Impairment of cocaine-mediated behaviours in mice by clinically relevant Ras-ERK inhibitors.
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ABSTRACT:
SUBMITTER: Papale A
PROVIDER: S-EPMC4996650 | biostudies-literature | 2016 Aug
REPOSITORIES: biostudies-literature
Publications
Impairment of cocaine-mediated behaviours in mice by clinically relevant Ras-ERK inhibitors.
Papale Alessandro A Morella Ilaria Maria IM Indrigo Marzia Tina MT Bernardi Rick Eugene RE Marrone Livia L Marchisella Francesca F Brancale Andrea A Spanagel Rainer R Brambilla Riccardo R Fasano Stefania S
eLife 20160824
Ras-ERK signalling in the brain plays a central role in drug addiction. However, to date, no clinically relevant inhibitor of this cascade has been tested in experimental models of addiction, a necessary step toward clinical trials. We designed two new cell-penetrating peptides - RB1 and RB3 - that penetrate the brain and, in the micromolar range, inhibit phosphorylation of ERK, histone H3 and S6 ribosomal protein in striatal slices. Furthermore, a screening of small therapeutics currently in cl ...[more]
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