Data set describing the in vitro biological activity of JMV2009, a novel silylated neurotensin(8–13) analog

• DOI: 10.1016/j.dib.2020.105884
• Publication Date: 2020-06-20T17:55:44Z
• Authors: Élie Besserer-Offroy; Pascal Tétreault; Rebecca L Brouill...; Adeline René; Alexandre Murza; Roberto Fanelli; Karyn Kirby; Alexandre Parent; Isabelle Dubuc; Nicolas Beaudet; Jérôme Côté; Jean-Michel Longpré; Jean Martinez; Florine Cavelier; Philippe Sarret
• Keywords: Internalization

Neurotensin (NT) is a tridecapeptide displaying interesting antinociceptive properties through its action on receptors, NTS1 and NTS2. Neurotensin-like compounds have been shown to exert better than morphine at equimolar doses. In this article, we characterized the molecular effects of novel neurotensin (8-13) (NT(8-13)) analog containing an unnatural amino acid. This compound, named JMV2009, displays Silaproline in position 10 replacement proline native NT(8-13). We first examined binding affinities NT(8-13) derivative both NTS2 receptor sites by performing competitive displacement iodinated NT purified cell membranes. Then, evaluated ability JMV2009 activate NTS1-related G proteins as well promote recruitment β-arrestins 1 2 using BRET-based cellular assays live cells. next assessed induce p42/p44 MAPK phosphorylation receptors internalization western blot cell-surface ELISA, respectively. Finally, determined vitro plasma stability derivative. article associated with original "Pain relief devoid opioid side following central silylated analog" published European Journal Pharmacology[1]. The reader directed for results interpretation, comments, discussion.