Discovery of [1,2,4]Triazolo[1,5-<i>a</i>]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists
Ryota Nakajima, Hiroyuki Oono, Sakae Sugiyama, Yohei Matsueda, Tomohide Ida, Shinji Kakuda, Jun Hirata, Atsushi Baba, Akito Makino, Ryo Matsuyama, Ryan D. White, Ryan P. Wurz, Youngsook Shin, Xiaoshan Min, Angel Guzmán-Pérez, Zhulun Wang, Antony Symons, Sanjay K. Singh, Srinivasa Reddy Mothe, Sergei A. Belyakov, Anjan Chakrabarti, Satoshi Shuto
Abstract
in a human whole-blood assay and a mouse IL-18/23-induced cytokine expression model revealed its robust and dose-dependent inhibitory effect on IL-17A production.
Topics & Concepts
RAR-related orphan receptor gammaOrphan receptorInverse agonistPharmacologyChemistryAgonistStereochemistryIn vivoPiperazineReceptorMedicineTranscription factorBiochemistryBiologyGeneBiotechnologyPsoriasis: Treatment and PathogenesisCytokine Signaling Pathways and InteractionsAsthma and respiratory diseases