1zom: Difference between revisions

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{{STRUCTURE_1zom|  PDB=1zom  |  SCENE=  }}  
{{STRUCTURE_1zom|  PDB=1zom  |  SCENE=  }}  


'''Crystal Structure of the Catalytic Domain of Coagulation Factor XI in complex with a peptidomimetic Inhibitor'''
===Crystal Structure of the Catalytic Domain of Coagulation Factor XI in complex with a peptidomimetic Inhibitor===




==Overview==
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Human coagulation factor XIa (FXIa), a serine protease activated by site-specific cleavage of factor XI by thrombin, FXIIa, or autoactivation, is a critical enzyme in the amplification phase of the coagulation cascade. To investigate the potential of FXIa inhibitors as safe anticoagulants, a series of potent, selective peptidomimetic inhibitors of FXIa were designed and synthesized. Some of these inhibitors showed low nanomolar FXIa inhibitory activity with &gt;1000-fold FXa selectivity and &gt;100-fold thrombin selectivity. The X-ray structure of one of these inhibitors, 36, demonstrates its unique binding interactions with FXIa. Compound 32 caused a doubling of the activated partial thromboplastin time in human plasma at 2.4 microM and was efficacious in a rat model of venous thrombosis. These data suggest that factor XIa plays a significant role in venous thrombosis and may be a suitable target for the development of antithrombotic therapy.
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==Disease==
==Disease==
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[[Category: Fxia]]
[[Category: Fxia]]
[[Category: Inhibitor]]
[[Category: Inhibitor]]
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Revision as of 19:24, 27 July 2008

File:1zom.png

Template:STRUCTURE 1zom

Crystal Structure of the Catalytic Domain of Coagulation Factor XI in complex with a peptidomimetic InhibitorCrystal Structure of the Catalytic Domain of Coagulation Factor XI in complex with a peptidomimetic Inhibitor

Template:ABSTRACT PUBMED 17181160

DiseaseDisease

Known disease associated with this structure: Factor XI deficiency, autosomal dominant OMIM:[264900], Factor XI deficiency, autosomal recessive OMIM:[264900]

About this StructureAbout this Structure

1ZOM is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants., Lin J, Deng H, Jin L, Pandey P, Quinn J, Cantin S, Rynkiewicz MJ, Gorga JC, Bibbins F, Celatka CA, Nagafuji P, Bannister TD, Meyers HV, Babine RE, Hayward NJ, Weaver D, Benjamin H, Stassen F, Abdel-Meguid SS, Strickler JE, J Med Chem. 2006 Dec 28;49(26):7781-91. PMID:17181160

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