Author/Authors :
Nathan D. Waal، نويسنده , , Wenjin Yang، نويسنده , , Johan D. Oslob، نويسنده , , Michelle R. Arkin، نويسنده , , Jennifer Hyde، نويسنده , , Wanli Lu، نويسنده , , Robert S. McDowell، نويسنده , , Chul H. Yu، نويسنده , , Brian C. Raimundo، نويسنده ,
Abstract :
The identification, design, and synthesis of a series of novel sulfamide- and urea-based small-molecule antagonists of the protein–protein interaction IL-2/IL-2Rα are described. Installation of a furan carboxylic acid fragment onto a low-micromolar sulfamide resulted in a 23-fold improvement in activity, providing a sub-micromolar, nonpeptidic IL-2 inhibitor (IC50 = 0.60 μM).
Keywords :
Fragment assembly , IL-2 , Protein–protein interaction , cytokine
