1biw

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==Overview==
==Overview==
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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.
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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.
==Disease==
==Disease==
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Stromelysin 1]]
[[Category: Stromelysin 1]]
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[[Category: Almstead, N.G.]]
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[[Category: Almstead, N G.]]
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[[Category: Anastasio, M.B.]]
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[[Category: Anastasio, M B.]]
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[[Category: Barnett, B.L.]]
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[[Category: Barnett, B L.]]
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[[Category: Bradley, R.S.]]
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[[Category: Bradley, R S.]]
[[Category: Cheng, M.]]
[[Category: Cheng, M.]]
[[Category: De, B.]]
[[Category: De, B.]]
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[[Category: Dunaway, C.M.]]
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[[Category: Dunaway, C M.]]
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[[Category: McIver, J.M.]]
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[[Category: McIver, J M.]]
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[[Category: McPhail, S.J.]]
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[[Category: McPhail, S J.]]
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[[Category: Mieling, G.E.]]
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[[Category: Mieling, G E.]]
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[[Category: Natchus, M.G.]]
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[[Category: Natchus, M G.]]
[[Category: Pikul, S.]]
[[Category: Pikul, S.]]
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[[Category: Snider, C.E.]]
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[[Category: Snider, C E.]]
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[[Category: Taiwo, Y.O.]]
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[[Category: Taiwo, Y O.]]
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[[Category: Wahl, C.T.]]
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[[Category: Wahl, C T.]]
[[Category: CA]]
[[Category: CA]]
[[Category: S80]]
[[Category: S80]]
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[[Category: structure-based drug design]]
[[Category: structure-based drug design]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 15:32:20 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 11:55:46 2008''

Revision as of 09:55, 21 February 2008


1biw, resolution 2.5Å

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DESIGN AND SYNTHESIS OF CONFORMATIONALLY-CONSTRAINED MMP INHIBITORS

Contents

Overview

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.

Disease

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

About 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.

Reference

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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