Structural highlights
Function
[ALDR_HUMAN] Catalyzes the NADPH-dependent reduction of a wide variety of carbonyl-containing compounds to their corresponding alcohols with a broad range of catalytic efficiencies.
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
Efforts to identify treatments for chronic diabetic complications have resulted in the discovery of a novel series of highly potent and selective [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]ac etic acid aldose reductase inhibitors. The lead candidate, [6-methyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridi n-1-yl]acetic acid example 16, inhibits aldose reductase with an IC50 of 8 nM, while being inactive against aldehyde reductase (IC50>100 microM), a related enzyme involved in the detoxification of reactive aldehydes.
Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]ac etic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.,Van Zandt MC, Doan B, Sawicki DR, Sredy J, Podjarny AD Bioorg Med Chem Lett. 2009 Apr 1;19(7):2006-8. Epub 2009 Feb 12. PMID:19250825[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Van Zandt MC, Doan B, Sawicki DR, Sredy J, Podjarny AD. Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]ac etic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. Bioorg Med Chem Lett. 2009 Apr 1;19(7):2006-8. Epub 2009 Feb 12. PMID:19250825 doi:10.1016/j.bmcl.2009.02.037
