Trk receptor
Trk receptors are a family of tyrosine kinases that regulates synaptic strength and plasticity in the mammalian nervous system. Trk receptors affect neuronal survival and differentiation through several signal cascades. However, the activation of these receptors also has significant effects on functional properties of neurons. The three most common types of trk receptors are trkA, trkB, and trkC. Each of these receptor types has different binding affinity to certain types of neurotrophins. The differences in the signaling initiated by these distinct types of receptors are important for generating diverse biological responses. The activation of Trk receptors by neurotrophin binding may lead to activation of signal cascades resulting in promoting survival and other functional regulation of cells.
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GW 441756是特异的高活性原肌球蛋白相关激酶A(TrkA)抑制剂,IC50为2 nM,对c-Raf1和CDK2几乎无活性。
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GNF-5837是一个Trk抑制剂,对表达融合蛋白Tel-TrkC,Tel-TrkB和Tel-TrkA的细胞IC50分别为7,9和11 nM。
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ANA-12是TrkB高效选择性抑制剂,在小鼠模型中有抗焦虑抑郁活性。
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