Literature DB >> 15357969

Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target.

Fredik Lehmann1, Saba Haile, Eva Axen, Carmen Medina, Jonas Uppenberg, Stefan Svensson, Thomas Lundbäck, Lena Rondahl, Tjeerd Barf.   

Abstract

Low micromolar human A-FABP inhibitors were found by utilizing a fluorescence polarization assay, X-ray crystallography and modeling. The carbazole- and indole-based inhibitors displayed approximately 10-fold preferences over human H-FABP and E-FABP, and are highly selective against I-FABP. This communication describes the SAR for drug-like synthetic inhibitors of human A-FABP.

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Year:  2004        PMID： 15357969     DOI： 10.1016/j.bmcl.2004.06.057

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


  22 in total

1.  BMS309403 directly suppresses cardiac contractile function.

Authors:  Christiane Look; Ingo Morano; Monika Ehrhart-Bornstein; Stefan R Bornstein; Valéria Lamounier-Zepter
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2011-07-16       Impact factor: 3.000

2.  Structural analysis of ibuprofen binding to human adipocyte fatty-acid binding protein (FABP4).

Authors:  Javier M González; S Zoë Fisher
Journal:  Acta Crystallogr F Struct Biol Commun       Date:  2015-01-28       Impact factor: 1.056

3.  Interaction Analysis of FABP4 Inhibitors by X-ray Crystallography and Fragment Molecular Orbital Analysis.

Authors:  Uno Tagami; Kazutoshi Takahashi; Shunsuke Igarashi; Chieko Ejima; Tomomi Yoshida; Sen Takeshita; Wataru Miyanaga; Masayuki Sugiki; Munetaka Tokumasu; Toshihiro Hatanaka; Tatsuki Kashiwagi; Kohki Ishikawa; Hiroshi Miyano; Toshimi Mizukoshi
Journal:  ACS Med Chem Lett       Date:  2016-02-16       Impact factor: 4.345

4.  Calcium-dependent release of adipocyte fatty acid binding protein from human adipocytes.

Authors:  I Schlottmann; M Ehrhart-Bornstein; M Wabitsch; S R Bornstein; V Lamounier-Zepter
Journal:  Int J Obes (Lond)       Date:  2013-12-19       Impact factor: 5.095

5.  Dimethylaminophenyl Hydrazides as Inhibitors of the Lipid Transport Protein LprG in Mycobacteria.

Authors:  Lu Bai; Lia A Parkin; Hong Zhang; Rebecca Shum; Mary L Previti; Jessica C Seeliger
Journal:  ACS Infect Dis       Date:  2020-03-03       Impact factor: 5.084

6.  Benzbromarone, an old uricosuric drug, inhibits human fatty acid binding protein 4 in vitro and lowers the blood glucose level in db/db mice.

Authors:  Hai-yan Cai; Ting Wang; Jian-chun Zhao; Peng Sun; Gui-rui Yan; Hai-peng Ding; Ying-xia Li; He-yao Wang; Wei-liang Zhu; Kai-xian Chen
Journal:  Acta Pharmacol Sin       Date:  2013-09-30       Impact factor: 6.150

7.  Small-molecule inhibitors of FABP4/5 ameliorate dyslipidemia but not insulin resistance in mice with diet-induced obesity.

Authors:  Hong Lan; Cliff C Cheng; Timothy J Kowalski; Ling Pang; Lixin Shan; Cheng-Chi Chuang; James Jackson; Alberto Rojas-Triana; Loretta Bober; Li Liu; Johannes Voigt; Peter Orth; Xianshu Yang; Gerald W Shipps; Joseph A Hedrick
Journal:  J Lipid Res       Date:  2011-02-04       Impact factor: 5.922

8.  Expression, purification, crystallization and structure of human adipocyte lipid-binding protein (aP2).

Authors:  Eric Marr; Mark Tardie; Maynard Carty; Tracy Brown Phillips; Ing-Kae Wang; Walt Soeller; Xiayang Qiu; George Karam
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2006-10-25

Review 9.  Fatty acid-binding proteins: role in metabolic diseases and potential as drug targets.

Authors:  Masato Furuhashi; Gökhan S Hotamisligil
Journal:  Nat Rev Drug Discov       Date:  2008-06       Impact factor: 84.694

Review 10.  Metabolic functions of FABPs--mechanisms and therapeutic implications.

Authors:  Gökhan S Hotamisligil; David A Bernlohr
Journal:  Nat Rev Endocrinol       Date:  2015-08-11       Impact factor: 43.330
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