Design, Synthesis, and Evaluation of an α-Helix Mimetic Library Targeting Protein− Protein Interactions

A Shaginian, LR Whitby, S Hong, I Hwang…

Index: Shaginian, Alex; Whitby, Landon R.; Hong, Sukwon; Hwang, Inkyu; Farooqi, Bilal; et al. Journal of the American Chemical Society, 2009 , vol. 131, p. 5564 - 5572

Full Text: HTML

Citation Number: 113

Abstract

The design and solution-phase synthesis of an α-helix mimetic library as an integral component of a small-molecule library targeting protein− protein interactions are described. The iterative design, synthesis, and evaluation of the candidate α-helix mimetic was initiated from a precedented triaryl template and refined by screening the designs for inhibition of MDM2/p53 binding. Upon identifying a chemically and biologically satisfactory design and ...