Species-dependent binding of new synthesized bicalutamide analogues to albumin by optical biosensor analysis

Journal of Pharmaceutical and Biomedical Analysis
Cecilia FortugnoCarlo Bertucci

Abstract

The binding of some novel bicalutamide analogues to human serum albumin (HSA) and rat serum albumin (RSA) was investigated by surface plasmon resonance (SPR) based optical biosensor technique. The serum protein binding of the bicalutamide analogues was determined and compared to that of the parent compound. Furthermore, HSA and RSA were used as target plasma proteins, in order to highlight possible differences among species when performing pharmacokinetic studies. HSA and RSA were covalently immobilized on carboxymethyl dextran matrixes, using an amine coupling procedure. The anchoring method was validated by determining the dissociation constant (KD) of a standard analyte to confirm that the binding properties of the proteins were maintained. The ranking of the bicalutamide analogues for their HSA and RSA bound fractions was used to compare the behaviour of the two albumins. Most of the bicalutamide analogues showed higher binding levels with respect to the lead compound, (R)-bicalutamide. Further, meaningful differences in the binding level to the two serum proteins were obtained. The dissociation constants (KD) of the interaction between the lead compound, (R)-bicalutamide, and the two proteins were calculated. As a result, ...Continue Reading

References

Sep 21, 2000·Pharmaceutical Science & Technology Today·D G Myszka, R L Rich
Mar 16, 2002·Science·W David Wilson
Apr 10, 2002·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·David S Hage
Jul 18, 2002·Nature Reviews. Drug Discovery·Matthew A Cooper
Aug 6, 2003·Journal of Pharmaceutical and Biomedical Analysis·Carlo Bertucci, Samanta Cimitan
Oct 1, 1993·British Journal of Clinical Pharmacology·I D CockshottD C Jones
Sep 20, 2005·Journal of Molecular Biology·Jamie GhumanStephen Curry
Nov 15, 2006·Current Pharmaceutical Design·Walter Huber, Francis Mueller
Sep 28, 2007·Combinatorial Chemistry & High Throughput Screening·Carlo BertucciMarco Pistolozzi
Jun 17, 2008·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Hee Seung Kim, Irving W Wainer
Oct 22, 2008·Journal of Pharmaceutical Sciences·Nathan E BaskenMark A Green
May 11, 2010·Analytical and Bioanalytical Chemistry·Karine VuignierSophie Martel
Jul 27, 2010·Analytical and Bioanalytical Chemistry·Carlo BertucciAngela De Simone
Jan 11, 2012·Molecular Aspects of Medicine·Gabriella FanaliPaolo Ascenzi
Jun 14, 2012·ACS Medicinal Chemistry Letters·Greta VarchiGabriella Castoria

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Citations

Apr 20, 2017·Sensors·Dario CompagnoneAntonella Tajani

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