Eur J Med Chem 2018 Jan 14;144:887-897. Epub 2017 Dec 14.
Research Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel, Pleinlaan 2, 1050, Brussels, Belgium. Electronic address:
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J Pharmacol Exp Ther 2009 Jul 15;330(1):268-75. Epub 2009 Apr 15.
AstraZeneca Pharmaceutical LLP, CNS/Pain HTS Center, 1800 Concord Pike, Wilmington, DE 19850-5437, USA.
Neuromedin U (NMU), through its cognate receptor NMUR2 in the central nervous system, regulates several important physiological functions, including energy balance, stress response, and nociception. By random screening of our corporate compound collection with a ligand binding assay, we discovered (R)-5'-(phenylaminocarbonylamino)spiro[1-azabicyclo[2.2. Read More
Bioorg Med Chem 2012 Aug 9;20(15):4751-9. Epub 2012 Jun 9.
IRBM P. Angeletti, 00040 Pomezia (RM), Italy.
Neuromedin U (NMU) is an endogenous peptide, whose role in the regulation of feeding and energy homeostasis is well documented. Two NMU receptors have been identified: NMUR1, expressed primarily in the periphery, and NMUR2, expressed predominantly in the brain. We recently demonstrated that acute peripheral administration of NMU exerts potent but acute anorectic activity and can improve glucose homeostasis, with both actions mediated by NMUR1. Read More
J Pept Sci 2015 Feb 17;21(2):85-94. Epub 2014 Dec 17.
Gubra ApS, Agern Alle 1, 2970, Hørsholm, Denmark; The Novo Nordisk Foundation Center for Basic Metabolic Research, University of Copenhagen, Blegdamsvej 3B, 2200, Copenhagen N, Denmark.
Neuromedin U (NMU) is a 25 amino acid peptide expressed and secreted in the brain and gastrointestinal tract. Data have shown that peripheral administration of human NMU decreases food intake and body weight and improves glucose tolerance in mice, suggesting that NMU receptors constitute a possible anti-diabetic and anti-obesity drug target. However, the clinical use of native NMU is hampered by a poor pharmacokinetic profile. Read More
Bioorg Med Chem 2017 04 21;25(8):2307-2312. Epub 2017 Feb 21.
Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd., Fujisawa 251-8555, Japan.
Neuromedin U (NMU) is a neuropeptide known to regulate food intake and energy homeostasis that is widely distributed in the gastrointestinal tract, hypothalamus, and pituitary. A short form of NMU, porcine NMU-8 has potent agonist activity for the receptors NMUR1 and NMUR2; however, its short half-life precludes its effective use in vivo. To address this limitation, we designed and synthesized NMU-8 analogs modified by polyethylene glycol (PEG) with a molecular weight of 30kDa (PEG30k) via a variety of linkers (i. Read More