Progress on Allosteric Inhibitors Targeting SHP2 and PROTAC Drugs
The protein tyrosine phosphatase containing Src homology 2(SH2)domain(SHP2)is the first oncogenic protein confirmed belong to the protein tyrosine phosphatase(PTP)family.It has the potential to regulate multiple signaling pathways,including RAS-RAF-ERK,PI3K-AKT,and JAK-STAT,making it an important target for anti-tumor drug discovery.SHP2 also plays a critical role in promoting tumor cell resistance and modulating immune cell function in the tumor microenvironment.The discovery of allosteric inhibitors has advanced the development of SHP2 drugs,with several allosteric inhibitor drugs currently in clinical trials as monotherapy or combination therapy.At the same time,proteolysis targeting chimeras(PROTACs),a novel drug design approach,are being widely used in the development of SHP2-targeting drugs.This article summarizes the clinical research results of allosteric inhibitors targeting SHP2,and outlines the progress of PROTAC-SHP2 drug development,with the aim of providing inspiration for the design and improvement of SHP2 drug molecules.
The protein tyrosine phosphatase containingSrc homology 2(SHP2)Domain allosteric inhibitorsProteolysis targeting chimeras
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维普
