Literature DB >> 19188063

Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators.

Teruyuki Nishimura1, Tomoharu Iino, Morihiro Mitsuya, Makoto Bamba, Hitomi Watanabe, Daisuke Tsukahara, Kenji Kamata, Kaori Sasaki, Sumika Ohyama, Hideka Hosaka, Mayumi Futamura, Yasufumi Nagata, Jun-Ichi Eiki.   

Abstract

The identification and structure-activity-relationships (SARs) of novel 2-amino benzamide glucokinase activators are described. Compounds in this series were developed to be potent GK activators, and their binding mode to the GK protein was determined by crystal structure analysis. In vivo pharmacokinetic and acute in vivo efficacy studies of compound 18 are also described.

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Year:  2009        PMID: 19188063     DOI: 10.1016/j.bmcl.2009.01.053

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

1.  The use of docking-based comparative intermolecular contacts analysis to identify optimal docking conditions within glucokinase and to discover of new GK activators.

Authors:  Mutasem O Taha; Maha Habash; Mohammad A Khanfar
Journal:  J Comput Aided Mol Des       Date:  2014-03-08       Impact factor: 3.686

2.  Identification of RO4597014, a Glucokinase Activator Studied in the Clinic for the Treatment of Type 2 Diabetes.

Authors:  Yimin Qian; Wendy L Corbett; Steven J Berthel; Duk Soon Choi; Mark T Dvorozniak; Wanping Geng; Paul Gillespie; Kevin R Guertin; Nancy-Ellen Haynes; Robert F Kester; Francis A Mennona; David Moore; Jagdish Racha; Roumen Radinov; Ramakanth Sarabu; Nathan R Scott; Joseph Grimsby; Navita L Mallalieu
Journal:  ACS Med Chem Lett       Date:  2013-03-07       Impact factor: 4.345

3.  Nanosecond-Timescale Dynamics and Conformational Heterogeneity in Human GCK Regulation and Disease.

Authors:  Shawn M Sternisha; A Carl Whittington; Juliana A Martinez Fiesco; Carol Porter; Malcolm M McCray; Timothy Logan; Cristina Olivieri; Gianluigi Veglia; Peter J Steinbach; Brian G Miller
Journal:  Biophys J       Date:  2020-01-14       Impact factor: 4.033

4.  Strain analysis of protein structures and low dimensionality of mechanical allosteric couplings.

Authors:  Michael R Mitchell; Tsvi Tlusty; Stanislas Leibler
Journal:  Proc Natl Acad Sci U S A       Date:  2016-09-21       Impact factor: 11.205

Review 5.  Homotropic allosteric regulation in monomeric mammalian glucokinase.

Authors:  Mioara Larion; Brian G Miller
Journal:  Arch Biochem Biophys       Date:  2011-11-15       Impact factor: 4.013

Review 6.  Molecular and cellular regulation of human glucokinase.

Authors:  Shawn M Sternisha; Brian G Miller
Journal:  Arch Biochem Biophys       Date:  2019-01-11       Impact factor: 4.013

7.  Small-Molecule Allosteric Activation of Human Glucokinase in the Absence of Glucose.

Authors:  Joseph M Bowler; Katherine L Hervert; Mark L Kearley; Brian G Miller
Journal:  ACS Med Chem Lett       Date:  2013-09-05       Impact factor: 4.345

8.  Order-disorder transitions govern kinetic cooperativity and allostery of monomeric human glucokinase.

Authors:  Mioara Larion; Roberto Kopke Salinas; Lei Bruschweiler-Li; Brian G Miller; Rafael Brüschweiler
Journal:  PLoS Biol       Date:  2012-12-18       Impact factor: 8.029

  8 in total

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