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ROS1 inhibitors

Tuesday 1 November 2016

ROS1 inhibition; ROS1 Kinase Inhibitors

ROS1 is a pivotal transmembrane receptor protein tyrosine kinase which regulates several cellular processes like apoptosis, survival, differentiation, proliferation, cell migration, and transformation.

There is increasing evidence supporting that ROS1 plays an important role in different malignancies including glioblastoma, colorectal cancer, gastric adenocarcinoma, inflammatory myofibroblastic tumor, ovarian cancer, angiosarcoma, and non small cell lung cancer.

ROS1 has become a potential drug discovery target. ROS1 shares about 49% sequence homology with ALK primary structure; therefore, wide range of ALK kinase inhibitors have shown in vitro inhibitory activity against ROS1 kinase.

After crizotinib approval by FDA for the management of ALK-rearranged lung cancer, ROS1-positive tumors have been focused.

Paywall references

- ROS1 Kinase Inhibitors for Molecular-Targeted Therapies.
Al-Sanea MM, Abdelazem AZ, Park BS, Yoo KH, Sim T, Kwon YJ, Lee SH.
Curr Med Chem. 2016;23(2):142-60. Review.
PMID: 26438251