Trk Receptor
The NTRK1, NTRK2, and NTRK3 genes encode related single-pass transmembrane receptor tyrosine kinases, high affinity nerve growth factor receptor (TRKA), BDNF/NT-3 growth factor receptor (TRKB), and NT-3 growth factor receptor (TRKC), respectively, that function as high-affinity receptors for neurotrophins. TRK receptors contribute to neuronal development, function, survival, and proliferation during the development and into adulthood. Like other receptor tyrosine kinases, TRK proteins are activated following ligand binding to the extracellular domain of the receptor. Ligands for TRK proteins are the neurotrophins, a family of closely-related secreted proteins that were discovered and classified initially as proteins that were able to promote differentiation and survival in both sympathetic and sensory nerves.
Signaling via TRK proteins is achieved with specific neurotrophin ligands, which triggers receptor dimerization and phosphorylation, leading to the activation of downstream signaling cascades. Through binding to TRK receptors, neorotrophinss activate Ras, phosphatidylinositol-3 (PI3)-kinase, and phospholipase C-γ1 signaling pathways. By this signaling, neurotrophins ultimately regulate cell fate decisions, axon growth, dendrite growth, and pruning. In addition to the expression in the central nervous system (CNS), TRK proteins have also been identified in non-neuronal normal tissues and cells, including pancreatic beta cells, monocytes, lungs, and bone.
References
1.Hsiao SJ,et al. J Mol Diagn. 2019;21(4):553–571.
2.Lange AM, et al. Cancers (Basel). 2018;10(4):105.
Signaling via TRK proteins is achieved with specific neurotrophin ligands, which triggers receptor dimerization and phosphorylation, leading to the activation of downstream signaling cascades. Through binding to TRK receptors, neorotrophinss activate Ras, phosphatidylinositol-3 (PI3)-kinase, and phospholipase C-γ1 signaling pathways. By this signaling, neurotrophins ultimately regulate cell fate decisions, axon growth, dendrite growth, and pruning. In addition to the expression in the central nervous system (CNS), TRK proteins have also been identified in non-neuronal normal tissues and cells, including pancreatic beta cells, monocytes, lungs, and bone.
References
1.Hsiao SJ,et al. J Mol Diagn. 2019;21(4):553–571.
2.Lange AM, et al. Cancers (Basel). 2018;10(4):105.
Tyrosine Kinase
Trk Receptor
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ENT-C225
产品货号 : M36522
cas no: 2919962-53-9
ENT-C225 是一种有效的 TrkB 神经营养素受体激活剂。ENT-C225 对激活 TrkB 受体 (TrkBR) 的效力较高,并且具有较好的物理化学特性和神经保护特性。 -
CG 428
产品货号 : M35263
cas no: 2412055-93-5
CG428 是一种有效的、选择性的原肌球蛋白受体激酶 (TRK) 降解剂,具有抗肿瘤活性。CG428 降低 KM12 结直肠癌细胞中原肌球蛋白 3 (TPM3)-TRKA 融合蛋白的水平 (DC50 = 0.36 nM),并抑制下游 PLCγ1 磷酸化 (IC50 = 0.33 nM)。CG428 对 TRKA 的结合亲和力高于 TRKB 和 TRKC(Kd 分别为 1 nM、28 nM 和 4.2 nM)。此外,CG428 能有效抑制 KM12 细胞生长 (IC50 = 2.9 nM)。 -
GNF-8625 monopyridin-N-piperazine hydrochloride
产品货号 : M35176
cas no: 2412055-62-8
GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2) 是TRK 的抑制剂,信息来自专利 WO 2020038415 A1。 -
Cyclotraxin B
产品货号 : M30732
cas no: 1203586-72-4
Antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic properties in mice. -
(3aR)-Selitrectinib
产品货号 : M28716
cas no: 1350884-56-8
(6RS)-LOXO-195 是一种有效的选择性 Trk 酪氨酸激酶抑制剂。