Document Report Card

ID: ALA1122633

Journal: J Med Chem

Title: Interactions of antitumor drugs with natural DNA: 1H NMR study of binding mode and kinetics.

Authors: Feigon J, Denny WA, Leupin W, Kearns DR.

Abstract: 1H NMR has been used to study the interactions of over 70 clinical and experimental antitumor drugs with DNA. Spectra of the low-field (H-bonded imino proton) resonances of DNA were studied as a function of drug per base pair ratio. From the spectral changes observed, it was possible to distinguish three modes of drug binding (intercalation, groove binding, and nonspecific outside binding), to determine the kinetics of drug binding (approximate lifetime of the bound drug), and, in favorable cases, to determine the specificity of the drugs for A X T or G X C base pairs. This method is a useful assay for general drug-binding characteristics. For the intercalating compounds there appears to be a correlation between drug-binding kinetics and useful antitumor activity.

CiteXplore: 6708048

DOI: 10.1021/jm00370a007