1ad8
From Proteopedia
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==About this Structure== | ==About this Structure== | ||
| - | 1AD8 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 NA and MDL as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/ | + | 1AD8 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 NA and MDL as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/Thrombin Thrombin]], 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: CAT. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1AD8 OCA]]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| + | [[Category: Thrombin]] | ||
[[Category: Malikayil, J.A.]] | [[Category: Malikayil, J.A.]] | ||
[[Category: Schreuder, H.]] | [[Category: Schreuder, H.]] | ||
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[[Category: serine protease]] | [[Category: serine protease]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 10:34:29 2007'' |
Revision as of 08:29, 30 October 2007
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COMPLEX OF THROMBIN WITH AND INHIBITOR CONTAINING A NOVEL P1 MOIETY
Overview
An inhibitor of alpha-thrombin was designed on the basis of the X-ray, crystal structures of thrombin and trypsin. The design strategy employed, the geometric and electrostatic differences between the specificity, pockets of the two enzymes. These differences arise due to the replacement, of Ser 190 in trypsin by Ala 190 in thrombin. The new inhibitor contained, a tryptophan side chain instead of the arginine side chain that is present, in the prototypical thrombin inhibitors. This inhibitor had a Ki value of, 0.25 microM, displayed more than 400-fold specificity for thrombin over, trypsin, and doubled the rat plasma APTT at a concentration of 44.9, microM. The X-ray crystal structure of the inhibitor/alpha-thrombin, complex was determined. This represents the first reported, ... [(full description)]
About this Structure
1AD8 is a [Protein complex] structure of sequences from [Hirudo medicinalis] and [Homo sapiens] with NA and MDL as [ligands]. Active as [Thrombin], with EC number [3.4.21.5]. Structure known Active Site: CAT. Full crystallographic information is available from [OCA].
Reference
Molecular design and characterization of an alpha-thrombin inhibitor containing a novel P1 moiety., Malikayil JA, Burkhart JP, Schreuder HA, Broersma RJ Jr, Tardif C, Kutcher LW 3rd, Mehdi S, Schatzman GL, Neises B, Peet NP, Biochemistry. 1997 Feb 4;36(5):1034-40. PMID:9033393
Page seeded by OCA on Tue Oct 30 10:34:29 2007
