Preferred Label : EP2/EP4 Antagonist TPST-1495;
NCIt synonyms : PGE2 EP2/EP4 Receptor Antagonist TPST-1495; Prostaglandin E2 Receptor EP2/EP4 Antagonist TPST-1495; Dual EP2/4 Antagonist TPST-1495;
NCIt definition : An orally bioavailable, dual antagonist of the human prostaglandin E2 receptor subtypes
2 (EP2) and 4 (EP4), with potential immunomodulating and antineoplastic activities.
Upon oral administration, the EP2/EP4 antagonist TPST-1495 selectively targets and
binds to EP2 and EP4, inhibiting the binding of the immunosuppressive prostaglandin
E2 (PGE2) to EP2 and EP4. This prevents the activation of EP2 and EP4, and inhibits
PGE2-EP2/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-EP2/4
signaling pathway is over-activated. EP2 and EP4, G protein-coupled receptors (GPCRs)
that are overexpressed in certain types of cancers, promote tumor cell proliferation,
invasion, survival, and metastasis.;
Molecule name : TPST-1495; TPST 1495;
NCI Metathesaurus CUI : CL1412010;
Origin ID : C174460;
UMLS CUI : C5418097;
Semantic type(s)
- concept_is_in_subset
- has_target
