Article
Phosphorylation of SHP2 at Tyr62 Enables Acquired Resistance to SHP2 Allosteric Inhibitors in FLT3-ITD-Driven AML.
Cancer research - 6 Jun 2022
Pfeiffer Anamarija, Franciosa Giulia, Locard-Paulet Marie, Piga Ilaria, Reckzeh Kristian, Vemulapalli Vidyasiri, Blacklow Stephen C, Theilgaard-Mönch Kim, Jensen Lars J, Olsen Jesper V
Abstract excerpt
The protein tyrosine phosphatase SHP2 is crucial for oncogenic transformation of acute myeloid leukemia (AML) cells expressing mutated receptor tyrosine kinases. SHP2 is required for full RAS-ERK activation to promote cell proliferation and survival programs. Allosteric SHP2 inhibitors act by stabilizing SHP2 in its autoinhibited conformation and are currently being tested in clinical trials for tumors with...
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