2qd9

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[[Image:2qd9.jpg|left|200px]]
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{{STRUCTURE_2qd9| PDB=2qd9 | SCENE= }}
{{STRUCTURE_2qd9| PDB=2qd9 | SCENE= }}
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'''P38 Alpha Map Kinase inhibitor based on heterobicyclic scaffolds'''
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===P38 Alpha Map Kinase inhibitor based on heterobicyclic scaffolds===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 17664068 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17664068}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:45:56 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 02:21:08 2008''

Revision as of 23:21, 28 July 2008

Template:STRUCTURE 2qd9

P38 Alpha Map Kinase inhibitor based on heterobicyclic scaffolds

Template:ABSTRACT PUBMED 17664068

About this Structure

2QD9 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

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 Sep 15;17(18):5019-24. Epub 2007 Jul 21. PMID:17664068

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