Selective inhibitors of JAK1 targeting a subtype-restricted allosteric cysteine
M. E. Kavanagh, B. D. Horning, R. Khattri, N. Roy, J. P. Lu, L. R. Whitby, J. C. Brannon, A. Parker, J. M. Chick, C. L. Eissler, A. Wong, J. L. Rodriguez, S. Rodiles, K. Masuda, J. R. Teijaro, , B. F. Cravatt
This study identifies an allosteric cysteine in JAK1 and TYK2, develops inhibitors targeting it, and shows high subtype selectivity with minimal off-target effects.
bioRxiv · Jan 31, 2022 · PreprintPharmacology & Toxicology