Identification of an aminothiazole series of RORβ modulators

Crystallography has identified stearic acid, ALRT 1550 and ATRA as ligands that bind RORβ, however, none of these molecules represent good starting points to develop optimized small molecule modulators. Recently, Compound 1 was identified as a potent dual RORβ and RORγ inverse agonist with no activi...

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Pubblicato in:Bioorg Med Chem Lett
Autori principali: Patouret, Rémi, Doebelin, Christelle, Garcia-Ordonez, Ruben D., Chang, Mi Ra, Ruiz, Claudia, Cameron, Michael D., Griffin, Patrick R., Kamenecka, Theodore M.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2018
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5859951/
https://ncbi.nlm.nih.gov/pubmed/29534930
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2018.03.001
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