Zhu Z, Bulgakov O V, Scott S S, Dalton J T
Division of Pharmaceutics and Pharmaceutical Chemistry, College of Pharmacy, Ohio State University, Columbus, Ohio 43210, USA.
Biochem Biophys Res Commun. 2001 Jun 15;284(3):828-35. doi: 10.1006/bbrc.2001.5029.
A full-length human androgen receptor (hAR) cDNA was used to produce recombinant baculovirus. Spodoptera frugiperda (Sf9) cells infected with this virus expressed protein with an N-terminal hexahistidine tag (His(6)-hAR) in soluble and insoluble forms. The soluble cytosolic His(6)-hAR demonstrated similar association and dissociation half-times for mibolerone, similar binding affinity for mibolerone, and similar steroid specificity as bona fide AR. Under native conditions, the soluble cytosolic His(6)-hAR was purified to apparent homogeneity in the presence of dihydrotestosterone, using metal ion affinity chromatography. The insoluble pellet fraction was solubilized with strong denaturant 6 M guanidine HCl, and His(6)-hAR was purified from it in the presence of 6 M guanidine HCl. Both the solubilized crude pellet fraction and the solubilized/purified His(6)-hAR could be renatured to bind mibolerone. The baculovirus system will therefore provide an efficient means for producing hAR for ligand-binding assays, as well as purifying hAR for detailed molecular analyses.
使用全长人雄激素受体(hAR)cDNA制备重组杆状病毒。感染该病毒的草地贪夜蛾(Sf9)细胞以可溶性和不溶性形式表达带有N端六组氨酸标签(His(6)-hAR)的蛋白质。可溶性胞质His(6)-hAR对米勃酮表现出相似的结合和解离半衰期、对米勃酮具有相似的结合亲和力以及与真正的AR相似的类固醇特异性。在天然条件下,使用金属离子亲和色谱法,在二氢睾酮存在的情况下,将可溶性胞质His(6)-hAR纯化至表观均一性。不溶性沉淀部分用强变性剂6 M盐酸胍溶解,并在6 M盐酸胍存在的情况下从中纯化His(6)-hAR。溶解的粗沉淀部分和溶解/纯化的His(6)-hAR都可以复性以结合米勃酮。因此,杆状病毒系统将为生产用于配体结合测定的hAR以及纯化用于详细分子分析的hAR提供一种有效的方法。