Al-Sanea, M. M. Abdelazem, A. Z. Park, B. S. Yoo, K. H. Sim, T. Kwon, Y. J. Lee, S. H. 2024-01-20T05:02:55Z 2024-01-20T05:02:55Z 2021-09-03 2016-02 0929-8673 https://pubs.kist.re.kr/handle/201004/124480 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; thus, 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. Although significant advancements have been achieved in understanding ROS1 function and its signaling pathways plus recent discovery of small molecules modulating ROS1 protein, a vital need of medicinal chemistry efforts is still required to produce selective and potent ROS1 inhibitors as an important therapeutic strategy for different human malignancies. This review focuses on the current knowledge about different scaffolds targeting ROS1 rearrangements, methods to synthesis, and some biological data about the most potent compounds that have delivered various scaffold structures. English BENTHAM SCIENCE PUBL LTD ANAPLASTIC LYMPHOMA KINASE CELL LUNG-CANCER PROTEIN-TYROSINE-PHOSPHATASE C-ROS BIOLOGICAL EVALUATION THERAPEUTIC TARGET RECEPTOR ALK POTENT GLIOBLASTOMA ROS1 Kinase Inhibitors for Molecular-Targeted Therapies Article 10.2174/0929867322666151006093623 1 CURRENT MEDICINAL CHEMISTRY, v.23, no.2, pp.142 - 160 CURRENT MEDICINAL CHEMISTRY 23 2 142 160 scie scopus 000372330600004 2-s2.0-84958238291 Biochemistry & Molecular Biology Chemistry, Medicinal Pharmacology & Pharmacy Biochemistry & Molecular Biology Pharmacology & Pharmacy Article ANAPLASTIC LYMPHOMA KINASE CELL LUNG-CANCER PROTEIN-TYROSINE-PHOSPHATASE C-ROS BIOLOGICAL EVALUATION THERAPEUTIC TARGET RECEPTOR ALK POTENT GLIOBLASTOMA ROS1 kinase receptor tyrosine kinase cancer inhibitor translocation