2015 EJMC pre-pub.pdf (1.47 MB)
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Small lipidated anti-obesity compounds derived from neuromedin U

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journal contribution
posted 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.

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)

issn

0223-5234

eissn

1768-3254

Acceptance date

09/07/2015

Copyright date

2015

Available date

14/07/2017

Publisher version

http://www.sciencedirect.com/science/article/pii/S0223523415301525

Notes

The file associated with this record is under a 24-month embargo from publication in accordance with the publisher's self-archiving policy. The full text may be available through the publisher links provided above.

Language

en