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. published the artcile< Integrating Fragment Assembly and Biophysical Methods in the Chemical Advancement of Small-Molecule Antagonists of IL-2: An Approach for Inhibiting Protein-Protein Interactions>, Recommanded Product: Methyl 2,3-dichlorobenzoate, the main research area is interleukin 2 receptor antagonist drug design.
Fragment assembly has shown promise for discovering small-mol. antagonists for difficult targets, including protein-protein interactions. Here, the authors 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 series with nanomolar affinity. Fragment assembly was useful not only for hit identification, but also for lead optimization. Throughout the discovery process, biophys. methods and structural biol. demonstrated that compounds bound reversibly to IL-2 at the IL-2 receptor binding site.
Journal of Medicinal Chemistry published new progress about CD25 antigens Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (antagonists). 2905-54-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6Cl2O2, Recommanded Product: Methyl 2,3-dichlorobenzoate.
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Chlorides – an overview | ScienceDirect Topics