Raimundo, Brian C. published the artcileIntegrating 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: 2-Chloro-4-hydroxyphenylboronic acid, the publication is Journal of Medicinal Chemistry (2004), 47(12), 3111-3130, database is CAplus and MEDLINE.
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 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, Recommanded Product: 2-Chloro-4-hydroxyphenylboronic acid.
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