trk受体
原肌球蛋白受体激酶A
神经营养素
原肌球蛋白受体激酶B
可药性
原肌球蛋白受体激酶C
低亲和力神经生长因子受体
受体
基因亚型
生物
细胞生物学
激酶
蛋白激酶结构域
神经科学
化学
生物化学
神经营养因子
血小板源性生长因子受体
生长因子
基因
突变体
出处
期刊:Vitamins and hormones
日期:2017-01-01
卷期号:: 1-18
被引量:5
标识
DOI:10.1016/bs.vh.2016.10.001
摘要
Neurotrophins and their receptors (Trk) play key roles in the development of the nervous system and in cell survival. Trk receptors are therefore attractive pharmacological targets for brain disorders as well as for cancers. While the druggability of the extracellular domain of the receptors, that specifically binds neurotrophins, is yet to be proven, the intracellular kinase domains are attractive targets for small-molecule binding. The recent crystal structures of the three isoforms of the Trk family, TrkA, TrkB, and TrkC have been described in their apo forms and in complex with potent and selective pan-Trk inhibitors. The description of the kinase domain of each of the isoforms will be discussed in their apo forms or bound to potent inhibitors of interest in cancer therapy. Nononcology indications and selectivity issues will also be discussed.
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