1z71

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[[Image:1z71.gif|left|200px]]
[[Image:1z71.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1z71 |SIZE=350|CAPTION= <scene name='initialview01'>1z71</scene>, resolution 1.80&Aring;
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The line below this paragraph, containing "STRUCTURE_1z71", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=L17:L17'>L17</scene>, <scene name='pdbligand=TYS:SULFONATED+TYROSINE'>TYS</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Thrombin Thrombin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1z71| PDB=1z71 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1z71 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1z71 OCA], [http://www.ebi.ac.uk/pdbsum/1z71 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1z71 RCSB]</span>
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}}
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'''thrombin and P2 pyridine N-oxide inhibitor complex structure'''
'''thrombin and P2 pyridine N-oxide inhibitor complex structure'''
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[[Category: Wong, B.]]
[[Category: Wong, B.]]
[[Category: Yan, Y.]]
[[Category: Yan, Y.]]
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[[Category: thrombin inhibitor complex]]
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[[Category: Thrombin inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 17:15:27 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:30:24 2008''
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Revision as of 14:15, 3 May 2008

Image:1z71.gif

Template:STRUCTURE 1z71

thrombin and P2 pyridine N-oxide inhibitor complex structure


Overview

In this study, we have demonstrated that the critical hydrogen bonding motif of the established 3-aminopyrazinone thrombin inhibitors can be effectively mimicked by a 2-aminopyridine N-oxide. As this peptidomimetic core is more resistant toward oxidative metabolism, it also overcomes the metabolic liability associated with the pyrazinones. An optimization study of the P(1) benzylamide delivered the potent thrombin inhibitor 21 (K(i) = 3.2 nM, 2xaPTT = 360 nM), which exhibited good plasma levels and half-life after oral dosing in the dog (C(max) = 2.6 microM, t(1/2) = 4.5 h).

About this Structure

1Z71 is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold., Nantermet PG, Burgey CS, Robinson KA, Pellicore JM, Newton CL, Deng JZ, Selnick HG, Lewis SD, Lucas BJ, Krueger JA, Miller-Stein C, White RB, Wong B, McMasters DR, Wallace AA, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP, Lyle TA, Bioorg Med Chem Lett. 2005 Jun 2;15(11):2771-5. PMID:15911253 Page seeded by OCA on Sat May 3 17:15:27 2008

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