Danho W, Triscari J, Vincent G, Nakajima T, Taylor J, Kaiser E T
Exploratory Research, Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ.
Int J Pept Protein Res. 1988 Dec;32(6):496-505. doi: 10.1111/j.1399-3011.1988.tb01380.x.
Peptide fragments of pNPY corresponding to the C-terminal segments (13-36) and (25-36), the N-terminal segments (1-12) and (1-24), the segments (6-14) and (7-20), which contain a putative beta-turn, and the internal segments (13-24) and (20-30) were synthesized using solid phase methodology. These fragments were assayed for NPY receptor binding activity in the rat hypothalamus membrane preparation, enhancement of food intake in the rat following ivt administration and inhibition of electrically stimulated muscle contraction in the rat vas deferens. Only the C-terminal fragment (13-36) retained some of the activities of pNPY, appearing to act as a weak agonist, having an additive effect with pNPY on the inhibition of muscle contraction and prolonging the duration of action of pNPY in the feeding assay. It also had considerable alpha-helical character, as did pNPY. None of the other peptide fragments had any agonist or antagonist activity. These results suggest that the expression of full biological NPY activity requires both the C- and the N-terminal segments as well as a putative amphiphilic alpha-helical segment (14-31).
使用固相方法合成了与C末端片段（13 - 36）和（25 - 36）、N末端片段（1 - 12）和（1 - 24）、含有假定β-转角的片段（6 - 14）和（7 - 20）以及内部片段（13 - 24）和（20 - 30）相对应的pNPY肽片段。对这些片段进行了大鼠下丘脑膜制备中的NPY受体结合活性测定、静脉内注射后大鼠食物摄入量增加的测定以及大鼠输精管电刺激肌肉收缩抑制的测定。只有C末端片段（13 - 36）保留了一些pNPY的活性，似乎作为一种弱激动剂起作用，在抑制肌肉收缩方面与pNPY具有相加作用，并在进食试验中延长了pNPY的作用持续时间。它也具有相当程度的α-螺旋特征，pNPY也是如此。其他肽片段均无任何激动剂或拮抗剂活性。这些结果表明，完整生物学活性的NPY表达需要C末端和N末端片段以及一个假定的两亲性α-螺旋片段（14 - 31）。
