PTGS1
PTGS1 (Prostaglandin G/H synthase 1) is an enzyme. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it.
Overview
Dual cyclooxygenase and peroxidase that plays an important role in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response. The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes. This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins.
Open Targets scores its association with cancer at 0.62 (direct and indirect evidence; datatypes literature 0.93, animal model 0.64, genetic association 0.37, clinical 0.88).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · PTGS1 (Prostaglandin G/H synthase 1) is an enzyme. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it.
- 1 · What it is
PTGS1 (Prostaglandin G/H synthase 1) is an enzyme. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it.
- 2 · What goes wrong in cancer
Dual cyclooxygenase and peroxidase that plays an important role in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response.
- 3 · How drugs use it
No product in this corpus aims at PTGS1 yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
External identifiers
Sources: HGNC HGNC:9604 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P23219 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000095303 (association with cancer (MONDO_0004992) 0.62; (GraphQL API, CC0))
Biology
Dual cyclooxygenase and peroxidase that plays an important role in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response. The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes. This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins. The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. Location: Microsome membrane; Endoplasmic reticulum membrane (UniProt). Locus 9q33.2 (HGNC).
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: Open Targets known-drug datatype score 0.88. Evidence tier "approved-drug" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery for this target: (TITLE:"PTGS1" OR ABSTRACT:"PTGS1" OR TITLE:"prostaglandin-endoperoxide synthase 1" OR ABSTRACT:"prostaglandin-endoperoxide synthase 1" OR TITLE:"Prostaglandin G/H synthase 1" OR ABSTRACT:"Prostaglandin G/H synthase 1" OR TITLE:"COX1" OR ABSTRACT:"COX1" OR TITLE:"PGHS-1" OR ABSTRACT:"PGHS-1" OR TITLE:"PTGHS" OR ABSTRACT:"PTGHS") 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 PTGS1, not a curated reading list.