Literature DB >> 17502136

Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).

Richard Sulsky1, David R Magnin, Yanting Huang, Ligaya Simpkins, Prakash Taunk, Manorama Patel, Yeheng Zhu, Terry R Stouch, Donna Bassolino-Klimas, Rex Parker, Thomas Harrity, Robert Stoffel, David S Taylor, Thomas B Lavoie, Kevin Kish, Bruce L Jacobson, Steven Sheriff, Leonard P Adam, William R Ewing, Jeffrey A Robl.   

Abstract

Herein we report the first disclosure of biphenyl azoles that are nanomolar binders of adipocyte fatty acid binding protein (aFABP or aP2) with up to thousand-fold selectivity against muscle fatty acid binding protein and epidermal fatty acid binding protein. In addition a new radio-ligand to determine binding against the three fatty acid binding proteins was also synthesized.

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Year:  2006        PMID: 17502136     DOI: 10.1016/j.bmcl.2006.12.044

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


  47 in total

1.  Vasculo-protective effect of BMS-309403 is independent of its specific inhibition of fatty acid-binding protein 4.

Authors:  Yuta Okamura; Kosuke Otani; Akihiro Sekiguchi; Taisuke Kogane; Chiharu Kakuda; Yuzaburo Sakamoto; Tomoko Kodama; Muneyoshi Okada; Hideyuki Yamawaki
Journal:  Pflugers Arch       Date:  2017-04-13       Impact factor: 3.657

2.  Evidence for bidirectional endocannabinoid transport across cell membranes.

Authors:  Andrea Chicca; Janine Marazzi; Simon Nicolussi; Jürg Gertsch
Journal:  J Biol Chem       Date:  2012-08-09       Impact factor: 5.157

3.  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

4.  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

5.  Hydrogen-bonded His93 as a sensitive probe for identifying inhibitors of the endocannabinoid transport protein FABP7.

Authors:  Sergiy Tyukhtenko; Karrie Chan; Rubin Jiang; Han Zhou; Richard W Mercier; De-Ping Yang; Alexandros Makriyannis; Jason J Guo
Journal:  Chem Biol Drug Des       Date:  2014-10-16       Impact factor: 2.817

6.  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

7.  Adipocyte fatty acid-binding protein modulates inflammatory responses in macrophages through a positive feedback loop involving c-Jun NH2-terminal kinases and activator protein-1.

Authors:  Xiaoyan Hui; Huiying Li; Zhiguang Zhou; Karen S L Lam; Yang Xiao; Donghai Wu; Ke Ding; Yu Wang; Paul M Vanhoutte; Aimin Xu
Journal:  J Biol Chem       Date:  2010-02-09       Impact factor: 5.157

Review 8.  Small lipid-binding proteins in regulating endothelial and vascular functions: focusing on adipocyte fatty acid binding protein and lipocalin-2.

Authors:  Yu Wang
Journal:  Br J Pharmacol       Date:  2012-02       Impact factor: 8.739

9.  Fatty acid binding protein-4 (FABP4) is a hypoxia inducible gene that sensitizes mice to liver ischemia/reperfusion injury.

Authors:  Bingfang Hu; Yan Guo; Wojciech G Garbacz; Mengxi Jiang; Meishu Xu; Hai Huang; Allan Tsung; Timothy R Billiar; Sadeesh K Ramakrishnan; Yatrik M Shah; Karen S L Lam; Min Huang; Wen Xie
Journal:  J Hepatol       Date:  2015-06-10       Impact factor: 25.083

10.  Endothelial APLNR regulates tissue fatty acid uptake and is essential for apelin's glucose-lowering effects.

Authors:  Cheol Hwangbo; Jingxia Wu; Irinna Papangeli; Takaomi Adachi; Bikram Sharma; Saejeong Park; Lina Zhao; Hyekyung Ju; Gwang-Woong Go; Guoliang Cui; Mohammed Inayathullah; Judith K Job; Jayakumar Rajadas; Stephanie L Kwei; Ming O Li; Alan R Morrison; Thomas Quertermous; Arya Mani; Kristy Red-Horse; Hyung J Chun
Journal:  Sci Transl Med       Date:  2017-09-13       Impact factor: 17.956

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