DESIGN AND SYNTHESIS OF CONFORMATIONALLY-CONSTRAINED MMP INHIBITORS

File:1biw.jpg


1biw, resolution 2.5Å

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OverviewOverview

A novel series of conformationally constrained matrix metalloprotease inhibitors was identified. The potencies observed for these inhibitors were highly dependent upon the substitution pattern on the caprolactam ring as well as the succinate moiety.

DiseaseDisease

Known diseases associated with this structure: Coronary heart disease, susceptibility to OMIM:[185250]

About this StructureAbout this Structure

1BIW is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Stromelysin 1, with EC number 3.4.24.17 Full crystallographic information is available from OCA.

ReferenceReference

Design and synthesis of conformationally-constrained MMP inhibitors., Natchus MG, Cheng M, Wahl CT, Pikul S, Almstead NG, Bradley RS, Taiwo YO, Mieling GE, Dunaway CM, Snider CE, McIver JM, Barnett BL, McPhail SJ, Anastasio MB, De B, Bioorg Med Chem Lett. 1998 Aug 18;8(16):2077-80. PMID:9873489

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