Literature DB >> 24944745

Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.

Derun Li1, Zhicai Wu1, Yang Yu1, Richard G Ball1, Liangqin Guo1, Edward Sherer1, Shuwen He1, Qingmei Hong1, Zhong Lai1, Hongbo Qi1, Quang Truong1, David X Yang1, Gary G Chicchi1, Kwei-Lan Tsao1, Dorina Trusca1, Maria Trujillo1, Michele Pachanski1, George J Eiermann1, Andrew D Howard1, Yun-Ping Zhou1, Bei B Zhang1, Ravi P Nargund1, William K Hagmann1.   

Abstract

A novel class of small-molecule, highly potent, and subtype-selective somatostatin SST3 agonists was discovered through modification of a SST3 antagonist. As an example, (1R,2S)-9 demonstrated not only potent in vitro SST3 agonist activity but also in vivo SST3 agonist activity in a mouse oral glucose tolerance test (OGTT). These agonists may be useful reagents for studying the physiological roles of the SST3 receptor and may potentially be useful as therapeutic agents.

Entities:  

Keywords:  GPCR; Somatostatin; small-molecule SST3 agonists; somatostin receptor subtype 3 (SST3)

Year:  2014        PMID： 24944745      PMCID： PMC4060944          DOI： 10.1021/ml500079u

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


  23 in total

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8.  The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.

Authors:  Shuwen He; Zhixiong Ye; Quang Truong; Shrenik Shah; Wu Du; Liangqin Guo; Peter H Dobbelaar; Zhong Lai; Jian Liu; Tianying Jian; Hongbo Qi; Raman K Bakshi; Qingmei Hong; James Dellureficio; Alexander Pasternak; Zhe Feng; Reynalda deJesus; Lihu Yang; Mikhail Reibarkh; Scott A Bradley; Mark A Holmes; Richard G Ball; Rebecca T Ruck; Mark A Huffman; Frederick Wong; Koppara Samuel; Vijay B Reddy; Stan Mitelman; Sharon X Tong; Gary G Chicchi; Kwei-Lan Tsao; Dorina Trusca; Margaret Wu; Qing Shao; Maria E Trujillo; George J Eiermann; Cai Li; Bei B Zhang; Andrew D Howard; Yun-Ping Zhou; Ravi P Nargund; William K Hagmann
Journal:  ACS Med Chem Lett       Date:  2012-05-07       Impact factor: 4.345

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10.  Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice.

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  1 in total

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Authors:  Thomas Günther; Giovanni Tulipano; Pascal Dournaud; Corinne Bousquet; Zsolt Csaba; Hans-Jürgen Kreienkamp; Amelie Lupp; Márta Korbonits; Justo P Castaño; Hans-Jürgen Wester; Michael Culler; Shlomo Melmed; Stefan Schulz
Journal:  Pharmacol Rev       Date:  2018-10       Impact factor: 25.468
  1 in total

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