RON 激酶组成性激活突变体的晶体结构提示了一种分子内自身磷酸化假说。
The crystal structure of a constitutively active mutant RON kinase suggests an intramolecular autophosphorylation hypothesis.
机构信息
OSI Pharmaceuticals, Inc., 1 Bioscience Park Drive, Farmingdale, New York 11735, USA.
出版信息
Biochemistry. 2010 Sep 21;49(37):7972-4. doi: 10.1021/bi100409w.
PMID:20726546
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.
摘要
RON（M1254T）与 AMP-PNP 和 Mg（2+）复合物的结构揭示了 Tyr1238 的类似底物定位，以及 AMP-PNP 和 Mg（2+）成分的可能催化活性定位，并表明顺式磷酸化的趋势。该结构显示了致癌突变如何导致组成性激活，并为受体酪氨酸激酶的自磷酸化提出了一种机制假设。
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