albumin - publications

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1. Molecules. 2012 Feb 17;17(2):2000-14.

Impact of Halogen Substituents on Interactions between
2-Phenyl-2,3-dihydroqulinazolin-4(1H)-one Derivatives and Human Serum Albumin.

Liu F, Wang Y, Lv C, Wang L, Ou J, Wang M, Liu S.

Department of Applied Chemistry, China Agricultural University, Beijing 100193,
China. shangzho@cau.edu.cn.

A novel type of 2-(un)substituted phenyl-2,3-dihydroquinazolin-4(1H)-one (DQL)
derivatives were designed and synthesized to study the impact of halogen
substituents on interactions between DQL and human serum albumin (HSA) by
comparison methodology. The interactions between DQL and HSA were studied by
fluorescence spectroscopy. The intrinsic fluorescence of human serum albumin was
quenched by DQL through a static quenching mechanism. Site marker competitive
experiments showed that DQL bound to HSA in site II (subdomain IIIA). The binding
constants, the numbers of binding sites and the thermodynamic parameters were
measured too. The results indicated that the interactions were spontaneous,
mainly through hydrophobic forces, and the substitution by halogen atoms in the
benzene ring could increase the interactions between DQL and HSA. Furthermore,
the binding affinity was enhanced gradually with the increasing of halogen atomic
number.

PMID: 22343405 [PubMed - in process]