Preferred Label : GPR35 Inhibitor CT3001;
NCIt synonyms : G-protein Coupled Receptor 35 Inhibitor CT3001; GPR-35 Inhibitor CT3001;
NCIt definition : An orally bioavailable inhibitor of G-protein coupled receptor 35 (GPR35) and formulated
with polyethylene glycol 400 (PEG400), with potential antineoplastic activity. Upon
oral administration, GPR35 inhibitor CT3001 targets, binds to and inhibits the activity
of GPR35. As GPR35 promotes the activity of the transcription coactivators yes-associated
protein 1 (YAP) and transcriptional coactivator with PDZ-binding motif (TAZ), the
inhibition of GPR35 decreases YAP/TAZ activity and prevents the interaction between
YAP/TAZ and the transcription factor TEAD (TEA domain). This may inhibit YAP/TAZ-TEAD
promoted gene transcription involved in tumor cell proliferation, angiogenesis and
survival, and may inhibit tumor cell proliferation. In addition, CT3001 may abrogate
YAP/TAZ-mediated immunosuppression in the tumor microenvironment (TME) and may suppress
regulatory T-cells (Tregs) and increase cytotoxic T-lymphocyte (CTL) tumor infiltration.
This may promote an anti-tumor immune response. GPR35, an oncogenic protein and member
of the G protein-coupled receptor family, is overexpressed in a variety of tumors.
It promotes tumor immune escape and mediates YAP/TAZ oncogenic activation. Pegylation
increases the half-life of this agent.;
Molecule name : CT-3001; CT 3001;
Origin ID : C210701;
concept_is_in_subset
- has_target
