
Bioorganic and Medicinal Chemistry Letters p. 2907 - 2912 (2015)
Update date:2022-08-05
Topics:
Fauber, Benjamin P.
Gobbi, Alberto
Robarge, Kirk
Zhou, Aihe
Barnard, Adrian
Cao, Jianhua
Deng, Yuzhong
Eidenschenk, Céline
Everett, Christine
Ganguli, Arunima
Hawkins, Julie
Johnson, Adam R.
La, Hank
Norman, Maxine
Salmon, Gary
Summerhill, Susan
Ouyang, Wenjun
Tang, Wei
Wong, Harvey
The nuclear receptor (NR) retinoic acid receptor-related orphan receptor gamma (RORγ, RORc, or NR1F3) is a promising target for the treatment of autoimmune diseases. RORc is a critical regulator in the production of the pro-inflammatory cytokine interleukin-17. We discovered a series of potent and selective imidazo[1,5-a]pyridine and -pyrimidine RORc inverse agonists. The most potent compounds displayed >300-fold selectivity for RORc over the other ROR family members, PPARγ, and NRs in our cellular selectivity panel. The favorable potency, selectivity, and physiochemical properties of GNE-0946 (9) and GNE-6468 (28), in addition to their potent suppression of IL-17 production in human primary cells, support their use as chemical biology tools to further explore the role of RORc in human biology.
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