trk受体
原肌球蛋白受体激酶A
原肌球蛋白受体激酶B
神经营养素
低亲和力神经生长因子受体
原肌球蛋白受体激酶C
激酶
蛋白激酶结构域
生物
细胞生物学
化学
受体
神经营养因子
癌症研究
生物化学
基因
血小板源性生长因子受体
突变体
生长因子
作者
Thomas Bertrand,M. Kothe,J. Liu,A. Dupuy,Alexey Rak,Pierre‐François Berne,Samuel Davis,Tatiana Gladysheva,C. Valtre,J.Y. Crenne,Magali Mathieu
标识
DOI:10.1016/j.jmb.2012.08.002
摘要
The Trk family of neurotrophin receptors, which includes the three highly homologous proteins TrkA, TrkB and TrkC, is strongly associated with central and peripheral nervous system processes. Trk proteins are also of interest in oncology, since Trk activation has been observed in several cancer types. While Trk kinases are attractive oncology targets, selectivity might be more of an issue than for other kinases due to potential CNS side effects if several Trk kinases are simultaneously targeted. In order to address this issue, we present here the first structures of human TrkA and TrkB kinase domains and three complexes between TrkB and Trk inhibitors. These structures reveal different conformations of the kinase domain and suggest new regions of selectivity among the Trk family.
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