Structure-based design of Trifarotene (CD5789), a potent and selective RARγ agonist for the treatment of acne.

Etienne Thoreau,Jean-Marie Arlabosse,Claire Bouix-Peter,Sandrine Chambon, Laurent Chantalat,Sébastien Daver, Laurence Dumais, Gwenaëlle Duvert, Angélique Feret,Gilles Ouvry, Jonathan Pascau,Catherine Raffin,Nicolas Rodeville, Catherine Soulet, Samuel Tabet,Sandrine Talano, Thibaud Portal

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•X-ray of known RARγ-agonist CD437- RARγ complex was obtained.•Hypothesis for the isotype selectivity of known RARγ-agonist CD437 are presented.•Knowledge derived from the CD437- RARγ complex was used on a novel series of agonists.•Optimisation of potency, selectivity and metabolism led to the identification of CD5789.•CD5789, a potent and selective γ-selective RAR agonist is in Phase 3 clinical trials for the topical treatment of acne.

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Trifarotene,RARγ,CD5789,CD437,Acne

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