Shapiro Iu E, Gorbatiuk V Ia, Kabanov V M, Mazurov A A, Andronati S A, Lobasiuk B A, Golovenko N Ia, Rokachinskaia M G
Bioorg Khim. 1990 Dec;16(12):1607-17.
On the basis of the two-dimensional 1H NMR studies the conformation of melanocyte inhibiting hormone (HCl.Pro-Leu-Gly-NH2, MIF) and its five analogues with p-substituted phenylalanine has been determined. Structure-antidepressant activity relationship (examined by the Porsolt test) of MIF and its analogues has been estimated by means of the multivariate statistical analysis, the vicinal spin coupling constants, which determine phi and chi dihedral angles of the second amino acid and phi and dihedral angle of glycine, being selected as structural parameters. It is shown that a biologically active conformation (10-membered beta-turn II) is realized for the considered peptides.
基于二维¹H NMR研究,已确定黑素细胞抑制激素(HCl.Pro-Leu-Gly-NH₂,MIF)及其五种对-取代苯丙氨酸类似物的构象。通过多变量统计分析估计了MIF及其类似物的结构-抗抑郁活性关系(通过Porsolt试验检测),选择确定第二个氨基酸的φ和χ二面角以及甘氨酸的φ和二面角的邻位自旋偶合常数作为结构参数。结果表明,所考虑的肽实现了生物活性构象(10元β-转角II)。