Design, Synthesis, and Biological Evaluation of the First Radio-Metalated Neurotensin Analogue Targeting Neurotensin Receptor 2.

ABSTRACT: Neurotensin receptor 2 (NTS₂) is a well-known mediator of central opioid-independent analgesia. Seminal studies have highlighted NTS₂ overexpression in a variety of tumors including prostate cancer, pancreas adenocarcinoma, and breast cancer. Herein, we describe the first radiometalated neurotensin analogue targeting NTS₂. JMV 7488 (DOTA-(βAla)₂-Lys-Lys-Pro-(D)Trp-Ile-TMSAla-OH) was prepared using solid-phase peptide synthesis, then purified, radiolabeled with ⁶⁸Ga and ¹¹¹In, and investigated in vitro on HT-29 cells and MCF-7 cells, respectively, and in vivo on HT-29 xenografts. [⁶⁸Ga]Ga-JMV 7488 and [¹¹¹In]In-JMV 7488 were quite hydrophilic (logD_7.4 = -3.1 ± 0.2 and -2.7 ± 0.2,

SUBMITTER: Bodin S 

PROVIDER: S-EPMC9948202 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature