1biw
From Proteopedia
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|PDB= 1biw |SIZE=350|CAPTION= <scene name='initialview01'>1biw</scene>, resolution 2.5Å | |PDB= 1biw |SIZE=350|CAPTION= <scene name='initialview01'>1biw</scene>, resolution 2.5Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=S80:N1-HYDROXY-2-(3-HYDROXY-PROPYL)-3-ISOBUTYL-N4-[1-(2-METHOXY-ETHYL)-2-OXO-AZEPAN-3-YL]-SUCCINAMIDE'>S80</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> |
| - | |ACTIVITY= [http://en.wikipedia.org/wiki/Stromelysin_1 Stromelysin 1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.17 3.4.24.17] | + | |ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Stromelysin_1 Stromelysin 1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.17 3.4.24.17] </span> |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1biw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1biw OCA], [http://www.ebi.ac.uk/pdbsum/1biw PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1biw RCSB]</span> | ||
}} | }} | ||
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==Overview== | ==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. | 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:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=185250 185250]] | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Taiwo, Y O.]] | [[Category: Taiwo, Y O.]] | ||
[[Category: Wahl, C T.]] | [[Category: Wahl, C T.]] | ||
| - | [[Category: CA]] | ||
| - | [[Category: S80]] | ||
| - | [[Category: ZN]] | ||
[[Category: matrix metalloprotease]] | [[Category: matrix metalloprotease]] | ||
[[Category: osteoarthritis]] | [[Category: osteoarthritis]] | ||
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[[Category: structure-based drug design]] | [[Category: structure-based drug design]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 19:01:57 2008'' |
Revision as of 16:02, 30 March 2008
| |||||||
| , resolution 2.5Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , | ||||||
| Activity: | Stromelysin 1, with EC number 3.4.24.17 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
DESIGN AND SYNTHESIS OF CONFORMATIONALLY-CONSTRAINED MMP INHIBITORS
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.
About this Structure
1BIW is a Single protein structure of sequence from Homo sapiens. 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
Page seeded by OCA on Sun Mar 30 19:01:57 2008
Categories: Homo sapiens | Single protein | Stromelysin 1 | Almstead, N G. | Anastasio, M B. | Barnett, B L. | Bradley, R S. | Cheng, M. | De, B. | Dunaway, C M. | McIver, J M. | McPhail, S J. | Mieling, G E. | Natchus, M G. | Pikul, S. | Snider, C E. | Taiwo, Y O. | Wahl, C T. | Matrix metalloprotease | Osteoarthritis | Protein crystal structure | Stromelysin | Structure-based drug design
