2f9b
From Proteopedia
(New page: 200px<br /> <applet load="2f9b" size="450" color="white" frame="true" align="right" spinBox="true" caption="2f9b, resolution 2.54Å" /> '''Discovery of Novel ...) |
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| - | [[Image:2f9b.gif|left|200px]]<br /> | + | [[Image:2f9b.gif|left|200px]]<br /><applet load="2f9b" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="2f9b, resolution 2.54Å" /> | caption="2f9b, resolution 2.54Å" /> | ||
'''Discovery of Novel Heterocyclic Factor VIIa Inhibitors'''<br /> | '''Discovery of Novel Heterocyclic Factor VIIa Inhibitors'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Structure-activity relationships and binding mode of novel heterocyclic | + | Structure-activity relationships and binding mode of novel heterocyclic factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2-b]pyridine scaffold. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2F9B 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 N1H as [http://en.wikipedia.org/wiki/ligand ligand]. 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:// | + | 2F9B 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=N1H:'>N1H</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=2F9B OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Cabuslay, R.]] | [[Category: Cabuslay, R.]] | ||
[[Category: Hendrix, J.]] | [[Category: Hendrix, J.]] | ||
| - | [[Category: Katz, B | + | [[Category: Katz, B A.]] |
[[Category: Kolesnikov, A.]] | [[Category: Kolesnikov, A.]] | ||
[[Category: Rai, R.]] | [[Category: Rai, R.]] | ||
[[Category: Sanford, E.]] | [[Category: Sanford, E.]] | ||
| - | [[Category: Shrader, W | + | [[Category: Shrader, W D.]] |
| - | [[Category: Sprengeler, P | + | [[Category: Sprengeler, P A.]] |
[[Category: Stephens, R.]] | [[Category: Stephens, R.]] | ||
[[Category: Ton, T.]] | [[Category: Ton, T.]] | ||
[[Category: Torkelson, S.]] | [[Category: Torkelson, S.]] | ||
| - | [[Category: Young, W | + | [[Category: Young, W B.]] |
[[Category: Yu, C.]] | [[Category: Yu, C.]] | ||
[[Category: N1H]] | [[Category: N1H]] | ||
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[[Category: short hydrogen bond]] | [[Category: short hydrogen bond]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:19:02 2008'' |
Revision as of 15:19, 21 February 2008
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Discovery of Novel Heterocyclic Factor VIIa Inhibitors
Contents |
Overview
Structure-activity relationships and binding mode of novel heterocyclic factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2-b]pyridine scaffold.
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
2F9B is a Protein complex structure of sequences from Homo sapiens with as ligand. Active as Coagulation factor VIIa, with EC number 3.4.21.21 Full crystallographic information is available from OCA.
Reference
Discovery of novel heterocyclic factor VIIa inhibitors., Rai R, Kolesnikov A, Sprengeler PA, Torkelson S, Ton T, Katz BA, Yu C, Hendrix J, Shrader WD, Stephens R, Cabuslay R, Sanford E, Young WB, Bioorg Med Chem Lett. 2006 Apr 15;16(8):2270-3. Epub 2006 Feb 3. PMID:16460932
Page seeded by OCA on Thu Feb 21 17:19:02 2008
Categories: Coagulation factor VIIa | Homo sapiens | Protein complex | Cabuslay, R. | Hendrix, J. | Katz, B A. | Kolesnikov, A. | Rai, R. | Sanford, E. | Shrader, W D. | Sprengeler, P A. | Stephens, R. | Ton, T. | Torkelson, S. | Young, W B. | Yu, C. | N1H | Active site-directed inhibitor | Serine protease | Short hydrogen bond
