Preferred Label : EP4 Antagonist DT-9081;
NCIt synonyms : PGE2 Receptor Antagonist DT-9081; EP4 Receptor Antagonist DT-9081;
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 antagonist DT-9081 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 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 : DT-9081; DT 9081;
NCI Metathesaurus CUI : CL1912867;
Origin ID : C192802;
UMLS CUI : C5785425;
Semantic type(s)
- concept_is_in_subset
- has_target
