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Small lipidated anti-obesity compounds derived from neuromedin U.


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.

SUBMITTER: Micewicz ED 

PROVIDER: S-EPMC4543588 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature

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Small lipidated anti-obesity compounds derived from neuromedin U.

Micewicz Ewa D ED   Bahattab Omar S O OS   Willars Gary B GB   Waring Alan J AJ   Navab Mohamad M   Whitelegge Julian P JP   McBride William H WH   Ruchala Piotr P  

European journal of medicinal chemistry 20150714


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  ...[more]

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