ROS1 Kinase Inhibitors for Molecular-Targeted Therapies

Title
ROS1 Kinase Inhibitors for Molecular-Targeted Therapies
Authors
알사니어아메드박병선유경호심태보권영직이소하
Keywords
ROS1; Kinase; REceptor tyrosine kinase; translocation
Issue Date
2016-02
Publisher
Current medicinal chemistry
Citation
VOL 23, NO 23, 142-160
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/58566
ISSN
09298673
Appears in Collections:
KIST Publication > Article
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