Preferred Label : TGF-beta Receptor 1 Kinase Inhibitor SH3051;
NCIt synonyms : TGFbR1 Inhibitor SH3051;
NCIt definition : An orally bioavailable, small molecule inhibitor of the serine/threonine kinase transforming
growth factor-beta (TGF-beta) receptor 1 (TGFbR1; activin receptor-like kinase 5;
ALK5), with potential antineoplastic and immunomodulating activities. Upon administration,
TGFbR1 inhibitor SH3051 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 tumor cells. The TGF-beta
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 : SH 3051; SH-3051;
NCI Metathesaurus CUI : CL1407202;
Origin ID : C173370;
UMLS CUI : C5417964;
Semantic type(s)
- concept_is_in_subset
