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Prostaglandin-endoperoxide synthase 1 - COX1

Target Class Non-Kinase Enzymes FamilyCyclooxygenase
SpeciesHuman   
Background
This is one of two genes encoding similar enzymes that catalyze the conversion of arachinodate to prostaglandin. The encoded protein regulates angiogenesis in endothelial cells, and is inhibited by nonsteroidal anti-inflammatory drugs such as aspirin. Based on its ability to function as both a cyclooxygenase and as a peroxidase, the encoded protein has been identified as a moonlighting protein. The protein may promote cell proliferation during tumor progression. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Jan 2014]

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)
gastric and pulmonary bleeding; dyspepsia; renal dysfunction
Ref.
Bowes et. al. 2012
AntagonistIC50(nM)
Diclofenac3
Indomethacin43
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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