Preferred Label : SHP2 Inhibitor ET0038;
NCIt definition : An orally bioavailable allosteric inhibitor of protein tyrosine phosphatase (PTP)
non-receptor type 11 (SHP2; Src homology region 2 domain phosphatase; PTPN11), with
potential antineoplastic activity. Upon oral administration, SHP2 inhibitor ET0038
targets, binds to and inhibits the activity of SHP2. This prevents SHP2-mediated signaling,
inhibits MAPK signaling and prevents growth of SHP2-expressing tumor cells. SHP2,
an oncoprotein overexpressed in a variety of cancer cell types, regulates cell survival,
differentiation and proliferation through activation of the Ras-Raf-MEK-ERK signaling
pathway. The Ras-MAPK pathway is often hyperactivated in cancer cells due to specific
mutations and rearrangements, and are dependent on SHP2 for their oncogenic signaling.
SHP2 also regulates programmed cell death 1 (PD-1)-mediated signal transduction and
is involved in immune checkpoint modulation.;
Molecule name : ET-0038; ET 0038;
NCI Metathesaurus CUI : CL1905577;
Origin ID : C192173;
UMLS CUI : C5784959;
Semantic type(s)
- concept_is_in_subset
- has_target
