The DOI matches its Crossref record; 33 of the 33 references it cites were found in a registry or an index.
The melanocortin-4 receptor as target for obesity treatment: a systematic review of emerging pharmacological therapeutic options
Abstract
Obesity is one of the greatest public health challenges of the 21st century. Obesity is currently responsible for ∼0.7-2.8% of a country's health costs worldwide. Treatment is often not effective because weight regulation is complex. Appetite and energy control are regulated in the brain. Melanocortin-4 receptor (MC4R) has a central role in this regulation. MC4R defects lead to a severe clinical phenotype with lack of satiety and early-onset severe obesity. Preclinical research has been carried out to understand the mechanism of MC4R regulation and possible effectors. The objective of this study is to systematically review the literature for emerging pharmacological obesity treatment options. A systematic literature search was performed in PubMed and Embase for articles published until June 2012. The search resulted in 664 papers matching the search terms, of which 15 papers remained after elimination, based on the specific inclusion and exclusion criteria. In these 15 papers, different MC4R agonists were studied in vivo in animal and human studies. Almost all studies are in the preclinical phase. There are currently no effective clinical treatments for MC4R-deficient obese patients, although MC4R agonists are being developed and are entering phase I and II trials.
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“Substantial efforts have been made to develop small molecules as agonists of the MC4 receptor with some limited success (61).”
From ACTH Antagonists (2016) · cites this paper as [61]
Citations
Cites
Interacting Appetite-Regulating Pathways in the Hypothalamic Regulation of Body Weight
Kalra, S. P., Dube, M. G., Pu, S., Xu, B., Horváth, T. L., & Kalra, P. S. (1999) · Endocrine Reviews · doi:10.1210/edrv.20.1.0357 · Cited by 1,564
The economic burden of obesity worldwide: a systematic review of the direct costs of obesity
Withrow, D., & Alter, D. A. (2011) · Obesity Reviews · doi:10.1111/j.1467-789x.2009.00712.x · Cited by 1,083
Multicenter, placebo-controlled trial of lorcaserin for weight management.
Smith, S. R., Weissman, N. J., Anderson, C. M., Sanchez, M., Chuang, E., Stubbe, S., Bays, H., & Shanahan, W. R. (2010) · New England Journal of Medicine · doi:10.1056/nejmoa0909809 · Cited by 911
The FDA's Assessment of Two Drugs for Chronic Weight Management
Colman, E., Golden, J., Roberts, M., Egan, A., Weaver, J., & Rosebraugh, C. (2012) · New England Journal of Medicine · doi:10.1056/nejmp1211277 · Cited by 342
Gene-environment interaction and obesity
Qi, L., & Cho, Y. A. (2008) · Nutrition Reviews · doi:10.1111/j.1753-4887.2008.00128.x · Cited by 280
Social Position, Psychological Stress, and Obesity: A Systematic Review
Moore, C. J., & Cunningham, S. A. (2012) · Journal of the Academy of Nutrition and Dietetics · doi:10.1016/j.jand.2011.12.001 · Cited by 242
Kievit, P., Halem, H., Marks, D. L., Dong, J. Z., Glavas, M. M., Sinnayah, P., Pranger, L., Cowley, M. A., Grove, K. L., & Culler, M. D. (2013) · Diabetes · doi:10.2337/db12-0598 · Cited by 231
Targeting melanocortin receptors as potential novel therapeutics
Getting, S. J. (2006) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2005.06.022 · Cited by 194
Benoit, S. C., Schwartz, M. W., Lachey, J. L., Hagan, M. M., Rushing, P. A., Blake, K. A., Yagaloff, K. A., Kurylko, G., Franco, L., Danhoo, W., et al. (2000) · Journal of Neuroscience · doi:10.1523/jneurosci.20-09-03442.2000 · Cited by 178
Ward, K. R., Bardgett, J. F., Wolfgang, L., & Stocker, S. D. (2011) · Hypertension · doi:10.1161/hypertensionaha.110.160671 · Cited by 118
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Research works printed but not linked: 1
- Raun K, Conde-Frieboes KW, Sensfuss U, Wulff BS . A long acting, selective MC4 receptor agonist effectively reduces appetite and bodyweight in diet induced obese rats. Obes Rev 2011; 12: 279.
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Melanocortin-4 receptor–regulated energy homeostasis
Krashes, M. J., Lowell, B. B., & Garfield, A. S. (2016) · Nature Neuroscience · doi:10.1038/nn.4202 · Cited by 372
Evaluation of a melanocortin-4 receptor (MC4R) agonist (Setmelanotide) in MC4R deficiency
Collet, T.-H., Dubern, B., Mokrosinski, J., Connors, H., Keogh, J. M., Mendes de Oliveira, E., Henning, E., Poitou-Bernert, C., Oppert, J.-M., Tounian, P., et al. (2017) · Molecular Metabolism · doi:10.1016/j.molmet.2017.06.015 · Cited by 302
Gut-Brain Cross-Talk in Metabolic Control
Clemmensen, C., Müller, T. D., Woods, S. C., Berthoud, H., Seeley, R. J., & Tschöp, M. H. (2017) · Cell · doi:10.1016/j.cell.2017.01.025 · Cited by 309
Zaykov, A. N., Mayer, J. P., & DiMarchi, R. D. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2015.36 · Cited by 294
Rare Genetic Forms of Obesity: Clinical Approach and Current Treatments in 2016
Huvenne, H., Dubern, B., Clément, K., & Poitou, C. (2016) · Obesity Facts · doi:10.1159/000445061 · Cited by 302
Metadata
- Authors
- Fani, L., Bak, S., Delhanty, P., van Rossum, E. F. C., & van den Akker, E. L. T.
- Affiliations
- Erasmus MC (NL)
- ORCID
- Venue
- International Journal of Obesity
- Published
- 2013-06-18
- Volume
- 38
- Issue
- 2
- Pages
- 163-169
- ISSN
- 0307-0565 (ISSN-L)
- 1476-5497
- OpenAlex
- W2019132602
- Cited by
- 121
- References
- 33
- Citations by year
- 2025: 4 · 2024: 4 · 2023: 20 · 2022: 15 · 2021: 6 · 2020: 13 · 2019: 9 · 2018: 6 · 2017: 7 · 2016: 12 · 2015: 16 · 2014: 8 · 2013: 1
- FWCI
- 1.49
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Journal of Obesity (publishedVersion)
- PubMed (publishedVersion)
- EUR Research Repository (Erasmus University Rotterdam) (publishedVersion)
- EUR Research Repository (Erasmus University Rotterdam) (submittedVersion)
- Topics
- Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
- Health Sciences › Medicine › Pharmacology (medical) › Pharmacology and Obesity Treatment
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Adipokines, Inflammation, and Metabolic Diseases
- Keywords
- melanocortin-4 receptor, obesity treatment, MC4R agonist, appetite regulation, energy homeostasis, satiety, body weight regulation, pharmacotherapy
- MeSH terms
- Acetamides, alpha-MSH, Animals, Appetite Regulation, Energy Intake, Energy Metabolism, Gene Frequency, Genotype, Humans, Obesity, Peptides, Cyclic, Phenotype, Pyrrolidines, Receptors, Cell Surface, Spiro Compounds, Body Mass Index, Anti-Obesity Agents, Receptor, Melanocortin, Type 4
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