Logan T M, Thériault Y, Fesik S W
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064.
J Mol Biol. 1994 Feb 18;236(2):637-48. doi: 10.1006/jmbi.1994.1173.
Characterizing the structure properties of unfolded proteins is important for understanding the stability and folding of native proteins. However, little structural information is available for the unfolded state. Using recently developed heteronuclear multi-dimensional NMR techniques, the 1H, 13C and 15N chemical shift assignments of the FK506 binding protein (FKBP) unfolded in concentrated urea and guanidine hydrochloride (GuHCl) solutions have been obtained, and the structural properties of unfolded FKBP have been characterized. FKBP displays extensive conformational averaging when unfolded in urea and GuHCl, but defined regions of secondary structure are present. Subtle differences regarding the location and stability of the secondary structures exist between the two solvents. Secondary structure formation in unfolded FKPB was correlated with statistical and thermodynamic predictions of helix formation as well as with the three-dimensional structure of folded FKBP determined by NMR and X-ray crystallography. Residues involved in secondary structures in unfolded FKBP are generally found in the same type of secondary structure in the folded protein. An exception to this was found at the C terminus of FKBP, which forms a different secondary structure in the unfolded and folded states.
表征未折叠蛋白质的结构特性对于理解天然蛋白质的稳定性和折叠过程至关重要。然而,关于未折叠状态的结构信息却很少。利用最近开发的异核多维核磁共振技术,已获得在浓尿素和盐酸胍(GuHCl)溶液中未折叠的FK506结合蛋白(FKBP)的1H、13C和15N化学位移归属,并对未折叠的FKBP的结构特性进行了表征。当在尿素和GuHCl中未折叠时,FKBP呈现出广泛的构象平均化,但存在特定的二级结构区域。两种溶剂之间二级结构的位置和稳定性存在细微差异。未折叠的FKPB中的二级结构形成与螺旋形成的统计和热力学预测以及通过核磁共振和X射线晶体学确定的折叠FKBP的三维结构相关。未折叠的FKBP中参与二级结构的残基通常在折叠蛋白的相同类型二级结构中被发现。在FKBP的C末端发现了一个例外,它在未折叠和折叠状态下形成不同的二级结构。