1z6j: Difference between revisions

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[[Image:1z6j.gif|left|200px]]
{{Seed}}
[[Image:1z6j.png|left|200px]]


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{{STRUCTURE_1z6j|  PDB=1z6j  |  SCENE=  }}  
{{STRUCTURE_1z6j|  PDB=1z6j  |  SCENE=  }}  


'''Crystal Structure of a ternary complex of Factor VIIa/Tissue Factor/Pyrazinone Inhibitor'''
===Crystal Structure of a ternary complex of Factor VIIa/Tissue Factor/Pyrazinone Inhibitor===




==Overview==
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We describe the structure-based design, synthesis, and enzymatic activity of a series of substituted pyrazinones as inhibitors of the TF/VIIa complex. These inhibitors contain substituents meta to the P(1) amidine designed to explore additional interactions with the VIIa residues in the so-called 'S(1) side pocket'. A crystal structure of the designed inhibitors demonstrates the ability of the P(1) side pocket moiety to engage Lys192 and main chain of Gly216 via hydrogen bond interactions, thus, providing additional possibility for chemical modification to improve selectivity and/or physical properties of inhibitors.
The line below this paragraph, {{ABSTRACT_PUBMED_15913999}}, adds the Publication Abstract to the page
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{{ABSTRACT_PUBMED_15913999}}


==Disease==
==Disease==
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==Reference==
==Reference==
Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa., Schweitzer BA, Neumann WL, Rahman HK, Kusturin CL, Sample KR, Poda GI, Kurumbail RG, Stevens AM, Stegeman RA, Stallings WC, South MS, Bioorg Med Chem Lett. 2005 Jun 15;15(12):3006-11. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15913999 15913999]
Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa., Schweitzer BA, Neumann WL, Rahman HK, Kusturin CL, Sample KR, Poda GI, Kurumbail RG, Stevens AM, Stegeman RA, Stallings WC, South MS, Bioorg Med Chem Lett. 2005 Jun 15;15(12):3006-11. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15913999 15913999]
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex., South MS, Case BL, Wood RS, Jones DE, Hayes MJ, Girard TJ, Lachance RM, Nicholson NS, Clare M, Stevens AM, Stegeman RA, Stallings WC, Kurumbail RG, Parlow JJ, Bioorg Med Chem Lett. 2003 Jul 21;13(14):2319-25. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12824026 12824026]
Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors., Parlow JJ, Dice TA, Lachance RM, Girard TJ, Stevens AM, Stegeman RA, Stallings WC, Kurumbail RG, South MS, J Med Chem. 2003 Sep 11;46(19):4043-9. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12954057 12954057]
[[Category: Coagulation factor VIIa]]
[[Category: Coagulation factor VIIa]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Thrombosis]]
[[Category: Thrombosis]]
[[Category: Tissue factor]]
[[Category: Tissue factor]]
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