ArticleJournal of molecular endocrinology2015
Functions of DPLIY motif and helix 8 of human melanocortin-3 receptor.
Article in Journal of molecular endocrinology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 24 citations in OpenAlex.
- Neural Melanocortin Receptors in Fish: Insights into Growth Regulation and Aquaculture Advancement.Biomolecules · 2026Review
- Molecular cloning and functional characterization of melanocortin-3 receptor in grass carp (Ctenopharyngodon idella).Fish physiology and biochemistry · 2023Article
- Functional characterization of melanocortin-3 receptor in rainbow trout (Oncorhynchus mykiss).Fish physiology and biochemistry · 2022Article
- Functional Characterization of Melanocortin-3 Receptor in a Hibernating CavefishAnimals : an open access journal from MDPI · 2021Article
- Biased signaling in naturally occurring mutations of G protein-coupled receptors associated with diverse human diseases.Biochimica et biophysica acta. Molecular basis of disease · 2021Review
- Alanine Scanning Mutagenesis of the DRYxxI Motif and Intracellular Loop 2 of Human Melanocortin-4 Receptor.International journal of molecular sciences · 2020Article
- Insights into the Allosteric Mechanism of Setmelanotide (RM-493) as a Potent and First-in-Class Melanocortin-4 Receptor (MC4R) Agonist To Treat Rare Genetic Disorders of Obesity through an in Silico Approach.ACS chemical neuroscience · 2019Article
- Polymorphisms and mutations in the melanocortin-3 receptor and their relation to human obesity.Biochimica et biophysica acta. Molecular basis of disease · 2017Review
- Biased signaling at neural melanocortin receptors in regulation of energy homeostasis.Biochimica et biophysica acta. Molecular basis of disease · 2017Review
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
The melanocortin-3 receptor (MC3R) is a member of the family A G protein-coupled receptors (GPCRs). The MC3R remains the most enigmatic of the melanocortin receptors with regard to its physiological functions, especially its role in energy homeostasis. The N/DPxxY motif and the eighth helix (helix 8) in the carboxyl terminus of GPCRs have been identified to be important for receptor expression, ligand binding, signal transduction and internalization. To gain a better understanding of the structure-function relationship of MC3R, we performed a systematic study of all 20 residues in this domain using alanine-scanning mutagenesis. We showed that although all mutants were expressed normally on the cell surface, eleven residues were important for ligand binding and one was indispensable for downstream cAMP generation. F347A showed constitutive activity in cAMP signaling while all the other mutants had normal basal activities. We studied the signaling capacity of nine mutants in the ERK1/2 signaling pathway. All of these mutants showed normal basal ERK1/2 phosphorylation levels. The pERK1/2 levels of six binding- or signaling-defective mutants were enhanced upon agonist stimulation. The unbalanced cAMP and pERK1/2 signaling pathways suggested the existence of biased signaling in MC3R mutants. In summary, we showed that the DPLIY motif and helix 8 was important for MC3R activation and signal transduction. Our data led to a better understanding of the structure-function relationship of MC3R.
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