Han Daniel S, Wang Simon X, Weinstein Harel
Department of Physiology and Biophysics, Weill Medical College, Cornell University, 1300 York Avenue, New York, New York 10021, USA.
Biochemistry. 2008 Jul 15;47(28):7317-21. doi: 10.1021/bi800442g. Epub 2008 Jun 18.
G-Protein-coupled receptors (GPCRs) adopt various functionally relevant conformational states in cell signaling processes. Recently determined crystal structures of rhodopsin and the beta 2-adrenergic receptor (beta 2-AR) offer insight into previously uncharacterized active conformations, but the molecular states of these GPCRs are likely to contain both inactive and active-like conformational elements. We have identified conformational rearrangements in the dynamics of the TM7-HX8 segment that relate to the properties of the conserved NPxxY(x)5,6F motif and show that they can be used to identify active state-like conformational elements in the corresponding regions of the new structures of rhodopsin and the beta 2-AR.
G蛋白偶联受体（GPCRs）在细胞信号传导过程中呈现出各种功能相关的构象状态。最近确定的视紫红质和β2肾上腺素能受体（β2-AR）的晶体结构为以前未表征的活性构象提供了见解，但这些GPCRs的分子状态可能同时包含非活性和活性样构象元件。我们已经在TM7-HX8片段的动力学中鉴定出与保守的NPxxY(x)5,6F基序特性相关的构象重排，并表明它们可用于识别视紫红质和β2-AR新结构相应区域中的活性状态样构象元件。
