Einsiedel Jürgen, Hübner Harald, Hervet Maud, Härterich Steffen, Koschatzky Susanne, Gmeiner Peter
Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich Alexander University, D-91052 Erlangen, Germany.
Bioorg Med Chem Lett. 2008 Mar 15;18(6):2013-8. doi: 10.1016/j.bmcl.2008.01.110. Epub 2008 Feb 2.
To compare backbone-induced susceptibilities with affinity changes that are caused by side-chain modifications in the respective positions, structure activity relationship studies on a series of NT(8-13) analogues were performed providing valuable insights into the major requirement for neurotensin receptor recognition and activation. The data led us to highly potent NTR1 ligands and the generation of a pharmacophore model that will be helpful for the discovery of therapeutically relevant non-peptidic NTR1 agonists.
为了将主链诱导的敏感性与由相应位置侧链修饰引起的亲和力变化进行比较，我们对一系列NT(8 - 13)类似物进行了构效关系研究，从而为神经降压素受体识别和激活的主要要求提供了有价值的见解。这些数据使我们得到了高效的NTR1配体，并生成了一个药效团模型，这将有助于发现具有治疗相关性的非肽类NTR1激动剂。
