Unit

UNIT 3.1 Cyclooxygenase Assays

  1. James K. Gierse,
  2. Carol M. Koboldt

Published Online: 1 MAY 2001

DOI: 10.1002/0471141755.ph0301s00

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

Gierse, J. K. and Koboldt, C. M. 2001. Cyclooxygenase Assays. Current Protocols in Pharmacology. 00:3.1:3.1.1–3.1.16.

Author Information

  1. Searle Research and Development, Chesterfield, Missouri

Publication History

  1. Published Online: 1 MAY 2001
  2. Published Print: MAR 1998

Abstract

Cyclooxygenase (COX, also known as prostaglandin H2 synthase, PGH2) is one of the most significant enzymes in pharmacology since COX inhibition is the mechanism of action of most nonsteroidal anti-inflammatory drugs (NSAIDs). There are two forms: COX-1 is a constitutive form of the enzyme that has been linked to the production of physiologically important prostaglandins that may play a role in homeostasis (gastric, renal, etc.). COX-2 is inducible by cytokines and growth factors, and induction of COX-2 is linked to inflammatory cell types and tissues, so COX-2 is believed to be the target for the anti-inflammatory actions of NSAIDs. COX-2 also exists in a constitutive form in kidney and brain. Thus, there is an ongoing effort to identify compounds that will inhibit COX-2 in preference to COX-1 since such an agent may be a safer, and perhaps more efficacious, NSAID. Three assays are provided in this unit for measuring COX activity: one is to measure the final product of the reaction, PGE2, by ELISA; another is to measure directly the oxygen uptake that occurs during the first step of the reaction using an oxygen sensor; and the third is to measure the second reaction (peroxidase function) spectrophotometrically.