In vitro selection of a peptide aptamer that potentiates inhibition of cyclin-dependent kinase 2 by purvalanol

Abstract

To increase the inhibitory activity of purvalanol against cyclin-dependent kinase 2, we increased the extent of interaction between the inhibitor and the target by coupling a peptide aptamer to purvalanol. The peptide–purvalanol conjugate, selected using a ribosome display, had a significantly enhanced inhibitory effect compared with purvalanol alone. The technique is useful as another type of fragment-based drug design tool.