1o0d: Difference between revisions

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==Overview==
==Overview==
Synthesis of thrombin inhibitors and their binding mode to thrombin is, described. Modification of the P1 moiety leads to an increased selectivity, versus trypsin. The observed selectivity is discussed in view of their, thrombin-inhibitor complex X-ray structures.
Synthesis of thrombin inhibitors and their binding mode to thrombin is described. Modification of the P1 moiety leads to an increased selectivity versus trypsin. The observed selectivity is discussed in view of their thrombin-inhibitor complex X-ray structures.


==Disease==
==Disease==
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[[Category: Thrombin]]
[[Category: Thrombin]]
[[Category: Bauke, D.]]
[[Category: Bauke, D.]]
[[Category: Hoeffken, H.W.]]
[[Category: Hoeffken, H W.]]
[[Category: Hornberger, W.]]
[[Category: Hornberger, W.]]
[[Category: Lange, U.E.]]
[[Category: Lange, U E.]]
[[Category: Mack, H.]]
[[Category: Mack, H.]]
[[Category: Seitz, W.]]
[[Category: Seitz, W.]]
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[[Category: ternary complex; thrombin/active-site inhibitor/exo-site inhibitor]]
[[Category: ternary complex; thrombin/active-site inhibitor/exo-site inhibitor]]


''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:31:44 2008''
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Revision as of 15:12, 21 February 2008

File:1o0d.jpg


1o0d, resolution 2.44Å

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Human Thrombin complexed with a d-Phe-Pro-Arg-type Inhibitor and a C-terminal Hirudin derived exo-site inhibitor

OverviewOverview

Synthesis of thrombin inhibitors and their binding mode to thrombin is described. Modification of the P1 moiety leads to an increased selectivity versus trypsin. The observed selectivity is discussed in view of their thrombin-inhibitor complex X-ray structures.

DiseaseDisease

Known diseases associated with this structure: Dysprothrombinemia OMIM:[176930], Hyperprothrombinemia OMIM:[176930], Hypoprothrombinemia OMIM:[176930]

About this StructureAbout this Structure

1O0D is a Protein complex structure of sequences from Homo sapiens with as ligand. Active as Thrombin, with EC number 3.4.21.5 Full crystallographic information is available from OCA.

ReferenceReference

D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety., Lange UE, Baucke D, Hornberger W, Mack H, Seitz W, Hoffken HW, Bioorg Med Chem Lett. 2003 Jun 16;13(12):2029-33. PMID:12781189

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