ROS

The ROS1 gene encodes a receptor protein-tyrosine kinase that consists of 2347 amino acid residues making it the largest member of this enzyme-receptor family. The ROS1 fusion partners include CD74, CCKC6, EZR, FIG, KDELR2, LRIG3, MSN, SDC4, SLC34A2, TMEM106B, TMP, and TPD-52L1. Physiological ROS1 is closely related to the ALK, LTK, and insulin receptor protein-tyrosine kinases[1]. Moreover, several of the ROS1 fusion proteins are implicated in the pathogenesis of a very small proportion of other cancers including glioblastoma, angiosarcoma, and cholangiocarcinoma as well as ovarian, gastric, and colorectal carcinomas. The occurrence of oncogenic ROS1 fusion proteins, particularly in non-small cell lung cancer, has fostered considerable interest in the development of ROS1 inhibitors[2].


[1] R Roskoski Jr. ROS1 protein-tyrosine kinase inhibitors in the treatment of ROS1 fusion protein-driven non-small cell lung cancers. Pharmacol Res. 2017 Jul;121:202-212.
[2] DB Costa et al. Clinical Experience With Crizotinib in Patients With Advanced ALK-Rearranged Non-Small-Cell Lung Cancer and Brain Metastases. J Clin Oncol. 2015 Jun 10;33(17):1881-8.

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Axon ID Name Description From price
2978 Brigatinib Potent, selective, and orally active anaplastic lymphoma kinase (ALK) inhibitor €80.00
2553 LY 2801653 Orally bioavailable multi-kinase inhibitor with potent activity against c-MET €120.00
2600 PF 06463922 Potent, orally available and brain-penetrant ALK/ROS1 selective inhibitor €105.00

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