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Old drugs with new skills: fenoprofen as an allosteric enhancer at melanocortin receptor 3
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Old drugs with new skills: fenoprofen as an allosteric enhancer at melanocortin receptor 3
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Journal Article
Old drugs with new skills: fenoprofen as an allosteric enhancer at melanocortin receptor 3
2017
Overview
The efficiency of drug research and development has paradoxically declined over the last decades despite major scientific and technological advances, promoting new cost-effective strategies such as drug repositioning by systematic screening for new actions of known drugs. Here, we performed a screening for positive allosteric modulators (PAMs) at melanocortin (MC) receptors. The non-steroidal anti-inflammatory drug fenoprofen, but not the similar compound ibuprofen, presented PAM activity at MC
3
, MC
4
, and MC
5
receptors. In a model of inflammatory arthritis, fenoprofen afforded potent inhibition while ibuprofen was nearly inactive. Fenoprofen presented anti-arthritic actions on cartilage integrity and synovitis, effects markedly attenuated in Mc3r−/− mice. Fenoprofen displayed pro-resolving properties promoting macrophage phagocytosis and efferocytosis, independently of cyclooxygenase inhibition. In conclusion, combining repositioning with advances in G-protein coupled receptor biology (
allosterism
) may lead to potential new therapeutics. In addition, MC
3
PAMs emerged as a viable approach to the development of innovative therapeutics for joint diseases.
Publisher
Springer International Publishing,Springer Nature B.V
Subject
/ Allosteric Regulation - drug effects
/ Animals
/ Anti-Inflammatory Agents, Non-Steroidal - pharmacology
/ Anti-Inflammatory Agents, Non-Steroidal - therapeutic use
/ Biomedical and Life Sciences
/ Fenoprofen - therapeutic use
/ Male
/ Mice
/ Nonsteroidal anti-inflammatory drugs
/ Original
/ Peritonitis - chemically induced
/ Prostaglandin endoperoxide synthase
/ Prostaglandin-Endoperoxide Synthases - chemistry
/ Prostaglandin-Endoperoxide Synthases - metabolism
/ R&D
/ Receptor, Melanocortin, Type 3 - chemistry
/ Receptor, Melanocortin, Type 3 - deficiency
/ Receptor, Melanocortin, Type 3 - genetics
