1hv7
From Proteopedia
(New page: 200px<br /><applet load="1hv7" size="450" color="white" frame="true" align="right" spinBox="true" caption="1hv7, resolution 1.7Å" /> '''PORCINE PANCREATIC EL...) |
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- | [[Image:1hv7.jpg|left|200px]]<br /><applet load="1hv7" size=" | + | [[Image:1hv7.jpg|left|200px]]<br /><applet load="1hv7" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1hv7, resolution 1.7Å" /> | caption="1hv7, resolution 1.7Å" /> | ||
'''PORCINE PANCREATIC ELASTASE COMPLEXED WITH GW311616A'''<br /> | '''PORCINE PANCREATIC ELASTASE COMPLEXED WITH GW311616A'''<br /> | ||
==Overview== | ==Overview== | ||
- | The discovery of a potent intracellular inhibitor of human neutrophil | + | The discovery of a potent intracellular inhibitor of human neutrophil elastase which is orally active and has a long duration of action is described. The pharmacodynamic and pharmacokinetic properties of a trans-lactam development candidate, GW311616A, are described. |
==About this Structure== | ==About this Structure== | ||
- | 1HV7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Sus_scrofa Sus scrofa] with SO4 and 616 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Pancreatic_elastase Pancreatic elastase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.36 3.4.21.36] Full crystallographic information is available from [http:// | + | 1HV7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Sus_scrofa Sus scrofa] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=616:'>616</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Pancreatic_elastase Pancreatic elastase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.36 3.4.21.36] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1HV7 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Sus scrofa]] | [[Category: Sus scrofa]] | ||
- | [[Category: Singh, O | + | [[Category: Singh, O M.]] |
[[Category: Skarzynski, T.]] | [[Category: Skarzynski, T.]] | ||
[[Category: 616]] | [[Category: 616]] | ||
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[[Category: serine protease-inhibitor complex]] | [[Category: serine protease-inhibitor complex]] | ||
- | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:05:09 2008'' |
Revision as of 11:05, 21 February 2008
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PORCINE PANCREATIC ELASTASE COMPLEXED WITH GW311616A
Overview
The discovery of a potent intracellular inhibitor of human neutrophil elastase which is orally active and has a long duration of action is described. The pharmacodynamic and pharmacokinetic properties of a trans-lactam development candidate, GW311616A, are described.
About this Structure
1HV7 is a Single protein structure of sequence from Sus scrofa with and as ligands. Active as Pancreatic elastase, with EC number 3.4.21.36 Full crystallographic information is available from OCA.
Reference
The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate., Macdonald SJ, Dowle MD, Harrison LA, Shah P, Johnson MR, Inglis GG, Clarke GD, Smith RA, Humphreys D, Molloy CR, Amour A, Dixon M, Murkitt G, Godward RE, Padfield T, Skarzynski T, Singh OM, Kumar KA, Fleetwood G, Hodgson ST, Hardy GW, Finch H, Bioorg Med Chem Lett. 2001 Apr 9;11(7):895-8. PMID:11294386
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