Ohman A, Lycksell P O, Andell S, Langel U, Bartfai T, Gräslund A
Department of Biophysics, Arrhenius Laboratories, Stockholm University, Sweden.
Biochim Biophys Acta. 1995 Jun 14;1236(2):259-65. doi: 10.1016/0005-2736(95)00056-9.
Circular dichroism spectroscopy has been used to study how different solvents stabilize secondary structure in the neuropeptide galanin (rat), two N-terminal fragments of galanin, galanin(1-12) and galanin(1-16), and six other differently charged analogs. Among these analogs, the peptide M40, galanin(1-13)-Pro-Pro-Ala-Leu-Ala-Leu-Ala amide, is a high affinity, receptor subtype specific galanin receptor antagonist. The different solvents include sodium dodecyl sulfate (SDS) micelle solutions, 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) and 1,2-dioleoyl-sn-glycero-3-phosphoglycerol (DOPG) vesicle solutions. 100% 1,1,1,3,3,3-hexafluoro-2-propanol (HFP) and 100% 2,2,2-trifluoroethanol (TFE). DOPC vesicles did not change the structure of the peptides as compared to aqueous solvent. The negatively charged DOPG vesicles and SDS micelles induced similar changes towards alpha-helical structures in all peptides. The HFP and TFE solvents have an even stronger tendency to stabilize alpha-helical conformations in these peptides. Since DOPG vesicles can be considered as a model system for negatively charged biological membranes, the solution structures observed in the presence of DOPG or SDS may be the most relevant for the in vivo situation. Correlations between the binding affinity of the peptides to hippocampal galanin receptors and their observed structures in the DOPG solvent were investigated.
圆二色光谱已被用于研究不同溶剂如何稳定神经肽甘丙肽(大鼠)、甘丙肽的两个N端片段甘丙肽(1 - 12)和甘丙肽(1 - 16)以及其他六种带不同电荷的类似物的二级结构。在这些类似物中,肽M40,即甘丙肽(1 - 13)-脯氨酸-脯氨酸-丙氨酸-亮氨酸-丙氨酸-亮氨酸-丙氨酸酰胺,是一种高亲和力、受体亚型特异性的甘丙肽受体拮抗剂。不同的溶剂包括十二烷基硫酸钠(SDS)胶束溶液、1,2 - 二油酰 - sn - 甘油 - 3 - 磷酸胆碱(DOPC)和1,2 - 二油酰 - sn - 甘油 - 3 - 磷酸甘油(DOPG)囊泡溶液、100% 1,1,1,3,3,3 - 六氟 - 2 - 丙醇(HFP)和100% 2,2,2 - 三氟乙醇(TFE)。与水性溶剂相比,DOPC囊泡不会改变肽的结构。带负电荷的DOPG囊泡和SDS胶束在所有肽中诱导出朝向α - 螺旋结构的类似变化。HFP和TFE溶剂在稳定这些肽的α - 螺旋构象方面具有更强的趋势。由于DOPG囊泡可被视为带负电荷生物膜的模型系统,在DOPG或SDS存在下观察到的溶液结构可能与体内情况最为相关。研究了肽与海马甘丙肽受体的结合亲和力与其在DOPG溶剂中观察到的结构之间的相关性。