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Biology

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2018

Inhibitor

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Theobromine And Related Methylxanthines As Inhibitors Of Primary Amine Oxidase, Padraig Shanahan, Jeffrey O’Sullivan, Keith Tipton, Gemma Kinsella, Barry Ryan, Gary Henehan Oct 2018

Theobromine And Related Methylxanthines As Inhibitors Of Primary Amine Oxidase, Padraig Shanahan, Jeffrey O’Sullivan, Keith Tipton, Gemma Kinsella, Barry Ryan, Gary Henehan

Articles

Methylxanthines are the most widely consumed drugs in the world and evidence of their health benefits has been growing in recent years. Primary Amine Oxidase (PrAO) has been recognised as a therapeutic target for amelioration of inflammatory, vascular and neurodegenerative diseases. Previous work in our laboratories showed that caffeine inhibited Bovine PrAO with a Ki of 1.0mM using benzylamine as substrate.

This study aimed to extend our previous work and explore the possibility that related methylxanthines might influence PrAO activity. While paraxanthine, theophylline and 7-methylxanthine had little effect on PrAO, theobromine was a noncompetitive inhibitor with a Ki of 276±44µM. …