Schloss P, Hermans-Borgmeyer I, Betz H, Gundelfinger E D
ZMBH, Universität Heidelberg, FRG.
EMBO J. 1988 Sep;7(9):2889-94. doi: 10.1002/j.1460-2075.1988.tb03146.x.
The ard gene of Drosophila melanogaster encodes a structural homologue of vertebrate nicotinic acetylcholine receptors (AChR) and is expressed exclusively in nervous tissue. To study the nature of the ARD protein, antibodies were raised against fusion constructs containing two regions of this polypeptide. One segment is putatively extracellular (amino acids 65-212), the other domain is exposed to the cytoplasm (amino acids 305-444). The ARD antisera obtained served to investigate the physical relationship between the ARD protein and alpha-bungarotoxin (alpha-Btx) binding sites occurring in Drosophila. Two different high-affinity binding sites for [125I]alpha-Btx, a highly potent antagonist of vertebrate muscle AChR, were detected in fly head membranes. Equilibrium binding and kinetic studies revealed Kd values of approximately 0.1 nM (site 1) and approximately 4 nM (site 2). The estimated maximal binding (Bmax) was approximately 240 and 1080 fmol/mg protein respectively. Both sites exhibited a nicotinic-cholinergic pharmacology. Immunoprecipitation experiments with the ARD antisera indicated that the ARD protein is associated with the [125I]alpha-Btx binding site 1 only. These data support the previously postulated hypothesis that the ARD protein is part of an alpha-Btx binding neuronal AChR of Drosophila. Furthermore, they indicate heterogeneity in nicotinic-cholinergic binding sites in the insect nervous system.
黑腹果蝇的ard基因编码脊椎动物烟碱型乙酰胆碱受体(AChR)的结构同源物,且仅在神经组织中表达。为了研究ARD蛋白的性质,制备了针对包含该多肽两个区域的融合构建体的抗体。一个片段可能位于细胞外(氨基酸65 - 212),另一个结构域暴露于细胞质(氨基酸305 - 444)。所获得的ARD抗血清用于研究ARD蛋白与果蝇中出现的α-银环蛇毒素(α-Btx)结合位点之间的物理关系。在蝇头膜中检测到了[125I]α-Btx(脊椎动物肌肉AChR的一种高效拮抗剂)的两种不同的高亲和力结合位点。平衡结合和动力学研究揭示,位点1的Kd值约为0.1 nM,位点2的Kd值约为4 nM。估计的最大结合量(Bmax)分别约为240和1080 fmol/mg蛋白。两个位点均表现出烟碱型胆碱能药理学特性。用ARD抗血清进行的免疫沉淀实验表明,ARD蛋白仅与[125I]α-Btx结合位点1相关。这些数据支持了先前提出的假说,即ARD蛋白是果蝇α-Btx结合神经元AChR的一部分。此外,它们表明昆虫神经系统中烟碱型胆碱能结合位点存在异质性。