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EP4 is one of the receptors for prostaglandin E2, a signal many tumours release that quietens the immune cells around them. EP4 blockers are meant to lift that suppression, and two are in early trials, one with pembrolizumab.
PTGER4, the EP4 receptor (chromosome 5p13.1), is a receptor for prostaglandin E2 that signals through G(s) proteins to stimulate adenylate cyclase (UniProt P35408). A 2017 Oncoimmunology study described prostaglandin E2 as a powerful immunosuppressor in the tumour microenvironment acting through its four receptors, EP1 to EP4; the oral EP4-specific antagonist E7046 inhibited prostaglandin E2-driven pro-tumour myeloid cells and reduced or rejected established mouse tumours in a manner dependent on myeloid and CD8 T cells (Albu et al., doi:10.1080/2162402X.2017.1338239). In OnCo, INV-1120 is an EP4 antagonist tested alone and with pembrolizumab, and DT-9081 an oral EP4 antagonist aimed at prostaglandin E2 made by COX-2-positive tumours.
In plain words · EP4 is one of the receptors for prostaglandin E2, a signal many tumours release that quietens the immune cells around them. EP4 blockers are meant to lift that suppression, and two are in early trials, one with pembrolizumab.
EP4 is one of the receptors for prostaglandin E2, a signal many tumours release that quietens the immune cells around them. EP4 blockers are meant to lift that suppression, and two are in early trials, one with pembrolizumab.
G protein-coupled receptor for prostaglandin E2 coupled to G(s) and cyclic AMP (UniProt P35408).
1 product aims at EP4 (PTGER4): small molecules. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
G protein-coupled receptor for prostaglandin E2 coupled to G(s) and cyclic AMP (UniProt P35408).
INV-1120 is an experimental EP4 antagonist from Shenzhen Ionova Life Sciences, in phase 1 trials for advanced solid tumours.
Query for this target: (TITLE:"EP4" OR ABSTRACT:"EP4" OR TITLE:"PTGER4" OR ABSTRACT:"PTGER4" OR TITLE:"prostaglandin E receptor 4" OR ABSTRACT:"prostaglandin E receptor 4" OR TITLE:"EP4 receptor" OR ABSTRACT:"EP4 receptor") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about EP4 (PTGER4), not a curated reading list.
Shares Metastatic cancer (cancer that has spread) and the tag pipeline-gap-target.
Shares Metastatic cancer (cancer that has spread) and the tag pipeline-gap-target.
Shares Metastatic cancer (cancer that has spread) and the tag pipeline-gap-target.
Shares Metastatic cancer (cancer that has spread) and the tag pipeline-gap-target.
Shares INV-1120, Metastatic cancer (cancer that has spread).
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