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Combinatorial Chemistry & High Throughput Screening


ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Novel Affinity Ligands for Chromatography Using Combinatorial Chemistry

Author(s): Tor Regberg, Charlotta Lindquist, Ake Pilotti, Christel Ellstrom, Lars Fagerstam, Ann Eckersten, Yasuro Shinohara, Steven L. Gallion and Joseph C. Hogan

Volume 14, Issue 4, 2011

Page: [267 - 278] Pages: 12

DOI: 10.2174/138620711795222482

Price: $65


Spatially addressable combinatorial libraries were synthesized by solution phase chemistry and screened for binding to human serum albumin. Members of arylidene diamide libraries were among the best hits found, having submicromolar binding affinities. The results were analyzed by the frequency with which particular substituents appeared among the most potent compounds. After immobilization of the ligands either through the oxazolone or the amine substituent, characterization by surface plasmon resonance showed that ibuprofen affected the binding kinetics, but phenylbutazone did not. It is therefore likely that these compounds bind to Site 2 in sub domain IIIA of human serum albumin (HSA).

Keywords: Affinity chromatography, combinatorial chemistry, high-throughput screening, arylidene diamide library, Ligands, macromolecules, structure-activity relationships, HPLC, Immobilization, Solution Phase Screening

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