The binding site of acetylcholine receptor as visualized in the X-Ray structure of a complex between alpha-bungarotoxin and a mimotope peptide.

Harel M; Kasher R; Nicolas A; Guss JM; Balass M; Fridkin M; Smit AB; Brejc K; Sixma TK; Katchalski-Katzir E; Sussman JL; Fuchs S

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The binding site of acetylcholine receptor as visualized in the X-Ray structure of a complex between alpha-bungarotoxin and a mimotope peptide.

机译：乙酰胆碱受体的结合位点在α-邦加毒素和模拟表位多肽之间的复合物的X射线结构中可见。

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We have determined the crystal structure at 1.8 A resolution of a complex of alpha-bungarotoxin with a high affinity 13-residue peptide that is homologous to the binding region of the alpha subunit of acetylcholine receptor. The peptide fits snugly to the toxin and adopts a beta hairpin conformation. The structures of the bound peptide and the homologous loop of acetylcholine binding protein, a soluble analog of the extracellular domain of acetylcholine receptor, are remarkably similar. Their superposition indicates that the toxin wraps around the receptor binding site loop, and in addition, binds tightly at the interface of two of the receptor subunits where it inserts a finger into the ligand binding site, thus blocking access to the acetylcholine binding site and explaining its strong antagonistic activity.

机译：我们已经确定了α-邦格鲁毒素与高亲和力13-残基肽的复合物在1.8 A分辨率下的晶体结构，该肽与乙酰胆碱受体的α亚基的结合区同源。该肽紧贴毒素，并采用β发夹结构。结合的肽的结构和乙酰胆碱结合蛋白的同源环（乙酰胆碱受体的胞外域的可溶性类似物）非常相似。它们的叠加表明该毒素包裹在受体结合位点环周围，此外，在两个受体亚基的界面处紧密结合，在该处将手指插入配体结合位点，从而阻止了对乙酰胆碱结合位点的访问，并解释了其强大的拮抗活性。

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《Neuron》 |2001年第2期|共11页
作者
Harel M; Kasher R; Nicolas A; Guss JM; Balass M; Fridkin M; Smit AB; Brejc K; Sixma TK; Katchalski-Katzir E; Sussman JL; Fuchs S;
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正文语种 eng
中图分类神经生理学;
关键词
Bungarotoxins; Crystallography; X-Ray; Peptide Fragments; Receptors; Cholinergic; 环蛇毒素类; 结晶学; X线; 肽碎片; 受体; 胆碱能;

机译：Bungarotoxins;Crystallography;X-Ray;Peptide Fragments;Receptors;Cholinergic;环蛇毒素类;结晶学;X线;肽碎片;受体;胆碱能;

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专利

1. 管藻目绿藻刺松藻PSⅡ捕光复合物多肽结构分析 [J] . 陈敏, 李爱芬, 周百成植物学报（英文版） . 2002,第002期
2. The binding site of acetylcholine receptor as visualized in the X-Ray structure of a complex between alpha-bungarotoxin and a mimotope peptide. [J] . Harel M, Kasher R, Nicolas A, Neuron . 2001,第2期

机译：乙酰胆碱受体的结合位点在α-邦加毒素和模拟表位多肽之间的复合物的X射线结构中可见。
3. Design and synthesis of peptides that bind alpha-bungarotoxin with high affinity and mimic the three-dimensional structure of the binding-site of acetylcholine receptor. [J] . Katchalski Katzir E, Kasher R, Balass M, Biophysical Chemistry: An International Journal Devoted to the Physical Chemistry of Biological Phenomena . 2003,第1a3期

机译：设计和合成以高亲和力结合α-真菌毒素并模拟乙酰胆碱受体结合位点的三维结构的肽。
4. Molecular characterization of Dalpha6 and Dalpha7 nicotinic acetylcholine receptor subunits from Drosophila: formation of a high-affinity alpha-bungarotoxin binding site revealed by expression of subunit chimeras. [J] . Lansdell SJ, Millar NS Journal of Neurochemistry: Offical Journal of the International Society for Neurochemistry . 2004,第2期

机译：果蝇的Dalpha6和Dalpha7烟碱乙酰胆碱受体亚基的分子表征：亚基嵌合体的表达揭示了高亲和力的α-真菌毒素结合位点的形成。
5. MOLECULAR BASIS OF THE MAJOR DIFFERENCE BETWEEN THE X-RAY STRUCTURE OF CYTOCHROME b_6f COMPLEX FROM M. LAMINOSUS AND C. REINHARDTII: THE BINDING SITE OF TRIDECYL-STIGMATELLIN [C] . Jiusheng Yan, William A. Cramer International Congress of Photosynthesis . 2005

机译：分子基于M.Laminosus和C.Reinhardtii的细胞色素B_6F复合物的X射线结构的主要差异：TrideCyl-stigmatelin的结合位点
6. Nicotinic acetylcholine receptors that bind alpha-bungarotoxin on neurons. [D] . Pugh, Phyllis Cheri. 1995

机译：与神经元上的α-真菌毒素结合的烟碱型乙酰胆碱受体。
7. Neuronal acetylcholine receptors in Drosophila: the ARD protein is a component of a high-affinity alpha-bungarotoxin binding complex. [O] . P Schloss, I Hermans-Borgmeyer, H Betz, 1988

机译：果蝇中的神经元乙酰胆碱受体：ARD蛋白是高亲和力的α-真菌毒素结合复合物的组成部分。
8. The binding site of acetylcholine receptor as visualized in the X-ray structure of a complex between alpha-bungarotoxin and a mimotope peptide [O] . Harel, M., Kasher, R., Nicolas, A., 2001

机译：乙酰胆碱受体的结合位点在α-邦加毒素和模拟表位肽之间的复合物的X射线结构中可见
9. Spatial Relationships between Drug Binding Sites on the Surface of the Acetylcholine Receptor: Preparation and Interaction of Fluorescent Alpha-Toxins and Decidium with the Acetylcholine Receptor [R] . Johnson, D. A. 1985

机译：乙酰胆碱受体表面药物结合位点的空间关系：荧光α-毒素和蜕膜与乙酰胆碱受体的制备及相互作用

The binding site of acetylcholine receptor as visualized in the X-Ray structure of a complex between alpha-bungarotoxin and a mimotope peptide.

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