Preferred Label : TRK/RET Inhibitor ND-003;
NCIt definition : An orally bioavailable small molecule inhibitor of multiple kinases, including tropomyosin-related-kinase
(TRK) and rearranged during transfection (RET), with potential antineoplastic activity.
Upon oral administration, TRK/RET inhibitor ND-003 targets and binds to TRK and fusion
proteins containing sequences from neurotrophic tyrosine receptor kinase (NTRK). This
inhibits neurotrophin-TRK interaction and TRK activation, thereby preventing the activation
of downstream signaling pathways, including the PI3K, RAS/MAPK/ERK and PLC-gamma pathways
that are activated by these kinases. This results in both the induction of cellular
apoptosis and the inhibition of cell growth in tumors that overexpress TRK and/or
express NTRK fusion proteins. TRK/RET inhibitor ND-003 also targets and binds to RET,
thereby inhibiting the activity of RET. This results in an inhibition of cell growth
of tumors that exhibit increased RET activity. TRK, a family of receptor tyrosine
kinases (RTKs) activated by neurotrophins, is encoded by NTRK family genes. The expression
of either mutated forms of, or fusion proteins involving NTRK family members results
in uncontrolled TRK signaling, which plays an important role in tumor cell growth,
survival, invasion and treatment resistance. RET overexpression, activating mutations,
and fusions result in the upregulation and/or overactivation of RET tyrosine kinase
activity in various cancer cell types. Dysregulated RET activity plays a key role
in the development and progression of certain cancers.;
Molecule name : ND 003; JND-5932; ND-003; JND 5932;
NCI Metathesaurus CUI : CL1927036;
Origin ID : C204808;
UMLS CUI : C5908066;
Semantic type(s)
- concept_is_in_subset
- has_target
