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Prostaglandin-endoperoxide synthase 2 - COX2

Target Class Non-Kinase Enzymes FamilyCyclooxygenase
SpeciesHuman   
Background
Prostaglandin-endoperoxide synthase (PTGS), also known as cyclooxygenase, is the key enzyme in prostaglandin biosynthesis, and acts both as a dioxygenase and as a peroxidase. There are two isozymes of PTGS: a constitutive PTGS1 and an inducible PTGS2, which differ in their regulation of expression and tissue distribution. This gene encodes the inducible isozyme. It is regulated by specific stimulatory events, suggesting that it is responsible for the prostanoid biosynthesis involved in inflammation and mitogenesis. [provided by RefSeq, Feb 2009]

Protein Source
Human(recombinant): Expressed in Sf9 insect cells using baculovirus
Readout
Enzymatic activity
Method
Detect conversion of arachidonic acid to PPG2 using fluorometirc readout
Substrate
Arachidonic Acid
Agonist Effect (Activation)
insufficient information
Antagonist Effect (Inhibition)
anti-inflammatory activity; anti-mitogenic effects; myocardial infarction; increase BP; ischaemic stroke; atherothrombosis
Ref.
Bowes et. al. 2012
AntagonistIC50(nM)
Diclofenac13
NS-398 24
COX enzyme stocks are diluted in Assay Buffer (TPP-500 + 100 nM Hematin) and allowed to equilibrate with compounds at RT for 30 minutes (binding incubation). Arachidonic acid (17 uM) and Ampliflu Red (25 uM) are prepared and dispensed into reaction plate. Plates read immediately on a fluorimeter with the emission detection at 590 nm with excitation wavelength 544 nm.
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