5gds: Difference between revisions
New page: left|200px<br /> <applet load="5gds" size="450" color="white" frame="true" align="right" spinBox="true" caption="5gds, resolution 2.1Å" /> '''HIRUNORMS ARE TRUE H... |
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==About this Structure== | ==About this Structure== | ||
5GDS is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with NAG 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=5GDS OCA]]. | 5GDS is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with NAG as [[http://en.wikipedia.org/wiki/ligand ligand]]. 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=5GDS OCA]]. | ||
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Thrombin]] | |||
[[Category: Bolognesi, M.]] | [[Category: Bolognesi, M.]] | ||
[[Category: Galdiero, S.]] | [[Category: Galdiero, S.]] | ||
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[[Category: thrombin synthetic inhibitors]] | [[Category: thrombin synthetic inhibitors]] | ||
''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 12:19:54 2007'' | ||
Revision as of 13:15, 30 October 2007
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HIRUNORMS ARE TRUE HIRUDIN MIMETICS. THE CRYSTAL STRUCTURE OF HUMAN ALPHA-THROMBIN:HIRUNORM V COMPLEX
OverviewOverview
A novel class of synthetic, multisite-directed thrombin inhibitors, known, as hirunorms, has been described recently. These compounds were designed, to mimic the binding mode of hirudin, and they have been proven to be very, strong and selective thrombin inhibitors. Here we report the crystal, structure of the complex formed by human alpha-thrombin and hirunorm V, a, 26-residue polypeptide containing non-natural amino acids, determined at, 2.1 A resolution and refined to an R-factor of 0.176. The structure, reveals that the inhibitor binding mode is distinctive of a true hirudin, mimetic, and it highlights the molecular basis of the high inhibitory, potency (Ki is in the picomolar range) and the strong selectivity of, hirunorm V. Hirunorm V interacts through the N-terminal tetrapeptide ... [(full description)]
About this StructureAbout this Structure
5GDS is a [Single protein] structure of sequence from [Homo sapiens] with NAG as [ligand]. Active as [Thrombin], with EC number [3.4.21.5]. Structure known Active Site: CAT. Full crystallographic information is available from [OCA].
ReferenceReference
Hirunorms are true hirudin mimetics. The crystal structure of human alpha-thrombin-hirunorm V complex., De Simone G, Lombardi A, Galdiero S, Nastri F, Della Morte R, Staiano N, Pedone C, Bolognesi M, Pavone V, Protein Sci. 1998 Feb;7(2):243-53. PMID:9521099
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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- Homo sapiens
- Single protein
- Thrombin
- Bolognesi, M.
- Galdiero, S.
- Lombardi, A.
- Morte, R.Della.
- Nastri, F.
- Pavone, V.
- Pedone, C.
- Simone, G.De.
- Staiano, N.
- NAG
- Antithrombotics
- Blood coagulation
- Complex (serine protease/inhibitor)
- Hirudin-like binding mode
- Hirunorms
- Thrombin synthetic inhibitors