title: Stereoselective binding of chiral drugs to plasma proteins.
abstract: Chiral drugs show distinct biochemical and pharmacological behaviors in the human body. The binding of chiral drugs to plasma proteins usually exhibits stereoselectivity, which has a far-reaching influence on their pharmacological activities and pharmacokinetic profiles. In this review, the stereoselective binding of chiral drugs to human serum albumin (HSA), α1-acid glycoprotein (AGP) and lipoprotein, three most important proteins in human plasma, are detailed. Furthermore, the application of AGP variants and recombinant fragments of HSA for studying enantiomer binding properties is also discussed. Apart from the stereoselectivity of enantiomer-protein binding, enantiomer-enantiomer interactions that may induce allosteric effects are also described. Additionally, the techniques and methods used to determine drug-protein binding parameters are briefly reviewed.
authors.affiliation: Laboratory of Pharmaceutical Analysis and Drug Metabolism, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
authors.forename: Qi
authors.initials: Q
authors.lastname: Shen
authors.forename: Lu
authors.initials: L
authors.lastname: Wang
authors.forename: Hui
authors.initials: H
authors.lastname: Zhou
authors.forename: Hui-di
authors.initials: HD
authors.lastname: Jiang
authors.forename: Lu-shan
authors.initials: LS
authors.lastname: Yu
authors.forename: Su
authors.initials: S
authors.lastname: Zeng
mesh_terms: D000494:Allosteric Regulation / Q000502:physiology; D000818:Animals; D001798:Blood Proteins / Q000737:chemistry* / Q000378:metabolism*; D006801:Humans; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism*; D011485:Protein Binding / Q000502:physiology; D013237:Stereoisomerism
chemical_list: D001798:Blood Proteins; D004364:Pharmaceutical Preparations