Pseudoirreversible inhibition elicits persistent efficacy of a sphigosine-1-phosphate receptor-1 antagonist
Y. Maruyama, Y. Ohsawa, T. Suzuki, Y. Yamauchi, K. Ohno, H. Inoue, A. Yamamoto, M. Hayashi, Y. Okuhara, W. Muramatsu, K. Namiki, M. Miyauchi, T. Miyao, N. Hagiwara, T. Ishikawa, , T. Akiyama
This study identifies KSI-6666 as a pseudoirreversible S1PR1 antagonist that suppresses inflammation through interaction with a methionine residue.
bioRxiv · May 8, 2023 · PreprintPharmacology & Toxicology