Ontology highlight
ABSTRACT:
SUBMITTER: Du G
PROVIDER: S-EPMC7493195 | biostudies-literature | 2020 Feb
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20200130 4
SRC is a major regulator of many signaling pathways and contributes to cancer development. However, development of a selective SRC inhibitor has been challenging, and FDA-approved SRC inhibitors, dasatinib and bosutinib, are multitargeted kinase inhibitors. Here, we describe our efforts to develop a selective SRC covalent inhibitor by targeting cysteine 277 on the P-loop of SRC. Using a promiscuous covalent kinase inhibitor (CKI) <b>SM1-71</b> as a starting point, we developed covalent inhibitor ...[more]