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3cg2

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{{STRUCTURE_3cg2| PDB=3cg2 | SCENE= }}
{{STRUCTURE_3cg2| PDB=3cg2 | SCENE= }}
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'''P38 Alpha Kinase complexed with a Pyrazolo-Pyrimidine based inhibitor'''
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===P38 Alpha Kinase complexed with a Pyrazolo-Pyrimidine based inhibitor===
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==Overview==
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The synthesis and structure-activity relationships (SAR) of p38alpha MAP kinase inhibitors based on a pyrazolo-pyrimidine scaffold are described. These studies led to the identification of compound 2x as a potent and selective inhibitor of p38alpha MAP kinase with excellent cellular potency toward the inhibition of TNFalpha production. Compound 2x was highly efficacious in vivo in inhibiting TNFalpha production in an acute murine model of TNFalpha production. X-ray co-crystallography of a pyrazolo-pyrimidine analog 2b bound to unphosphorylated p38alpha is also disclosed.
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(as it appears on PubMed at http://www.pubmed.gov), where 18359226 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18359226}}
==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 Mon Jul 28 14:59:06 2008''

Revision as of 11:59, 28 July 2008

Image:3cg2.png

Template:STRUCTURE 3cg2

P38 Alpha Kinase complexed with a Pyrazolo-Pyrimidine based inhibitor

Template:ABSTRACT PUBMED 18359226

About this Structure

3CG2 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Pyrazolo-pyrimidines: A novel heterocyclic scaffold for potent and selective p38alpha inhibitors., Das J, Moquin RV, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K, Bioorg Med Chem Lett. 2008 Mar 10;. PMID:18359226

Page seeded by OCA on Mon Jul 28 14:59:06 2008

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