Structure-based de novo design of ligands using a three-dimensional model of the insulin receptor

…, L Wei, FP Ottensmeyer, I Goldfine, BA Maddux…

文献索引：Tan, Christopher; Wei, Lianhu; Ottensmeyer, F. Peter; Goldfine, Ira; Maddux, Betty A.; Yip, Cecil C.; Batey, Robert A.; Kotra, Lakshmi P. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 6 p. 1407 - 1410

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被引用次数: 18

摘要

For the first time, a three-dimensional model of the insulin receptor is used in the de novo design of novel ligands that potentially mimic interactions of insulin at its receptor. Compound 4 competed with insulin as seen in autophosphorylation assays and inhibited up to 68% of IR autophosphorylation at 300 μM of 4 in 3T3IR cells induced by 1 nM insulin. This model provides a basis for the design of potent insulin receptor ligands.