title: Rapid analysis of interaction between six drugs and β2-adrenergic receptor by injection amount-dependent method.
abstract: Drug-protein interaction analysis has become a considerable topic in life science which includes clarifying protein functions, explaining drug action mechanisms and uncovering novel drug candidates. This work was to determine the association constants (KA) of six drugs to β2-adrenergic receptor by injection amount-dependent method using stationary phase containing the immobilized receptor. The values of KAwere calculated to be (25.85 ± 0.035) × 104m-1for clorprenaline, (42.51 ± 0.054) × 104m-1for clenbuterol, (6.67 ± 0.008) × 104m-1for terbutaline, (33.99 ± 0.025) × 104m-1for tulobuterol, (7.59 ± 0.011) × 104m-1for salbutamol and (78.52 ± 0.087) × 104m-1for bambuterol. This rank order agreed well with the data determined by zonal elution, frontal analysis and nonlinear chromatography, even using different batches of β2-AR column. A good correlation was found between the association constants by the current method and radio-ligand binding assay. Our data indicates that the injection amount-dependent method is a powerful alternative for rapid analysis of ligand-receptor interactions.
authors.affiliation: Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, College of Life Sciences, Northwest University, Xi'an, China.
authors.forename: Kaizhu
authors.initials: K
authors.lastname: Zeng
authors.affiliation: Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, College of Life Sciences, Northwest University, Xi'an, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
authors.affiliation: Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, College of Life Sciences, Northwest University, Xi'an, China.
authors.forename: Zhenyu
authors.initials: Z
authors.lastname: Sun
authors.affiliation: Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, College of Life Sciences, Northwest University, Xi'an, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Li
authors.affiliation: Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, College of Life Sciences, Northwest University, Xi'an, China.
authors.forename: Sha
authors.initials: S
authors.lastname: Liao
authors.affiliation: Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, College of Life Sciences, Northwest University, Xi'an, China.
authors.forename: Xinfeng
authors.initials: X
authors.lastname: Zhao
authors.affiliation: Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, College of Life Sciences, Northwest University, Xi'an, China.
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Zheng
mesh_terms: D002845:Chromatography / Q000379:methods; D004347:Drug Interactions; D008962:Models, Theoretical; D011485:Protein Binding; D011869:Radioligand Assay; D018343:Receptors, Adrenergic, beta-2 / Q000187:drug effects* / Q000378:metabolism
chemical_list: D018343:Receptors, Adrenergic, beta-2
keywords: association constants (KA); injection amount-dependent method; β2-adrenergic receptor