2qd9: Difference between revisions

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.

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] Known structural/functional Site: <scene name='pdbsite=AC1:Lgf Binding Site For Residue A 361'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2QD9 OCA].  

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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17664068 17664068]

[[Category: Sack, J.S.]]

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