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

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 repres...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-06, Vol.13 (12), p.2055-2058
Main Authors: WRIGHT, Stephen W, CARLO, Anthony A, WANG, Ing-Kae, BAUER, Paul H, DANLEY, Dennis E, HAGEMAN, David L, KARAM, George A, MANSOUR, Mahmoud N, MCCLURE, Lester D, PANDIT, Jayvardhan, SCHULTE, Gayle K, TREADWAY, Judith L
Format: Article
Language:English
Subjects:
Adenosine Monophosphate - metabolism
Allosteric Site
Animals
Biological and medical sciences
Crystallography, X-Ray
Dose-Response Relationship, Drug
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - metabolism
Enzyme Inhibitors - pharmacology
Fructose-Bisphosphatase - antagonists & inhibitors
Fructose-Bisphosphatase - metabolism
General and cellular metabolism. Vitamins
Humans
Indoles - chemistry
Indoles - metabolism
Indoles - pharmacology
Medical sciences
Models, Molecular
Pharmacology. Drug treatments
Propionates - chemistry
Propionates - metabolism
Propionates - pharmacology
Rabbits
Rats
Recombinant Proteins - antagonists & inhibitors
Recombinant Proteins - metabolism
Structure-Activity Relationship
Swine
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00310-X