1dth

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==Overview==
==Overview==
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Matrix metalloproteinase enzymes have been implicated in degenerative, processes like tumor cell invasion, metastasis, and arthritis. Specific, metalloproteinase inhibitors have been used to block tumor cell, proliferation. We have examined the interaction of batimastat (BB-94) with, a metalloproteinase [atrolysin C (Ht-d), EC 3.4.24.42] active site at, 2.0-angstroms resolution (R = 16.8%). The title structure exhibits an, unexpected binding geometry, with the thiophene ring deeply inserted into, the primary specificity site. This unprecedented binding geometry, dramatizes the significance of the cavernous primary specificity site, pointing the way for the design of a new generation of potential antitumor, drugs.
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Matrix metalloproteinase enzymes have been implicated in degenerative processes like tumor cell invasion, metastasis, and arthritis. Specific metalloproteinase inhibitors have been used to block tumor cell proliferation. We have examined the interaction of batimastat (BB-94) with a metalloproteinase [atrolysin C (Ht-d), EC 3.4.24.42] active site at 2.0-angstroms resolution (R = 16.8%). The title structure exhibits an unexpected binding geometry, with the thiophene ring deeply inserted into the primary specificity site. This unprecedented binding geometry dramatizes the significance of the cavernous primary specificity site, pointing the way for the design of a new generation of potential antitumor drugs.
==About this Structure==
==About this Structure==
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Botos, I.]]
[[Category: Botos, I.]]
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[[Category: Liotta, L.A.]]
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[[Category: Liotta, L A.]]
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[[Category: Meyer, E.F.]]
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[[Category: Meyer, E F.]]
[[Category: Scapozza, L.]]
[[Category: Scapozza, L.]]
[[Category: Zhang, D.]]
[[Category: Zhang, D.]]
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[[Category: zinc]]
[[Category: zinc]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 09:35:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:20:15 2008''

Revision as of 10:20, 21 February 2008


1dth, resolution 2.0Å

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METALLOPROTEASE

Overview

Matrix metalloproteinase enzymes have been implicated in degenerative processes like tumor cell invasion, metastasis, and arthritis. Specific metalloproteinase inhibitors have been used to block tumor cell proliferation. We have examined the interaction of batimastat (BB-94) with a metalloproteinase [atrolysin C (Ht-d), EC 3.4.24.42] active site at 2.0-angstroms resolution (R = 16.8%). The title structure exhibits an unexpected binding geometry, with the thiophene ring deeply inserted into the primary specificity site. This unprecedented binding geometry dramatizes the significance of the cavernous primary specificity site, pointing the way for the design of a new generation of potential antitumor drugs.

About this Structure

1DTH is a Single protein structure of sequence from Crotalus atrox with , and as ligands. Active as Atrolysin C, with EC number 3.4.24.42 Known structural/functional Sites: , , and . Full crystallographic information is available from OCA.

Reference

Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding., Botos I, Scapozza L, Zhang D, Liotta LA, Meyer EF, Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54. PMID:8610113

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