2b7d: Difference between revisions
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New page: left|200px<br /> <applet load="2b7d" size="450" color="white" frame="true" align="right" spinBox="true" caption="2b7d, resolution 2.24Å" /> '''Factor VIIa Inhibit... |
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[[Image:2b7d.gif|left|200px]]<br /> | [[Image:2b7d.gif|left|200px]]<br /><applet load="2b7d" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2b7d" size=" | |||
caption="2b7d, resolution 2.24Å" /> | caption="2b7d, resolution 2.24Å" /> | ||
'''Factor VIIa Inhibitors: Chemical Optimization, Preclinical Pharmacokinetics, Pharmacodynamics, and Efficacy in a Baboon Thrombosis Model'''<br /> | '''Factor VIIa Inhibitors: Chemical Optimization, Preclinical Pharmacokinetics, Pharmacodynamics, and Efficacy in a Baboon Thrombosis Model'''<br /> | ||
==Overview== | ==Overview== | ||
Highly selective and potent factor VIIa-tissue factor (fVIIa.TF) complex | Highly selective and potent factor VIIa-tissue factor (fVIIa.TF) complex inhibitors were generated through structure-based design. The pharmacokinetic properties of an optimized analog (9) were characterized in several preclinical species, demonstrating pharmacokinetic characteristics suitable for once-a-day dosing in humans. Analog 9 inhibited platelet and fibrin deposition in a dose-dependent manner after intravenous administration in a baboon thrombosis model, and a pharmacodynamic concentration-response model was developed to describe the platelet deposition data. Results for heparin and enoxaparin (Lovenox) in the baboon model are also presented. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
2B7D 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 C1B 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:// | 2B7D 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=C1B:'>C1B</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=2B7D OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Elrod, K | [[Category: Elrod, K C.]] | ||
[[Category: Green, M | [[Category: Green, M J.]] | ||
[[Category: Hanson, S | [[Category: Hanson, S R.]] | ||
[[Category: Hu, H.]] | [[Category: Hu, H.]] | ||
[[Category: Janc, J | [[Category: Janc, J W.]] | ||
[[Category: Katz, B | [[Category: Katz, B A.]] | ||
[[Category: Kolesnikov, A.]] | [[Category: Kolesnikov, A.]] | ||
[[Category: Leahy, E | [[Category: Leahy, E M.]] | ||
[[Category: Liu, L.]] | [[Category: Liu, L.]] | ||
[[Category: Marzec, U | [[Category: Marzec, U M.]] | ||
[[Category: Mordenti, J.]] | [[Category: Mordenti, J.]] | ||
[[Category: Rai, R.]] | [[Category: Rai, R.]] | ||
[[Category: Shrader, W | [[Category: Shrader, W D.]] | ||
[[Category: Sprengeler, P | [[Category: Sprengeler, P A.]] | ||
[[Category: Torkelson, S.]] | [[Category: Torkelson, S.]] | ||
[[Category: Young, W | [[Category: Young, W B.]] | ||
[[Category: Yu, C.]] | [[Category: Yu, C.]] | ||
[[Category: C1B]] | [[Category: C1B]] | ||
[[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 16:34:53 2008'' | ||
