1awf: Difference between revisions
New page: left|200px<br /> <applet load="1awf" size="450" color="white" frame="true" align="right" spinBox="true" caption="1awf, resolution 2.2Å" /> '''NOVEL COVALENT THROM... |
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==About this Structure== | ==About this Structure== | ||
1AWF is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Hirudo_medicinalis Hirudo medicinalis]] and [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with GR4 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1AWF OCA]]. | 1AWF is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Hirudo_medicinalis Hirudo medicinalis]] and [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with GR4 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/Hydrolase Hydrolase]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5]]. Structure known Active Site: NUL. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1AWF OCA]]. | ||
==Reference== | ==Reference== | ||
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[[Category: trypsin like proteinase]] | [[Category: trypsin like proteinase]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 08:43:08 2007'' | ||
Revision as of 09:38, 30 October 2007
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NOVEL COVALENT THROMBIN INHIBITOR FROM PLANT EXTRACT
OverviewOverview
High-throughput screening of methanolic extracts from the leaves of the, plant Lantana camara identified potent inhibitors of human alpha-thrombin, which were shown to be 5,5-trans-fused cyclic lactone euphane triterpenes, [O'Neill et al. (1998) J. Nat. Prod. (submitted for publication)]., Proflavin displacement studies showed the inhibitors to bind at the active, site of alpha-thrombin and alpha-chymotrypsin. Kinetic analysis of, alpha-thrombin showed tight-binding reversible competitive inhibition by, both compounds, named GR133487 and GR133686, with respective kon values at, pH 8.4 of 1.7 x 10(6) s-1 M-1 and 4.6 x 10(6) s-1 M-1. Electrospray, ionization mass spectrometry of thrombin/inhibitor complexes showed the, tight-bound species to be covalently attached, suggesting acyl-enzyme, ... [(full description)]
About this StructureAbout this Structure
1AWF is a [Protein complex] structure of sequences from [Hirudo medicinalis] and [Homo sapiens] with GR4 as [ligand]. Active as [Hydrolase], with EC number [3.4.21.5]. Structure known Active Site: NUL. Full crystallographic information is available from [OCA].
ReferenceReference
Novel natural product 5,5-trans-lactone inhibitors of human alpha-thrombin: mechanism of action and structural studies., Weir MP, Bethell SS, Cleasby A, Campbell CJ, Dennis RJ, Dix CJ, Finch H, Jhoti H, Mooney CJ, Patel S, Tang CM, Ward M, Wonacott AJ, Wharton CW, Biochemistry. 1998 May 12;37(19):6645-57. PMID:9578548
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