Small lipidated anti-obesity compounds derived from neuromedin U
journal contributionposted on 13.01.2016, 09:53 by E. D. Micewicz, O. S. Bahattab, Gary Brian Willars, A. J. Waring, M. Navab, J. P. Whitelegge, W. H. McBride, P. Ruchala
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.