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Neuropeptide Y5 rec...
Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults
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Erondu, Ngozi (author)
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Gantz, Ira (author)
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Musser, Bret (author)
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Suryawanshi, Shailaja (author)
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Mallick, Madhuja (author)
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Addy, Carol (author)
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Cote, Josee (author)
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Bray, George (author)
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Fujioka, Ken (author)
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Bays, Harold (author)
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Hollander, Priscilla (author)
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Sanabria-Bohorquez, Sandra M. (author)
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Eng, WaiSi (author)
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- Långström, Bengt (author)
- Uppsala universitet,Institutionen för biokemi och organisk kemi
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Hargreaves, Richard J. (author)
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Burns, H. Donald (author)
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Kanatani, Akio (author)
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Fukami, Takehiro (author)
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MacNeil, Douglas J. (author)
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Gottesdiener, Keith M. (author)
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Amatruda, John M. (author)
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Kaufman, Keith D. (author)
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Heymsfield, Steven B. (author)
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(creator_code:org_t)
- Elsevier BV, 2006
- 2006
- English.
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In: Cell Metabolism. - : Elsevier BV. - 1550-4131. ; 4:4, s. 275-282
- Related links:
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http://www.cell.com/...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- Neuropeptide Y (NPY) is a potent orexigenic neuropeptide, and antagonism of NPY Y1 and NPY Y5 receptors (NPYxR) is considered a potentially important anti-obesity drug target. We tested the hypothesis that blockade of the NPY5R will lead to weight loss in humans using MIK-0557, a potent, highly selective, orally active NPY5R antagonist. The initial series of experiments reported herein, including a multiple-dose positron-emission tomography study and a 12 week proof-of concept/dose-ranging study, suggested an optimal MK-0557 dose of 1 mg/day. The hypothesis was then tested in a 52 week, multicenter, randomized, double-blind, placebo-controlled trial involving 1661 overweight and obese patients. Although statistically significant at 52 weeks, the magnitude of induced weight loss was not clinically meaningful. These observations provide the first clinical insight into the human NPY-energy homeostatic pathway and suggest that solely targeting the NPY5R in future drug development programs is unlikely to produce therapeutic efficacy.
Subject headings
- NATURVETENSKAP -- Biologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences (hsv//eng)
Keyword
- Biology
- Biologi
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Erondu, Ngozi
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Gantz, Ira
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Musser, Bret
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Suryawanshi, Sha ...
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Mallick, Madhuja
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Addy, Carol
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show more...
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Cote, Josee
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Bray, George
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Fujioka, Ken
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Bays, Harold
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Hollander, Prisc ...
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Sanabria-Bohorqu ...
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Eng, WaiSi
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Långström, Bengt
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Hargreaves, Rich ...
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Burns, H. Donald
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Kanatani, Akio
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Fukami, Takehiro
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MacNeil, Douglas ...
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Gottesdiener, Ke ...
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Amatruda, John M ...
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Kaufman, Keith D ...
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Heymsfield, Stev ...
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- About the subject
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Biological Scien ...
- Articles in the publication
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Cell Metabolism
- By the university
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Uppsala University