MC5R Membrane Protein Introduction

Introduction of MC5R

MC5R, a 325-amino acid protein, is a 7-transmembrane receptor in human belonging to the G-protein coupled receptor families involved in the regulation of thrombotic response. This protein is encoded by the MC5R gene that located on chromosome 18 in the human genome. The receptors for MC peptides belong to the GPCR superfamily, and are classified into five subtypes: MC1R, MC2R, MC3R, MC4R, and MC5R. MC1R is a classical α-MSH receptor, and MC2R is a classical ACTH receptor. MC5R is present in human sebaceous glands and rat preputial cells.

Function of MC5R Membrane Protein

Similar to other GPCRs, the MCRs are the smallest known GPCRs and have many features, containing potential N-glycosylation sites in their N-terminal domains, recognition sites for PKA and PKC phosphorylation, and conserved cysteine residues in their C-terminal ends. MCR-1 functions as the effector for melanocortin action in the skin in the periphery. MCR-2, found in the adrenal glands, is the adrenocorticotropin receptor. Additionally, MCR-5 expressed in muscle may mediate thermoregulation. MCRs play an important role in the mediation of lipolysis in intact human white adipose tissue. When co-treating with β-adrenergic antagonist propranolol, the lipolytic response of MC5R shows decreased in intact human white adipose tissue and indicates that the effect may be dependent on neuronal innervation via noradrenalin release. The effects on lipolysis in white adipose tissue may be physiologically relevant in the progress of developing an anti-obesity therapeutic drug with selective MC4R/MC5R properties.

Fig.1 MCR mediates lipolysis in intact human white adipose tissue. (Møller, 2015)

Application of MC5R Membrane Protein in Literature

1. Matsuda N., et al. Left-right pigmentation pattern of Japanese flounder corresponds to expression levels of melanocortin receptors (MC1R and MC5R), but not to agouti signaling protein 1 (ASIP1) expression. Gen Comp Endocrinol. 2018, 492: 387-392. PubMed ID: 29574149.
   
   

   This article reports that MC1R and MC5R contribute to pigmentation and hypermelanosis in Japanese flounder.

2. Fleming K.A., et al. Structure-Activity Relationship Studies of a Macrocyclic AGRP-Mimetic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] Yield Potent and Selective Melanocortin-4 Receptor Antagonists and Melanocortin-5 Receptor Inverse Agonists That Increase Food Intake in Mice. ACS Chem Neurosci. 2018, 9(5):1141-1151 PubMed ID: 29363944
   
   

   Authors focus on the role of the melanocortin system in diseases of negative energy balance, which enable to be used in the design of molecular probes to examine the physiological functions of the mMC5R.

3. Møller C.L., et al. Melanocortin agonists stimulate lipolysis in human adipose tissue explants but not in adipocytes. BMC Res Notes. 2015, 8(1): 559. PubMed ID: 26459134
   
   

   This article finds that lipolysis in white adipose tissue may be associated with physiological aspects, when developing an anti-obesity therapeutic drug with selective MC4R/MC5R properties.

4. Yang Y., et al. Molecular characterization of human melanocortin-5 receptor ligand-receptor interaction. Biochemistry. 2013, 52(10): 1737-45. PubMed ID: 23414113
   
   

   This article provides important information about the structural aspects of hMC5R responsible for ligand binding and receptor signaling.

5. Hatta N., et al. Expression, candidate gene, and population studies of the melanocortin 5 receptor. J Invest Dermatol. 2001, 16(4): 564-70. PubMed ID: 11286624
   
   

   This article finds no evidence of a causative role for melanocortin 5 receptor in sebaceous gland dysfunction and the pathophysiologic role of the melanocortin 5 receptor in man requires further study.

MC5R Preparation Options

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Reference

1. Møller C L, et al. (2015). Melanocortin agonists stimulate lipolysis in human adipose tissue explants but not in adipocytes. BMC Res Notes. 8(1), 559.

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