e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: an approach for inhibiting protein-protein …
BC Raimundo, JD Oslob, AC Braisted…
Index: 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. Journal of Medicinal Chemistry, 2004 , vol. 47, # 12 p. 3111 - 3130
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) interaction. By use of fragment-based approaches, a compound with millimolar affinity was evolved to a hit series with low micromolar activity, and these compounds were optimized into a lead ...
