Cyclooxygenase (COX) enzymes are primarily associated in initiating syntheses of prostaglandins responsible for regulating physiological processes and immune responses. Whereas COX-2 over-expression has been implicated in various pathological conditions associated with inflammatory diseases. Even neurodegenerative and cancerous tissues have been observed to contain elevated levels of COX-2. There are two isoforms: COX-1 is constitutively expressed in most cell types whereas COX-2 is induced by inflammatory and proliferative conditions. COX inhibitors have been commonly used in clinics as expansive class of NSAIDs. But it has been difficult to determine the activity of isoform selective COX towards inhibitor development and furthering understanding of its biological roles. Fluorescent probes attached to COX inhibitors have been developed but may affect the enzymatic levels and most are associated with high background signals. In this study we have developed an isoform selective activity based probe for COX-2 to further demonstrate its performance in vitro and in live cell models of inflammation.

Development of an activity-based probe for cyclooxygenase-2 (COX-2)

2019 Fall National Meeting

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