Article
Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity.
Nature structural biology - 1 Sept 2003
Fitzgerald Catherine E, Patel Sangita B, Becker Joseph W, Cameron Patricia M, Zaller Dennis, Pikounis Vasilis Bill, O'Keefe Stephen J, Scapin Giovanna
Abstract excerpt
The quinazolinone and pyridol-pyrimidine classes of p38 MAP kinase inhibitors have a previously unseen degree of specificity for p38 over other MAP kinases. Comparison of the crystal structures of p38 bound to four different compounds shows that binding of the more specific molecules is characterized by a peptide flip between Met109 and Gly110. Gly110 is a residue specific to the alpha, beta and gamma isoforms of...
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