NMR diffusion and relaxation studies of 2-nitroimidazole and albumin interactions

Abstract

Nitroimidazole derivatives are of current interest in the development of hypoxia targeting agents and show potential in the establishment of quantitative measures of tumor hypoxia. In this study, the binding of 2-nitroimidazole to albumin was probed using NMR diffusion and relaxation measurements. Binding studies were conducted at three different protein concentrations (0.23, 0.30 and 0.38mM) with drug concentrations ranging from 0.005-0.16M at 298K. Quantitative assessments of the binding model were made by evaluating the number of binding sites, n, and association constant, K. These were determined to be 21±3 and 53±4M^-1, respectively.

Keywords: 2-nitroimidazole; Diffusion; Hypoxia; Relaxation.