Small lipidated anti-obesity compounds derived from neuromedin U

源自神经调节素 U 的小脂质化抗肥胖化合物

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作者:Ewa D Micewicz, Omar S O Bahattab, Gary B Willars, Alan J Waring, Mohamad Navab, Julian P Whitelegge, William H McBride, Piotr Ruchala

Abstract

A small library of truncated/lipid-conjugated neuromedin U (NmU) analogs was synthesized and tested in vitro using an intracellular calcium signaling assay. The selected, most active analogs were then tested in vivo, and showed potent anorexigenic effects in a diet-induced obese (DIO) mouse model. The most promising compound, NM4-C16 was effective in a once-weekly-dose regimen. Collectively, our findings suggest that short, lipidated analogs of NmU are suitable leads for the development of novel anti-obesity therapeutics.

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