Literature DB >> 26204509

Small lipidated anti-obesity compounds derived from neuromedin U.

Ewa D Micewicz1, Omar S O Bahattab2, Gary B Willars2, Alan J Waring3, Mohamad Navab4, Julian P Whitelegge5, William H McBride1, Piotr Ruchala6.   

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.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Antiobesity agents; Lipid-conjugated peptides; Neuromedin U receptor agonists; Obesity

Mesh：

Substances：

Year:  2015        PMID： 26204509      PMCID： PMC4543588          DOI： 10.1016/j.ejmech.2015.07.020

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  102 in total

1.  L-4F differentially alters plasma levels of oxidized fatty acids resulting in more anti-inflammatory HDL in mice.

Authors:  Satoshi Imaizumi; Victor Grijalva; Mohamad Navab; Brian J Van Lenten; Alan C Wagner; G M Anantharamiah; Alan M Fogelman; Srinivasa T Reddy
Journal:  Drug Metab Lett       Date:  2010-08

2.  Distribution and characterisation of neuromedin U-like immunoreactivity in rat brain and intestine and in guinea pig intestine.

Authors:  S J Augood; J R Keast; P C Emson
Journal:  Regul Pept       Date:  1988-04

3.  Transgenic overexpression of neuromedin U promotes leanness and hypophagia in mice.

Authors:  T J Kowalski; B D Spar; L Markowitz; M Maguire; A Golovko; S Yang; C Farley; J A Cook; G Tetzloff; L Hoos; R A Del Vecchio; T M Kazdoba; M F McCool; J J Hwa; L A Hyde; H Davis; G Vassileva; J A Hedrick; E L Gustafson
Journal:  J Endocrinol       Date:  2005-04       Impact factor: 4.286

4.  Neuromedin U is regulated by the metastasis suppressor RhoGDI2 and is a novel promoter of tumor formation, lung metastasis and cancer cachexia.

Authors:  Y Wu; K McRoberts; S S Berr; H F Frierson; M Conaway; D Theodorescu
Journal:  Oncogene       Date:  2006-07-31       Impact factor: 9.867

5.  Minihepcidins prevent iron overload in a hepcidin-deficient mouse model of severe hemochromatosis.

Authors:  Emilio Ramos; Piotr Ruchala; Julia B Goodnough; Léon Kautz; Gloria C Preza; Elizabeta Nemeth; Tomas Ganz
Journal:  Blood       Date:  2012-09-18       Impact factor: 22.113

6.  Identification of receptors for neuromedin U and its role in feeding.

Authors:  A D Howard; R Wang; S S Pong; T N Mellin; A Strack; X M Guan; Z Zeng; D L Williams; S D Feighner; C N Nunes; B Murphy; J N Stair; H Yu; Q Jiang; M K Clements; C P Tan; K K McKee; D L Hreniuk; T P McDonald; K R Lynch; J F Evans; C P Austin; C T Caskey; L H Van der Ploeg; Q Liu
Journal:  Nature       Date:  2000-07-06       Impact factor: 49.962

7.  Signaling and ligand binding by recombinant neuromedin U receptors: evidence for dual coupling to Galphaq/11 and Galphai and an irreversible ligand-receptor interaction.

Authors:  Paul J Brighton; Philip G Szekeres; Alan Wise; Gary B Willars
Journal:  Mol Pharmacol       Date:  2004-08-26       Impact factor: 4.436

8.  Neuromedin U causes biphasic cardiovascular effects and impairs baroreflex function in rostral ventrolateral medulla of spontaneously hypertensive rat.

Authors:  Ahmed A Rahman; Israt Z Shahid; Paul M Pilowsky
Journal:  Peptides       Date:  2013-03-25       Impact factor: 3.750

9.  Structure-activity relationships of rat neuromedin U for smooth muscle contraction.

Authors:  N Sakura; S Ohta; Y Uchida; K Kurosawa; K Okimura; T Hashimoto
Journal:  Chem Pharm Bull (Tokyo)       Date:  1991-08       Impact factor: 1.645

Review 10.  Neuromedin U and its receptors: structure, function, and physiological roles.

Authors:  Paul J Brighton; Philip G Szekeres; Gary B Willars
Journal:  Pharmacol Rev       Date:  2004-06       Impact factor: 25.468
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  4 in total

1.  Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists.

Authors:  An De Prins; Charlotte Martin; Yannick Van Wanseele; Csaba Tömböly; Dirk Tourwé; Vicky Caveliers; Birgitte Holst; Ann Van Eeckhaut; Mette M Rosenkilde; Ilse Smolders; Steven Ballet
Journal:  ACS Med Chem Lett       Date:  2018-04-23       Impact factor: 4.345

2.  Effects of peripheral administration of a Neuromedin U receptor 2-selective agonist on food intake and body weight in obese mice.

Authors:  T Kaisho; H Nagai; T Asakawa; N Suzuki; H Fujita; K Matsumiya; N Nishizawa; Y Kanematsu-Yamaki; K Dote; J-I Sakamoto; T Asami; S Takekawa
Journal:  Int J Obes (Lond)       Date:  2017-07-31       Impact factor: 5.095

Review 3.  Exploring Molecular Insights of Cereal Peptidic Antioxidants in Metabolic Syndrome Prevention.

Authors:  Fred Kwame Ofosu; Dylis-Judith Fafa Mensah; Eric Banan-Mwine Daliri; Deog-Hwan Oh
Journal:  Antioxidants (Basel)       Date:  2021-03-26

Review 4.  Insects as a New Complex Model in Hormonal Basis of Obesity.

Authors:  Karolina Walkowiak-Nowicka; Szymon Chowański; Arkadiusz Urbański; Paweł Marciniak
Journal:  Int J Mol Sci       Date:  2021-10-14       Impact factor: 5.923
  4 in total

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