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Ref Type Journal Article
PMID (23957426)
Authors Liu W, Yu B, Xu G, Xu WR, Loh ML, Tang LD, Qu CK
Title Identification of cryptotanshinone as an inhibitor of oncogenic protein tyrosine phosphatase SHP2 (PTPN11).
Journal Vol Issue Date Pages Journal Short Title
Journal of medicinal chemistry 56 18 2013 Sep 26 7212-21 J Med Chem
URL
Abstract Text 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. Enzymatic kinetic analyses showed that cryptotanshinone was a mixed-type and irreversible inhibitor. This drug was further verified for its ability to block SHP2-mediated cell signaling and cellular functions. Furthermore, mouse myeloid progenitors and patient leukemic cells with the activating mutation E76K in PTPN11 were found to be sensitive to this inhibitor. Since cryptotanshinone is used to treat cardiovascular diseases in Asian countries, this drug has a potential to be used directly or to be further developed to treat PTPN11-associated malignancies.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Cryptotanshinone Cryptotanshinone 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
Cryptotanshinone SHP2 Inhibitor 20 Cryptotanshinone is an inhibitor of Shp2, which may result in cell growth inhibition and apoptosis (PMID: 23957426, PMID: 32612672).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References