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| {{STRUCTURE_2aig| PDB=2aig | SCENE= }} | | {{STRUCTURE_2aig| PDB=2aig | SCENE= }} |
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| '''ADAMALYSIN II WITH PEPTIDOMIMETIC INHIBITOR POL647'''
| | ===ADAMALYSIN II WITH PEPTIDOMIMETIC INHIBITOR POL647=== |
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| ==Overview==
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| Crotalus adamanteus snake venom adamalysin II is the structural prototype of the adamalysin or ADAM family comprising proteolytic domains of snake venom metalloproteinases, multimodular mammalian reproductive tract proteins, and tumor necrosis factor alpha convertase, TACE, involved in the release of the inflammatory cytokine, TNFalpha. The structure of adamalysin II in noncovalent complex with two small-molecule right-hand side peptidomimetic inhibitors (Pol 647 and Pol 656) has been solved using X-ray diffraction data up to 2.6 and 2.8 A resolution. The inhibitors bind to the S'-side of the proteinase, inserting between two protein segments, establishing a mixed parallel-antiparallel three-stranded beta-sheet and coordinate the central zinc ion in a bidentate manner via their two C-terminal oxygen atoms. The proteinase-inhibitor complexes are described in detail and are compared with other known structures. An adamalysin-based model of the active site of TACE reveals that these small molecules would probably fit into the active site cleft of this latter metalloproteinase, providing a starting model for the rational design of TACE inhibitors.
| | The line below this paragraph, {{ABSTRACT_PUBMED_9521103}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 9521103 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_9521103}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Snake venom]] | | [[Category: Snake venom]] |
| [[Category: Zinc protease]] | | [[Category: Zinc protease]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Apr 30 13:56:47 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 02:42:50 2008'' |
