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

  • Bioorg Med Chem Lett. 2003 Jun 16;13(12):2055-8. doi: 10.1016/s0960-894x(03)00310-x.
Stephen W Wright  1 ,  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
Affiliations
  • 1. Pfizer Central Research, Eastern Point Road, Box 8220-3141, Groton, CT 06340, USA. [email protected]
PMID: 12781194 DOI: 10.1016/s0960-894x(03)00310-x
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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