Literature DB >> 12781194

3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site.

Stephen W Wright1, Anthony A Carlo, Dennis E Danley, David L Hageman, George A Karam, Mahmoud N Mansour, Lester D McClure, Jayvardhan Pandit, Gayle K Schulte, Judith L Treadway, Ing-Kae Wang, Paul H Bauer.   

Abstract

3-(2-Carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid (MDL-29951), an antagonist of the glycine site of the NMDA receptor, has been found to be an allosteric inhibitor of the enzyme fructose 1,6-bisphosphatase. The compound binds at the AMP regulatory site by X-ray crystallography. This represents a new approach to inhibition of fructose 1,6-bisphosphatase and serves as a lead for further drug design.

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Year:  2003        PMID： 12781194     DOI： 10.1016/s0960-894x(03)00310-x

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


  6 in total

1.  Designing inhibitors against fructose 1,6-bisphosphatase: exploring natural products for novel inhibitor scaffolds.

Authors:  Sabrina Heng; Katharine M Harris; Evan R Kantrowitz
Journal:  Eur J Med Chem       Date:  2010-01-13       Impact factor: 6.514

2.  MB06322 (CS-917): A potent and selective inhibitor of fructose 1,6-bisphosphatase for controlling gluconeogenesis in type 2 diabetes.

Authors:  Mark D Erion; Paul D van Poelje; Qun Dang; Srinivas Rao Kasibhatla; Scott C Potter; M Rami Reddy; K Raja Reddy; Tao Jiang; William N Lipscomb
Journal:  Proc Natl Acad Sci U S A       Date:  2005-05-23       Impact factor: 11.205

3.  In silico identification of structure requirement for novel thiazole and oxazole derivatives as potent fructose 1,6-bisphosphatase inhibitors.

Authors:  Ming Hao; Xiaole Zhang; Hong Ren; Yan Li; Shuwei Zhang; Fang Luo; Mingjuan Ji; Guohui Li; Ling Yang
Journal:  Int J Mol Sci       Date:  2011-11-18       Impact factor: 5.923

4.  Toward the prediction of FBPase inhibitory activity using chemoinformatic methods.

Authors:  Ming Hao; Shuwei Zhang; Jieshan Qiu
Journal:  Int J Mol Sci       Date:  2012-06-07       Impact factor: 6.208

5.  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

6.  Modeling the metabolic interplay between a parasitic worm and its bacterial endosymbiont allows the identification of novel drug targets.

Authors:  David M Curran; Alexandra Grote; Nirvana Nursimulu; Adam Geber; Dennis Voronin; Drew R Jones; Elodie Ghedin; John Parkinson
Journal:  Elife       Date:  2020-08-11       Impact factor: 8.140
  6 in total

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