A Novel Method using Nuclear Magnetic Resonance for Plasma Protein Binding Assessment in Drug Discovery Programs

Publication date: Available online 31 January 2019Source: Journal of Pharmaceutical and Biomedical AnalysisAuthor(s): Mariana Gallo, Sara Matteucci, Nadine Alaimo, Erica Pitti, Maria V. Orsale, Vincenzo Summa, Daniel O. Cicero, Edith MonteagudoAbstractA new methodology based on Nuclear Magnetic Resonance (NMR) was developed to determine plasma protein binding (PPB) of drug candidates in drug discovery programs. A strong correlation was found between the attenuation of NMR signals of diverse drugs in the presence of different plasma concentrations and their fraction bound (fb) reported in the literature. Based on these results, a protocol for a rapid calculation of fb of small molecules was established. The advantage of using plasma instead of purified recombinant proteins and the possibility of pool analysis to increase throughput were also evaluated. This novel methodology proved to be very versatile, cost-effective, fast and suitable for automation. As a plus, it contemporarily provides a quality check and solubility of the compound.
Source: Journal of Pharmaceutical and Biomedical Analysis - Category: Drugs & Pharmacology Source Type: research

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Source: NIH Calendar of Events - Category: American Health Source Type: events
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Source: NIH Calendar of Events - Category: American Health Source Type: events
Date: Monday, 01 27, 2020; Speaker: Lisa Ingraham, Ph.D., University of California, San Francisco; Porter Neuroscience Bldg, 35a; G620-640; Videocast Event
Source: NIH Calendar of Events - Category: American Health Source Type: events
Date: Friday, 11 22, 2019; Speaker: various; Building 38; Conference room B, second floor
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