Literature DB >> 19762234

Synthesis, SAR, and X-ray structure of tricyclic compounds as potent FBPase inhibitors.

Tomoharu Tsukada1, Mizuki Takahashi, Toshiyasu Takemoto, Osamu Kanno, Takahiro Yamane, Sayako Kawamura, Takahide Nishi.   

Abstract

With the aim of discovering a novel class of fructose-1,6-bisphosphatase (FBPase) inhibitors, a series of compounds based on tricyclic scaffolds was synthesized. Extensive SAR studies led to the finding of 8l with an IC50 value of 0.013 microM against human FBPase. An X-ray crystallographic study revealed that 8l bound at AMP binding sites of human liver FBPase with hydrogen bonding interactions similar to AMP.

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Year:  2009        PMID: 19762234     DOI: 10.1016/j.bmcl.2009.08.081

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


  3 in total

1.  Discovery of Novel Indole Derivatives as Fructose-1,6-bisphosphatase Inhibitors and X-ray Cocrystal Structures Analysis.

Authors:  Xiaoyu Wang; Rui Zhao; Wenming Ji; Jie Zhou; Quan Liu; Linxiang Zhao; Zhufang Shen; Shuainan Liu; Bailing Xu
Journal:  ACS Med Chem Lett       Date:  2021-12-20       Impact factor: 4.345

2.  Quadruple space-group ambiguity owing to rotational and translational noncrystallographic symmetry in human liver fructose-1,6-bisphosphatase.

Authors:  Armin Ruf; Tim Tetaz; Brigitte Schott; Catherine Joseph; Markus G Rudolph
Journal:  Acta Crystallogr D Struct Biol       Date:  2016-10-28       Impact factor: 7.652

3.  Structures of Leishmania Fructose-1,6-Bisphosphatase Reveal Species-Specific Differences in the Mechanism of Allosteric Inhibition.

Authors:  Meng Yuan; Montserrat G Vásquez-Valdivieso; Iain W McNae; Paul A M Michels; Linda A Fothergill-Gilmore; Malcolm D Walkinshaw
Journal:  J Mol Biol       Date:  2017-09-04       Impact factor: 5.469

  3 in total

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