; Angela Fu; Jonathan Houze; Leping Li; Jinqian Liu; Michiko Murakoshi; Kozo Oda; Ryo Okuyama; Futoshi Nara; Jeff Reagan; Ming Yu; Julio C Medina
Journal:  Bioorg Med Chem Lett       Date:  2012-07-23       Impact factor: 2.823

Review 4.  The therapeutic potential of GPR119 agonists for type 2 diabetes.

Authors:  Takahide Ohishi; Shigeru Yoshida
Journal:  Expert Opin Investig Drugs       Date:  2012-02-03       Impact factor: 6.206

5.  (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Authors:  Dooseop Kim; Liping Wang; Maria Beconi; George J Eiermann; Michael H Fisher; Huaibing He; Gerard J Hickey; Jennifer E Kowalchick; Barbara Leiting; Kathryn Lyons; Frank Marsilio; Margaret E McCann; Reshma A Patel; Aleksandr Petrov; Giovanna Scapin; Sangita B Patel; Ranabir Sinha Roy; Joseph K Wu; Matthew J Wyvratt; Bei B Zhang; Lan Zhu; Nancy A Thornberry; Ann E Weber
Journal:  J Med Chem       Date:  2005-01-13       Impact factor: 7.446

Review 6.  The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes.

Authors:  Daniel J Drucker; Michael A Nauck
Journal:  Lancet       Date:  2006-11-11       Impact factor: 79.321

7.  Risk of macrovascular and microvascular complications in Type 2 diabetes: results of longitudinal study design.

Authors:  Boguslawa Nazimek-Siewniak; DariuszK Moczulski; Wladyslaw Grzeszczak
Journal:  J Diabetes Complications       Date:  2002 Jul-Aug       Impact factor: 2.852

Review 8.  The role of sulphonylureas in the management of type 2 diabetes mellitus.

Authors:  Marc Rendell
Journal:  Drugs       Date:  2004       Impact factor: 9.546

9.  Phenylalanine derivatives as GPR142 agonists for the treatment of type II diabetes.

Authors:  Xiaohui Du; Yong-Jae Kim; Sujen Lai; Xi Chen; Mike Lizarzaburu; Simon Turcotte; Zice Fu; Qingxiang Liu; Ying Zhang; Alykhan Motani; Kozo Oda; Ryo Okuyama; Futoshi Nara; Michiko Murakoshi; Angela Fu; Jeff D Reagan; Peter Fan; Yumei Xiong; Wang Shen; Leping Li; Jonathan Houze; Julio C Medina
Journal:  Bioorg Med Chem Lett       Date:  2012-08-10       Impact factor: 2.823

10.  Banting Lecture. From the triumvirate to the ominous octet: a new paradigm for the treatment of type 2 diabetes mellitus.

Authors:  Ralph A Defronzo
Journal:  Diabetes       Date:  2009-04       Impact factor: 9.461
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  16 in total

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Journal:  Fam Cancer       Date:  2015-06       Impact factor: 2.375

2.  Discovery of DS-1558: A Potent and Orally Bioavailable GPR40 Agonist.

Authors:  Rieko Takano; Masao Yoshida; Masahiro Inoue; Takeshi Honda; Ryutaro Nakashima; Koji Matsumoto; Tatsuya Yano; Tsuneaki Ogata; Nobuaki Watanabe; Masakazu Hirouchi; Tomoko Yoneyama; Shuichiro Ito; Narihiro Toda
Journal:  ACS Med Chem Lett       Date:  2015-01-13       Impact factor: 4.345

Review 3.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

4.  Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.

Authors:  Liangqin Guo; Dann L Parker; Yi Zang; Ramzi F Sweis; Weiguo Liu; Edward C Sherer; Nicole Buist; Jenna Terebetski; Terri Kelly; Randal Bugianesi; Birgit T Priest; Karen H Dingley; Xiaofang Li; Stan Mitelman; Gino Salituro; Maria E Trujillo; Michele Pachanski; Melissa Kirkland; Mary Ann Powles; George J Eiermann; Yue Feng; Jin Shang; Andrew D Howard; Feroze Ujjainwalla; Christopher J Sinz; John S Debenham; Scott D Edmondson; Ravi P Nargund; William K Hagmann; Derun Li
Journal:  ACS Med Chem Lett       Date:  2016-10-12       Impact factor: 4.345

5.  Adaptive Changes in Glucose Homeostasis and Islet Function During Pregnancy: A Targeted Metabolomics Study in Mice.

Authors:  Ziyi Zhang; Anthony L Piro; Feihan F Dai; Michael B Wheeler
Journal:  Front Endocrinol (Lausanne)       Date:  2022-05-04       Impact factor: 6.055

Review 6.  Leveraging the Gut to Treat Metabolic Disease.

Authors:  Ruth E Gimeno; Daniel A Briere; Randy J Seeley
Journal:  Cell Metab       Date:  2020-03-17       Impact factor: 27.287

Review 7.  Glucagon-Like Peptide-1: Actions and Influence on Pancreatic Hormone Function.

Authors:  Ellen M Davis; Darleen A Sandoval
Journal:  Compr Physiol       Date:  2020-03-12       Impact factor: 8.915

Review 8.  Addressing unmet medical needs in type 2 diabetes: a narrative review of drugs under development.

Authors:  Friedrich Mittermayer; Erica Caveney; Claudia De Oliveira; Loukas Gourgiotis; Mala Puri; Li-Jung Tai; J Rick Turner
Journal:  Curr Diabetes Rev       Date:  2015

9.  GPR142 Agonists Stimulate Glucose-Dependent Insulin Secretion via Gq-Dependent Signaling.

Authors:  Jingru Wang; Juan J Carrillo; Hua V Lin
Journal:  PLoS One       Date:  2016-04-22       Impact factor: 3.240

10.  GPR142 Controls Tryptophan-Induced Insulin and Incretin Hormone Secretion to Improve Glucose Metabolism.

Authors:  Hua V Lin; Alexander M Efanov; Xiankang Fang; Lisa S Beavers; Xuesong Wang; Jingru Wang; Isabel C Gonzalez Valcarcel; Tianwei Ma
Journal:  PLoS One       Date:  2016-06-20       Impact factor: 3.240
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