What is it about?
For pharmacologists the availability or blockers of the function of protein target is integral to understanding their role in physiology. The paper is about characterising a class of blockers of the receptor FFA4 (which is also called GPR120) and defining their mechanism of action.
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Why is it important?
This is the first detailed characterisation of a molecule that acts as a blocker of the receptor FFA4. As the molecule is available commercially a number of research groups have started to use it but without understanding its mechanism of action or potential side-effects and other sites of action. We highlight where it can be used effectively and indicate some precautions that should be applied.
Perspectives
The study will lead to better understanding of the mode of action of a newly described FFA4 antagonist drug and hopefully to the development and use of better antagonists for this receptor.
Graeme Milligan
University of Glasgow
Read the Original
This page is a summary of: Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4, Molecular Pharmacology, April 2017, American Society for Pharmacology & Experimental Therapeutics (ASPET),
DOI: 10.1124/mol.116.107821.
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