2qd9: Difference between revisions
New page: left|200px<br /> <applet load="2qd9" size="450" color="white" frame="true" align="right" spinBox="true" caption="2qd9, resolution 1.70Å" /> '''P38 Alpha Map Kinas... |
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[[Image:2qd9. | [[Image:2qd9.jpg|left|200px]]<br /><applet load="2qd9" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="2qd9, resolution 1.70Å" /> | caption="2qd9, resolution 1.70Å" /> | ||
'''P38 Alpha Map Kinase inhibitor based on heterobicyclic scaffolds'''<br /> | '''P38 Alpha Map Kinase inhibitor based on heterobicyclic scaffolds'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
2QD9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with LGF as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24] Full crystallographic information is available from [http:// | 2QD9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=LGF:'>LGF</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2QD9 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:03:25 2008'' | ||
Revision as of 15:03, 23 January 2008
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P38 Alpha Map Kinase inhibitor based on heterobicyclic scaffolds
OverviewOverview
The synthesis and structure-activity relationships (SAR) of p38alpha MAP, kinase inhibitors based on heterobicyclic scaffolds are described. This, effort led to the identification of compound (21) as a potent inhibitor of, p38alpha MAP kinase with good cellular potency toward the inhibition of, TNF-alpha production. X-ray co-crystallography of an oxalamide analog (24), bound to unphosphorylated p38alpha is also disclosed.
About this StructureAbout this Structure
2QD9 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Mitogen-activated protein kinase, with EC number 2.7.11.24 Full crystallographic information is available from OCA.
ReferenceReference
Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds., Murali Dhar TG, Wrobleski ST, Lin S, Furch JA, Nirschl DS, Fan Y, Todderud G, Pitt S, Doweyko AM, Sack JS, Mathur A, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K, Bioorg Med Chem Lett. 2007 Jul 21;. PMID:17664068
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