PRLHR Membrane Protein Introduction

Introduction of PRLHR

Prolactin-releasing peptide receptor (PRLHR) is encoded by PRLHR gene. It belongs to the G-protein-coupled receptor (GPCR) family is the largest family of membrane-bound receptors and also the targets of many drugs. PRLHR is isolated and cloned from bovine hypothalamus using low stringency PCR primers designed against to the highly conserved GPCR transmembrane domains 2 and 6. Prolactin releasing peptide is the only ligand known to have significant affinity for GPR10. Meanwhile, PRLHR is also known as G-protein-coupled receptor 10 (GPR10) and hGR3.

Basic Information of PRLHR
Protein Name	Prolactin-releasing peptide receptor
Gene Name	PRLHR
Aliases	G-protein coupled receptor 10, GPR10, hGR3
Organism	Homo sapiens (Human)
UniProt ID	P49683
Transmembrane Times	7
Length (aa)	370
Sequence	MASSTTRGPRVSDLFSGLPPAVTTPANQSAEASAGNGSVAGADAPAVTPFQSLQLVHQLKGLIV LLYSVVVVVGLVGNCLLVLVIARVRRLHNVTNFLIGNLALSDVLMCTACVPLTLAYAFEPRGWV FGGGLCHLVFFLQPVTVYVSVFTLTTIAVDRYVVLVHPLRRRISLRLSAYAVLAIWALSAVLAL PAAVHTYHVELKPHDVRLCEEFWGSQERQRQLYAWGLLLVTYLLPLLVILLSYVRVSVKLRNRV VPGCVTQSQADWDRARRRRTFCLLVVIVVVFAVCWLPLHVFNLLRDLDPHAIDPYAFGLVQLLC HWLAMSSACYNPFIYAWLHDSFREELRKLLVAWPRKIAPHGQNMTVSVVI

Function of PRLHR Membrane Protein

The activity of PRLHR is mediated by prolactin-releasing peptide because it is identified as a receptor for prolactin-releasing peptide. PRLHR is highly expressed in the pituitary and is involved in the genesis of fibroids. The increased expression of PRLHR in patient’s leiomyoma samples resulting in the activation of AKT and MTOR. The treatment with PrRP-31 peptide to patients’ leiomyoma cells resulting in the increase in PI3K/AKT/MTOR signaling and proliferation compared with the normal myometrial-derived smooth muscle cells. Other reports reveal that PRLHR and other additional factors related to PRLHR have an important role in metabolic disorders. There are also numerous studies suggest that PrRP and PRLHR signaling pathway play a pivotal role in the homeostatic regulation of feeding and energy balance.

PRLHR Membrane Protein Introduction Fig.1 Schematic overview of signaling pathway of PRLHR (Rueda, 2013).

Application of PRLHR Membrane Protein in Literature

Rueda B.R., et al. No REST for fibroids. Proceedings of the National Academy of Sciences. 2013, 110(6):1980-1981. PubMed ID: 22730110

This article reviews the importance of PRLHR in the activation of the PI3K/AKT/MTOR signaling pathway, which suggests that PRLHR might to be a potential drug target for treatment of the proliferation of leiomyomas or cells derived from leiomyomas.
Varghese B.V., et al. Loss of the repressor REST in uterine fibroids promotes aberrant G protein-coupled receptor 10 expression and activates mammalian target of rapamycin pathway. Proceedings of the National Academy of Sciences. 2013, 110(6):2187-2192. PubMed ID: 3284171

This article reports that the interaction between GPR10 and its ligand, prolactin releasing peptide can activate the PI3K-AKT-mTOR pathways and promote the cell proliferation in cultured primary leiomyoma cells.
Wang Y., et al. Identification of the Receptors for Prolactin-Releasing Peptide (PrRP) and Carassius RFamide Peptide (C-RFa) in Chickens. Endocrinology. 2012, 153(4):1861-1874. PubMed ID: 22355069

This article identifies and clones the three PRLHR-like receptors, namely cPRLHR1, cPRLHR2, and cC-RFaR from chicken brain, and reports that they play similar roles in regulating food intake and pituitary functions in vertebrates.
Kuneš J., et al. Prolactin-releasing peptide: a new tool for obesity treatment. J. Endocrinol. 2016, 230(2):R51-R58. PubMed ID: 27418033

Authors in this group apply the PrRP and PrRP receptor knockout obesity mice model to demonstrate that prolactin-releasing peptide (PrRP) is involved in feeding and energy balance regulation. PrRP receptor might be a new target for obesity therapy.
Dodd G.T., et al. Physiological Roles of GPR10 and PrRP Signaling. Frontiers in Endocrinology. 2013, 4:20-29. PubMed ID: 23467899

This article reviews that the current knowledge of the PrRP and GPR10 signaling system and its future perspectives. The development of selective GPR10 agonists/antagonists will provide new treatments for the nervous system.

PRLHR Preparation Options

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Reference

Rueda B R and Davis J S. (2013). No REST for fibroids. Proceedings of the National Academy of Sciences. 110(6):1980-1981.

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