scholarly journals Discovery of Molecular Interactions of the Human Melanocortin-4 Receptor (hMC4R) Asp189 (D189) Amino Acid with the Endogenous G-Protein-Coupled Receptor (GPCR) Antagonist Agouti-Related Protein (AGRP) Provides Insights to AGRP’s Inverse Agonist Pharmacology at the hMC4R

2021 ◽  
Vol 12 (3) ◽  
pp. 542-556
Author(s):  
Mark D. Ericson ◽  
Erica M. Haslach ◽  
Sathya M. Schnell ◽  
Katie T. Freeman ◽  
Zhimin M. Xiang ◽  
...  
Keyword(s):  
Amino Acid ◽  
G Protein ◽  
Molecular Interactions ◽  
Inverse Agonist ◽  
Related Protein ◽  
G Protein Coupled Receptor ◽  
Melanocortin 4 Receptor ◽  
Agouti Related Protein ◽  
G Protein Coupled

scholarly journals Apoptosis Mediated by Activation of the G Protein-Coupled Receptor for Parathyroid Hormone (PTH)/ PTH-Related Protein (PTHrP)

2000 ◽  
Vol 14 (2) ◽  
pp. 241-254 ◽  
Author(s):  
Paul R. Turner ◽  
Suzanne Mefford ◽  
Sylvia Christakos ◽  
Robert A. Nissenson
Keyword(s):  
Parathyroid Hormone ◽  
G Protein ◽  
Related Protein ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals The single pass membrane protein MRAP2 regulates energy homeostasis by promoting primary cilia localization of the G protein-coupled receptor MC4R

2020 ◽  
Author(s):  
Adélaïde Bernard ◽  
Irene Ojeda Naharros ◽  
Florence Bourgain-Guglielmetti ◽  
Jordi Ciprin ◽  
Xinyu Yue ◽  
...  
Keyword(s):  
G Protein ◽  
Energy Homeostasis ◽  
Primary Cilia ◽  
Melanocortin Receptor ◽  
G Protein Coupled Receptor ◽  
Promoting Effect ◽  
Receptor Associated Protein ◽  
Extracellular Signals ◽  
Melanocortin 4 Receptor ◽  
G Protein Coupled

ABSTRACTThe G protein-coupled receptor MC4R (Melanocortin-4 Receptor) and its associated protein MRAP2 (Melanocortin Receptor-Associated Protein 2) are both essential for the regulation of food intake and body weight in humans and mice. MC4R localizes and functions at the neuronal primary cilium, a microtubule-based organelle that senses and relays extracellular signals. Here, we demonstrate that MRAP2 is critical for the ciliary localization and weight-regulating function of MC4R. Our data reveal that GPCR localization to primary cilia can require specific accessory proteins that may not be present in heterologous cell systems. Our findings also demonstrate the essential role of neuronal primary cilia localization of MC4R for adequate control of energy homeostasis and the obesity-promoting effect of genetic disruption of this pathway.

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