Melanocortin agonists stimulate lipolysis in human adipose tissue explants but not in adipocytes
Open accessAbstract
BACKGROUND: The central melanocortin system is broadly involved in the regulation of mammalian nutrient utilization. However, the function of melanocortin receptors (MCRs) expressed directly in peripheral metabolic tissues is still unclear. The objective of this study was to investigate the lipolytic capacity of MC1-5R in differentiated adipocytes versus intact white adipose tissue. RESULTS: Non-selective MCR agonist α-MSH, MC5R-selective agonist PG-901 and MC4R-selective agonist LY2112688 significantly stimulated lipolysis in intact white adipose tissue, whereas stimulation of MCRs in differentiated adipocytes failed to do so. The lipolytic response of MC5R was decreased in intact human white adipose tissue when co-treating with β-adrenergic antagonist propranolol, suggesting that the effect may be dependent on neuronal innervation via noradrenalin release. CONCLUSION: When developing an anti-obesity therapeutic drug with selective MC4R/MC5R properties, effects on lipolysis in white adipose tissue may be physiologically relevant.
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ACTH, α-MSH and other fragments lacking the C-terminal Arg-Phe sequence may have a life-saving effect in humans and experimental animals in conditions associated with severe tissue hypoxia.
“However, ACTH, α-MSH and other fragments lacking the C-terminal Arg-Phe sequence may also have a life-saving effect in humans and experimental animals in conditions associated with severe tissue hypoxia [2, 67–69].”
From Role of the brain melanocortins in blood pressure regulation (2017) · cites this paper as [68]
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- Authors
- Møller, C. L., Pedersen, S. B., Richelsen, B., Conde-Frieboes, K. W., Raun, K., Grove, K. L., & Wulff, B. S.
- Affiliations
- Novo Nordisk (Denmark) (DK)
- Aarhus University Hospital (DK)
- Oregon Health & Science University (US)
- Corresponding author
- Wulff, Birgitte Schjellerup
- Venue
- BMC Research Notes
- Published
- 2015-10-12
- Volume
- 8
- Issue
- 1
- Pages
- 559-559
- ISSN
- 1756-0500 (ISSN-L)
- PMC
- PMC4604100
- OpenAlex
- W2163062976
- Cited by
- 22
- References
- 58
- Citations by year
- 2026: 1 · 2025: 1 · 2024: 2 · 2023: 1 · 2022: 1 · 2021: 3 · 2020: 4 · 2019: 1 · 2018: 1 · 2017: 5 · 2016: 2
- FWCI
- 1.47
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- cc-by
- Locations
- BMC Research Notes (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Funders
- PO1 (PO1 OD0011092)
- Novo Nordisk A/S
- The Danish Ministry of Higher Education and Science
- Topics
- Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
- Health Sciences › Medicine › Physiology › Adipose Tissue and Metabolism
- Health Sciences › Medicine › Epidemiology › Adipokines, Inflammation, and Metabolic Diseases
- Keywords
- melanocortin agonists, lipolysis, white adipose tissue, adipocytes, melanocortin receptors, MC1R, MC5R, melanocortin-4 receptor, alpha-melanocyte-stimulating hormone, propranolol, norepinephrine, sympathetic innervation, anti-obesity drugs
- MeSH terms
- Fatty Acids, Female, Glycerol, Humans, Lipolysis, Models, Biological, Obesity, Peptides, Cyclic, Synapses, Adipocytes, Subcutaneous Tissue, Receptors, Melanocortin, Adipose Tissue, White, Melanocortins
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