1wv7
From Proteopedia
(New page: 200px<br /> <applet load="1wv7" size="450" color="white" frame="true" align="right" spinBox="true" caption="1wv7, resolution 2.70Å" /> '''Human Factor Viia-T...) |
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| - | [[Image:1wv7.gif|left|200px]]<br /> | + | [[Image:1wv7.gif|left|200px]]<br /><applet load="1wv7" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1wv7" size=" | + | |
caption="1wv7, resolution 2.70Å" /> | caption="1wv7, resolution 2.70Å" /> | ||
'''Human Factor Viia-Tissue Factor Complexed with ethylsulfonamide-D-5-propoxy-Trp-Gln-p-aminobenzamidine'''<br /> | '''Human Factor Viia-Tissue Factor Complexed with ethylsulfonamide-D-5-propoxy-Trp-Gln-p-aminobenzamidine'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Selective factor VIIa-tissue factor complex (FVIIa/TF) inhibition is seen | + | Selective factor VIIa-tissue factor complex (FVIIa/TF) inhibition is seen as a promising target for developing new anticoagulant drugs. Structure-based designs of the P3 moiety in the peptide mimetic factor VIIa inhibitor successfully lead to novel inhibitors with selectivity for FVIIa/TF and extrinsic coagulation the same as or even higher than those of previously reported peptide mimetic factor VIIa inhibitors. X-ray crystal structure analysis reveals that one of the novel inhibitors shows improved selectivity by forming interactions between the inhibitor and FVIIa as expected. Another of the novel inhibitors achieves improved selectivity through an unexpected hydrogen bond with Gln217, with a unique bent conformation in FVIIa/TF accompanied by conformational changes of the inhibitor and the protein. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1WV7 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with BGC, FUC, CA and 5PI as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Coagulation_factor_VIIa Coagulation factor VIIa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.21 3.4.21.21] Full crystallographic information is available from [http:// | + | 1WV7 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=BGC:'>BGC</scene>, <scene name='pdbligand=FUC:'>FUC</scene>, <scene name='pdbligand=CA:'>CA</scene> and <scene name='pdbligand=5PI:'>5PI</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Coagulation_factor_VIIa Coagulation factor VIIa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.21 3.4.21.21] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WV7 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: serine protease]] | [[Category: serine protease]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:48:24 2008'' |
Revision as of 13:48, 21 February 2008
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Human Factor Viia-Tissue Factor Complexed with ethylsulfonamide-D-5-propoxy-Trp-Gln-p-aminobenzamidine
Contents |
Overview
Selective factor VIIa-tissue factor complex (FVIIa/TF) inhibition is seen as a promising target for developing new anticoagulant drugs. Structure-based designs of the P3 moiety in the peptide mimetic factor VIIa inhibitor successfully lead to novel inhibitors with selectivity for FVIIa/TF and extrinsic coagulation the same as or even higher than those of previously reported peptide mimetic factor VIIa inhibitors. X-ray crystal structure analysis reveals that one of the novel inhibitors shows improved selectivity by forming interactions between the inhibitor and FVIIa as expected. Another of the novel inhibitors achieves improved selectivity through an unexpected hydrogen bond with Gln217, with a unique bent conformation in FVIIa/TF accompanied by conformational changes of the inhibitor and the protein.
Disease
Known diseases associated with this structure: Esophageal squamous cell carcinoma OMIM:[606551], Factor VII deficiency OMIM:[227500], Myocardial infarction, decreased susceptibility to OMIM:[227500]
About this Structure
1WV7 is a Protein complex structure of sequences from Homo sapiens with , , and as ligands. Active as Coagulation factor VIIa, with EC number 3.4.21.21 Full crystallographic information is available from OCA.
Reference
Structure-based design of P3 moieties in the peptide mimetic factor VIIa inhibitor., Kadono S, Sakamoto A, Kikuchi Y, Oh-eda M, Yabuta N, Yoshihashi K, Kitazawa T, Suzuki T, Koga T, Hattori K, Shiraishi T, Haramura M, Kodama H, Ono Y, Esaki T, Sato H, Watanabe Y, Itoh S, Ohta M, Kozono T, Biochem Biophys Res Commun. 2005 Feb 11;327(2):589-96. PMID:15629154
Page seeded by OCA on Thu Feb 21 15:48:24 2008
Categories: Coagulation factor VIIa | Homo sapiens | Protein complex | Esaki, T. | Haramura, M. | Hattori, K. | Itoh, S. | Kadono, S. | Kikuchi, Y. | Kitazawa, T. | Kodama, H. | Koga, T. | Kozono, T. | Oh-eda, M. | Ohta, M. | Ono, Y. | Sakamoto, A. | Sato, H. | Shiraishi, T. | Suzuki, T. | Watanabe, Y. | Yabuta, N. | Yoshihashi, K. | 5PI | BGC | CA | FUC | Serine protease
