Preferred Label : SHP2 Inhibitor RLY-1971;
NCIt definition : An orally bioavailable 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 RLY-1971 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 : RLY 1971; RLY-1971; GDC 1971; GDC-1971;
NCI Metathesaurus CUI : CL1406779;
Origin ID : C172988;
UMLS CUI : C5417952;
Semantic type(s)
- concept_is_in_subset
- has_target
