a Laboratoire de physique et biophysique , Université de Bordeaux Victor Segalen, GESVAB EA 3675, ISVV , 146 rue Léo Saignat, Bordeaux cedex , 33076 , France .
J Biomol Struct Dyn. 2013 Dec;31(12):1381-92. doi: 10.1080/07391102.2012.736776. Epub 2012 Nov 12.
Neurotensin (NT) is a tridecapeptide hormone in the periphery and neurotransmitter in the brain that principally activates three receptor subtypes, named NTS1, NTS2, and NTS3. Since little is known about its structure in the presence of its principal receptor NTS1, we determined it using the key domain of the receptor, i.e. the third extracellular loop. We conclude the following: (i) for the receptor fragment, NT binding modifies its central part, underlying the great flexibility and adaptability of this region; (ii) for bound NT, the extended conformation of its C-terminus is confirmed for the first time in experimental conditions and in the presence of a part of the receptor; and (iii) despite some substitutions, the human receptor residues that are involved in the interaction with NT could be similar to those of the rat receptor which play an important role in NT binding.
神经降压素（NT）是一种在周围神经系统中起激素作用，在大脑中起神经递质作用的十三肽。它主要激活三种受体亚型，分别命名为 NTS1、NTS2 和 NTS3。由于对其主要受体 NTS1 存在情况下的结构知之甚少，我们使用受体的关键结构域，即第三细胞外环，对其进行了测定。我们得出以下结论：（i）对于受体片段，NT 结合会改变其中心部分，这表明该区域具有很大的灵活性和适应性；（ii）对于结合的 NT，其 C 末端的伸展构象首次在实验条件下并在部分受体存在的情况下得到证实；（iii）尽管存在一些取代，与 NT 相互作用的人类受体残基可能与在 NT 结合中起重要作用的大鼠受体的残基相似。
