Jurkowski Wiktor, Yazdi Samira, Elofsson Arne
Center for Biomembrane Research, Stockholm Bioinformatics Center, Department of Biochemistry and Biophysics, Science for Life Laboratory, Stockholm University, Stockholm, Sweden.
Mol Membr Biol. 2013 Mar;30(2):206-16. doi: 10.3109/09687688.2012.750384. Epub 2012 Dec 13.
The galanin receptor family comprises of three members, GalR1, GalR2 and GalR3, all belonging to the G-protein-couple receptor superfamily. All three receptors bind the peptide hormone galanin, but show distinctly different binding properties to other molecules and effects on intracellular signaling. To gain insight on the molecular basis of receptor subtype specificity, we have generated a three-dimensional model for each of the galanin receptors based on its homologs in the same family. We found significant differences in the organization of the binding pockets among the three types of receptors, which might be the key for specific molecular recognition of ligands. Through docking of fragments of the galanin peptide and a number of ligands, we investigated the involvement of transmembrane and loop residues in ligand interaction.
甘丙肽受体家族由三个成员组成，即GalR1、GalR2和GalR3，它们均属于G蛋白偶联受体超家族。这三种受体都能结合肽类激素甘丙肽，但对其他分子的结合特性以及对细胞内信号传导的影响却明显不同。为了深入了解受体亚型特异性的分子基础，我们基于同一家族中的同源物为每种甘丙肽受体生成了三维模型。我们发现三种类型的受体在结合口袋的结构组织上存在显著差异，这可能是配体特异性分子识别的关键。通过对接甘丙肽片段和一些配体，我们研究了跨膜和环残基在配体相互作用中的作用。
