Abstract |
Selective activation of the NPY2 receptor to suppress appetite provides an approach to obesity management. Selective NPY2 PEGylated peptide agonists are described that consist of a peptide core corresponding to residues 25-36 of PYY and a nonpeptidic moiety at the peptide N-terminus that contributes to in vitro potency and in vivo efficacy and provides a PEGylation site. The lead peptide elicits a dose-dependent reduction of food intake in lean mice and of food intake, body weight, and fat mass in DIO mice.
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Authors | Kevin J Lumb, Lynn B DeCarr, Lucinda F Milardo, Michelle R Mays, Thomas M Buckholz, Stephen E Fisk, Carla M Pellegrino, Astrid A Ortiz, Cathy D Mahle |
Journal | Journal of medicinal chemistry
(J Med Chem)
Vol. 50
Issue 9
Pg. 2264-8
(May 03 2007)
ISSN: 0022-2623 [Print] United States |
PMID | 17425299
(Publication Type: Journal Article)
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Chemical References |
- Anti-Obesity Agents
- Oligopeptides
- Peptide Fragments
- Receptors, Neuropeptide Y
- neuropeptide Y2 receptor
- Peptide YY
- peptide YY (3-36)
- Polyethylene Glycols
- Cyclic AMP
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Topics |
- Animals
- Anti-Obesity Agents
(chemical synthesis, chemistry, pharmacology)
- Body Weight
(drug effects)
- Cyclic AMP
(biosynthesis)
- Eating
(drug effects)
- Humans
- Male
- Mice
- Mice, Inbred C57BL
- Oligopeptides
(chemical synthesis, chemistry, pharmacology)
- Peptide Fragments
(chemistry, pharmacology)
- Peptide YY
(chemistry, pharmacology)
- Polyethylene Glycols
(chemistry)
- Radioligand Assay
- Receptors, Neuropeptide Y
(agonists)
- Structure-Activity Relationship
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