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Biochemistry. 2010 Sep 21;49(37):7972-4. doi: 10.1021/bi100409w.

The crystal structure of a constitutively active mutant RON kinase suggests an intramolecular autophosphorylation hypothesis.

Author information

1
OSI Pharmaceuticals, Inc., 1 Bioscience Park Drive, Farmingdale, New York 11735, USA. jwang@osip.com

Abstract

A complex of RON(M1254T) with AMP-PNP and Mg(2+) reveals a substratelike positioning of Tyr1238 as well as likely catalysis-competent placement of the AMP-PNP and Mg(2+) components and indicates a tendency for cis phosphorylation. The structure shows how the oncogenic mutation may cause the constitutive activation and suggests a mechanistic hypothesis for the autophosphorylation of receptor tyrosine kinases.

PMID:
20726546
DOI:
10.1021/bi100409w
[Indexed for MEDLINE]

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