Preferred Label : EP4 Receptor Antagonist YY001;
NCIt synonyms : PGE2 Receptor Antagonist YY001; Prostaglandin E2 Receptor Antagonist YY001; EP4 Antagonist YY001;
NCIt definition : An orally bioavailable small molecule antagonist of the prostaglandin E2 receptor
EP4 subtype (PTGER4; EP4), with potential immunomodulating and antineoplastic activities.
Upon oral administration, EP4 receptor antagonist YY001 selectively targets and binds
to EP4, inhibiting the binding of the immunosuppressive prostaglandin E2 (PGE2) to
EP4. This prevents the activation of EP4 and inhibits PGE2-EP4-mediated signaling.
This inhibits PGE2-driven immune suppression by preventing the PGE2-mediated inhibition
of anti-tumor immune effector cells in the tumor microenvironment (TME), such as natural
killer (NK) cells, T-lymphocytes, dendritic cells (DCs) and M1 macrophages, and blocking
the PGE2-mediated increase in suppressive immune cells, such as myeloid derived suppressor
cells (MDSCs), M2 macrophages, and regulatory T cells (Tregs). This activates an anti-tumor
immune response and inhibits the proliferation of tumor cells in which the PGE2-EP4
signaling pathway is over-activated. EP4, a G protein-coupled receptor (GPCR) overexpressed
in certain types of cancers, promotes tumor cell proliferation and invasion.;
Molecule name : YY-001; YY 001;
Origin ID : C207269;
concept_is_in_subset
- has_target
