Ontology highlight
ABSTRACT:
SUBMITTER: Liu W
PROVIDER: S-EPMC4159095 | biostudies-literature | 2013 Sep
REPOSITORIES: biostudies-literature
Liu Wei W Yu Bing B Xu Gang G Xu Wei-Ren WR Loh Mignon L ML Tang Li-Da LD Qu Cheng-Kui CK
Journal of medicinal chemistry 20130904 18
Activating mutations of PTPN11 (encoding the SHP2 phosphatase) are associated with Noonan syndrome, childhood leukemias, and sporadic solid tumors. Virtual screening combined with experimental assays was performed to identify inhibitors of SHP2 from a database of natural products. This effort led to the identification of cryptotanshinone as an inhibitor of SHP2. Cryptotanshinone inhibited SHP2 with an IC50 of 22.50 μM. Fluorescence titration experiments confirmed that it directly bound to SHP2. ...[more]