Rational design of diflunisal analogues with reduced affinity for human serum albumin

…, PJ Hajduk, R Craig, R Bell, T Borre…

文献索引：Mao; Hajduk; Craig; Bell; Borre; Fesik Journal of the American Chemical Society, 2001 , vol. 123, # 43 p. 10429 - 10435

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被引用次数: 84

摘要

Many lead compounds bind to serum albumin and exhibit markedly reduced efficacy in vivo as compared to their potency in vitro. To aid in the design of compounds with reduced albumin binding, we performed nuclear magnetic resonance (NMR) structural and binding studies on the complex between domain III of human serum albumin (HSA-III) and diflunisal, a cyclooxygenase inhibitor with antiinflammatory activity. The structural studies indicate ...