225122-54-3Relevant articles and documents
Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: An approach for inhibiting protein-protein interactions
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.
, p. 3111 - 3130 (2007/10/03)
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)
Discovery of a potent small molecule IL-2 inhibitor through fragment assembly
Braisted, Andrew C.,Oslob, Johan D.,Delano, Warren L.,Hyde, Jennifer,McDowell, Robert S.,Waal, Nathan,Yu, Chul,Arkin, Michelle R.,Raimundo, Brian C.
, p. 3714 - 3715 (2007/10/03)
Using a site-directed fragment discovery method called tethering, we have identified a 60 nM small molecule antagonist of a cytokine/receptor interaction (IL-2/IL2Rα) with cell-based activity. Starting with a low micromolar hit, we employed a combination