Recognition and discrimination of DNA quadruplexes by acridine-peptide conjugates.

ABSTRACT: We have explored a series of trisubstituted acridine-peptide conjugates for their ability to recognize and discriminate between DNA quadruplexes derived from the human telomere, and the c-kit and N-ras proto-oncogenes. Quadruplex affinity was measured as the peptide sequences were varied, together with their substitution position on the acridine, and the identity of the C-terminus (acid or amide). Surface plasmon resonance measurements revealed that all compounds bound to the human telomeric quadruplex with sub-micromolar affinity. Docking calculations from molecular modelling studies were used to model the effects of substituent orientation and peptide sequence. Modelling and experiment were in agreement that placement of the peptide over the face of the acridine is detrimental to binding

SUBMITTER: Redman JE 

PROVIDER: S-EPMC2736543 | biostudies-literature | 2009 Jan

REPOSITORIES: biostudies-literature