posted on 2016-01-13, 09:53authored byE. 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.
History
Citation
European Journal of Medicinal Chemistry, 2015, 101, pp. 616-626
Author affiliation
/Organisation/COLLEGE OF MEDICINE, BIOLOGICAL SCIENCES AND PSYCHOLOGY/MBSP Non-Medical Departments/Molecular & Cell Biology
Version
AM (Accepted Manuscript)
Published in
European Journal of Medicinal Chemistry
Publisher
Elsevier, French Société de Chimie Thérapeutique (SCT)
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