Tropomyosin-related kinases (Trks) are receptor tyrosine kinases (RTK class VII, Trk receptor family) normally expressed in neuronal tissue where they play important role in both development and function of the nervous system[1]. The Trk receptor family is composed of three members (A, B, and C) activated by specific ligands called neurotrophins (NTs). Activations upon ligand binding triggers oligomerization of the receptors, phosphorylation of specific tyrosine residues in the kinase domain, and downstream signal transduction pathways, including survival, proliferation, and differentiation in normal and neoplastic neuronal cells. Deregulation of TrkA and TrkB and their cognate ligands has been described in numerous types of cancers including prostate, breast, colorectal, ovarian, lung, pancreas, melanoma, thyroid, and neuroblastoma and occurs mainly through wild type receptor overexpression, activation, amplification, and/or mutation. Importantly, increased Trks activation in tumor tissues correlates with an aggressive phenotype and poor clinical outcome[2].

[1] Trk receptors: mediators of neurotrophin action. A. Patapoutian, L. F. Reichardt. Curr. Opin. Neurobiol. 2001, 11, 272-280.
[2] Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors. Stéphane L. Raeppel, Frédéric Gaudette, Hannah Nguyen, et al. Int. J. Med. Chem. 2012, Article ID 412614.

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Axon ID Name Description From price
1610 AZ 23 TrkA and TrkB inhibitor €80.00
2248 GNF 5837 Potent, selective, and orally bioavailable tropomyosin receptor kinase (Trk) inhibitor €90.00
1251 GW 441756 TrkA inhibitor €75.00
3407 LOXO-101 sulfate First-in-class, potent, highly selective and ATP-competitive TRK inhibitor  Recently added €80.00

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