RET
The RET (“rearranged during transfection”) proto-oncogene encodes a receptor-type tyrosine kinase with an intracellular domain, a transmembrane domain, and an intracellular tyrosine kinase domain. The ligands for RET have been identified as neurotrophic factors of the glial cell-line derived neurotrophic factor (GDNF) family, including GDNF, neurturin, artemin, and persephin. All these factors activate RET via different glycosyl phosphatidylinositol-linked GFRa receptors.[1] The receptor appears to be essential for the normal development of several kinds of nerve cells, including nerves in the intestine (enteric neurons) and the autonomic nervous system. The RET protein is also necessary for normal kidney development and the production of sperm (spermatogenesis).[2] Mutations in the RET gene have been found in a number of human diseases, including several different cancers of neuroendocrine origin and a gut syndrome characterized by intestinal obstruction known as Hirschsprung’s disease[3].
[1] The RET proto-oncogene in human cancers. S.M. Jhiang. Oncogene 2000, 19, 5590-5597.
[2] Signaling by the RET receptor tyrosine kinase and its role in the development of the mammalian enteric nervous system. S. Taraviras, V. Pachnis et al. Development 1999, 126, 2785-2797.
[3] CF Ibáñez et al. Structure and physiology of the RET receptor tyrosine kinase. Cold Spring Harb Perspect Biol. 2013 Feb 1;5(2). pii: a009134.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 3854 | BLU-667 | Highly potent and selective next generation inhibitor of oncogenic RET fusion and activating mutation | €130.00 | |
| 3226 | RET agonist Q525 | Highly selective RET agonist | €120.00 | |
| 2667 | RET Inhibitor 2667 | Potent RTK inhibitor with activity against wild-type RET and its mutants | €125.00 | |
| 3195 | Selpercatinib | Potent, highly selective, and ATP-competitive RET inhibitor | €110.00 | |