Cyclooxygenase-1 (COX-1) (COX-1)

Cyclooxygenase-1 (COX-1), formally known as Prostaglandin-endoperoxide synthase 1 (PTGS1), is a constitutive enzyme responsible for the production of prostaglandins and thromboxanes that regulate essential physiological processes [1]. It is expressed in most tissues, where it maintains the integrity of the gastric mucosa, regulates renal blood flow, and facilitates platelet aggregation [2]. In the context of disease, COX-1 is a primary target for nonsteroidal anti-inflammatory drugs (NSAIDs) used to treat pain, fever, and inflammatory conditions [2]. While inhibiting COX-1 provides analgesic and anti-thrombotic benefits, it also leads to significant side effects, most notably gastrointestinal toxicity and renal dysfunction [2]. The interaction with S-ketoprofen acylglucuronide is of particular interest in pharmacology because this reactive metabolite can covalently bind to proteins, potentially altering enzyme activity or contributing to idiosyncratic drug reactions [3, 4]. Understanding the balance between the homeostatic roles of COX-1 and its inhibition by drugs like ketoprofen is crucial for optimizing therapeutic outcomes and minimizing adverse effects. Sources: [1] UniProt. P23219 - PTGS1_HUMAN. https://www.uniprot.org/uniprotkb/P23219/entry [2] StatPearls. NSAIDs. https://www.ncbi.nlm.nih.gov/books/NBK547742/ [3] Castillo, M., et al. (1995). Reactivity of ketoprofen glucuronides. PubMed PMID: 8500314. [4] PubChem. Ketoprofen. https://pubchem.ncbi.nlm.nih.gov/compound/Ketoprofen

Other names

PTGS1Prostaglandin-endoperoxide synthase 1PGHS-1Prostaglandin G/H synthase 1

Inhibition of the cyclooxygenase active site of the enzyme, preventing the conversion of arachidonic acid into prostaglandin H2 (PGH2), the precursor for various prostaglandins and thromboxanes.