Preferred Label : TGF-beta Receptor 1 Kinase Inhibitor YL-13027;
NCIt synonyms : TGFbR1 Inhibitor YL-13027;
NCIt definition : An orally bioavailable inhibitor of the serine/threonine kinase transforming growth
factor-beta receptor 1 (TGFbR1; activin receptor-like kinase 5; ALK5), with potential
antineoplastic and immunomodulating activities. Upon administration, TGF-betaR1 inhibitor
YL-13027 specifically targets and binds to TGFbR1, which prevents TGFbR1-mediated
signal transduction. This abrogates TGFbR1-mediated immunosuppression, enhances anti-tumor
immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte
(CTL)-mediated immune response against tumor cells leading to tumor cell death. This
may lead to a reduction in TGFbR1-dependent proliferation of cancer cells. The TGFb
signaling pathway is often deregulated in tumors and plays a key role in the regulation
of cell growth, differentiation, apoptosis, motility, invasion, and angiogenesis.
It plays a key role in immunosuppression in the TME and cancer cell progression.;
Molecule name : YL 13027; YL-13027;
NCI Metathesaurus CUI : CL1406216;
Origin ID : C172107;
UMLS CUI : C5417893;
Semantic type(s)
concept_is_in_subset