Department of Chemistry, University of Puerto Rico, San Juan, Puerto Rico.
Channels (Austin). 2011 Jul-Aug;5(4):345-56. doi: 10.4161/chan.5.4.17082. Epub 2011 Jul 1.
The nicotinic acetylcholine receptor (nAChR) is a member of a family of ligand-gated ion channels that mediate diverse physiological functions, including fast synaptic transmission along the peripheral and central nervous systems. Several studies have made significant advances toward determining the structure and dynamics of the lipid-exposed domains of the nAChR. However, a high-resolution atomic structure of the nAChR still remains elusive. In this study, we extended the Fourier transform coupled tryptophan scanning mutagenesis (FT-TrpScanM) approach to gain insight into the secondary structure of the δM3 transmembrane domain of the Torpedo californica nAChR, to monitor conformational changes experienced by this domain during channel gating, and to identify which lipid-exposed positions are linked to the regulation of ion channel kinetics. The perturbations produced by periodic tryptophan substitutions along the δM3 transmembrane domain were characterized by two-electrode voltage clamp and (125)I-labeled α-bungarotoxin binding assays. The periodicity profiles and Fourier transform spectra of this domain revealed similar helical structures for the closed- and open-channel states. However, changes in the oscillation patterns observed between positions Val-299 and Val-304 during transition between the closed- and open-channel states can be explained by the structural effects caused by the presence of a bending point introduced by a Thr-Gly motif at positions 300-301. The changes in periodicity and localization of residues between the closed-and open-channel states could indicate a structural transition between helix types in this segment of the domain. Overall, the data further demonstrate a functional link between the lipid-exposed transmembrane domain and the nAChR gating machinery.
烟碱型乙酰胆碱受体 (nAChR) 是配体门控离子通道家族的成员,介导多种生理功能,包括外周和中枢神经系统的快速突触传递。几项研究在确定 nAChR 的脂质暴露结构域的结构和动力学方面取得了重大进展。然而,nAChR 的高分辨率原子结构仍然难以捉摸。在这项研究中,我们扩展了傅里叶变换偶联色氨酸扫描诱变 (FT-TrpScanM) 方法,以深入了解加利福尼亚美洲电鳐 nAChR 的 δM3 跨膜域的二级结构,监测该结构域在通道门控过程中经历的构象变化,并确定哪些脂质暴露位置与离子通道动力学的调节有关。通过沿 δM3 跨膜域周期性色氨酸取代产生的扰动通过双电极电压钳和 (125)I 标记的α-银环蛇毒素结合测定来表征。该结构域的周期性分布和傅里叶变换谱揭示了关闭和开放通道状态的类似螺旋结构。然而,在关闭和开放通道状态之间的转变过程中观察到的位置 Val-299 和 Val-304 之间的振动模式变化可以通过在位置 300-301 处存在 Thr-Gly 基序引起的弯曲点引起的结构效应来解释。在关闭和开放通道状态之间的周期性和残基定位的变化可能表明该结构域的这一段中的螺旋类型之间发生了结构转变。总体而言,数据进一步证明了脂质暴露的跨膜结构域和 nAChR 门控机制之间的功能联系。