Small lipidated anti-obesity compounds derived from neuromedin U

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Abstract

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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Micewicz, E. D., Bahattab, O. S. O., Willars, G. B., Waring, A. J., Navab, M., Whitelegge, J. P., … Ruchala, P. (2015). Small lipidated anti-obesity compounds derived from neuromedin U. European Journal of Medicinal Chemistry, 101, 616–626. https://doi.org/10.1016/j.ejmech.2015.07.020

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