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

12:06 pm 20 Dec 2017

Available online: 6 December 2017

D.W. was supported by an Australian Postgraduate Award through the Western Sydney University and a South Western Sydney Local Health District Top-Up Scholarship from the Liverpool Radiation Oncology Department, Liverpool Hospital. The authors acknowledge the facilities, and the scientific and technical assistance of the National Imaging Facility, Western Sydney University Node.

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 0.38 mM) with drug concentrations ranging from 0.005–0.16 M at 298 K. 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 ± 4 M− 1, respectively.

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