Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: An approach for inhibiting protein-protein interactions
Fragment assembly has shown promise for discovering small-molecule antagonists for difficult targets, including protein-protein interactions. Here, we describe a process for identifying a 60 nM inhibitor of the interleukin-2 (IL-2)/IL-2 receptor (IL-2Rα)
Raimundo, Brian C.,Oslob, Johan D.,Braisted, Andrew C.,Hyde, Jennifer,McDowell, Robert S.,Randal, Mike,Waal, Nathan D.,Wilkinson, Jennifer,Yu, Chul H.,Arkin, Michelle R.