3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site |
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| Authors: | Wright Stephen W Carlo Anthony A Danley Dennis E Hageman David L Karam George A Mansour Mahmoud N McClure Lester D Pandit Jayvardhan Schulte Gayle K Treadway Judith L Wang Ing-Kae Bauer Paul H |
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| Affiliation: | Pfizer Central Research, Eastern Point Road, Box 8220-3141, Groton, CT 06340, USA. stephen_w_wright@groton.pfizer.com |
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| 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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