GPR171 Membrane Protein Introduction

Introduction of GPR171

GPR171 is encoded by the GPR171 gene. GPR171 belongs to the G-protein-coupled receptor (GPCR) family which are the most abundant cell surface receptors that can be targeted clinically. Based on sequence homology, GPR171 has been suggested to belong to a particular subfamily of GPRs, named P2Y receptors, which are activated by extracellular nucleotides.

Function of GPR171 Membrane Protein

GPR171 is a hypothalamic G protein-coupled receptor for BigLEN, which is a neuropeptide associated with feeding. The expression of GPR171 makes up BigLEN expression in the hypothalamus, and its activity and level increase in mice lacking BigLEN. At the same time, it will decrease BigLEN signaling and change food intake and metabolism in mice when researchers knock down the hypothalamic GPR171. To date, the BigLEN-GPR171 system is very important to regulate responses associated with feeding and metabolism in mice. Thus, GPR171 is a potential target for developing anti-obesity drugs. Moreover, GPR171 is putatively related to the P2Y family of purinergic receptors (P2YRs) for extracellular nucleotides, a group of mediators found to regulate hematopoietic progenitor cells (HPCs). GPR171 can also negatively regulate myeloid differentiation in murine hematopoietic progenitors, its expression is suppressed upon myeloid differentiation which is opposed to other members of the family highly expressed in granulocytes and monocytes.

Fig.1 G-protein-coupled receptor mechanism.

Application of GPR171 Membrane Protein in Literature

1. Bobeck E.N., et al. The BigLEN-GPR171 Peptide Receptor System within the Basolateral Amygdala Regulates Anxiety-Like Behavior and Contextual Fear Conditioning. Neuropsychopharmacology Official Publication of the American College of Neuropsychopharmacology. 2017, 42(13), 2527. PubMed ID: 28425495
   
   

   The results of this article indicate that the BigLEN-GPR171 system plays an important role in the pathology of anxiety and other mood disorders and could be a novel target to develop therapeutics to treat psychiatric disorders.

2. Wardman J.H., et al. Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake. Science Signaling. 2016, 9(430), ra55. PubMed ID: 27245612
   
   

   Authors in this article identify MS0015203 as an agonist of GPR171 and demonstrated the selectivity of MS0015203 for GPR171 by testing the binding of this compound to 80 other membrane proteins, including family A GPCRs. They also revealed that MS0015203 is a useful tool to probe the pharmacological and functional properties of GPR171 and that ligands targeting GPR171 may eventually lead to therapeutics for food-related disorders.

3. Dho S.H., et al. GPR171 expression enhances proliferation and metastasis of lung cancer cells. Oncotarget. 2016, 7(7):7856-7865. PubMed ID: 26760963
   
   

   This article reveals that inhibition of GPR171 synergistically enhanced the tumoricidal activity of an epidermal growth factor receptor (EGFR) inhibitor in lung cancer cells. It also indicates that GPR171 blockade is a promising antineoplastic strategy and provide a preclinical rationale for combined inhibition of GPR171 and EGFR.

4. Rossi., et al. Gpr171, a putative P2Y-like receptor, negatively regulates myeloid differentiation in murine hematopoietic progenitors. Experimental Hematology. 2013, 41(1), 102-112. PubMed ID: 23022127
   
   

   This article indicates that the orphan receptor Gpr171 negatively regulates myeloid differentiation, their phylogenic analyses suggest that Gpr171 may have followed a separate evolutionary pathway as compared to other P2YRs belonging to the same gene cluster.

5. Gomes I., et al. GPR171 is a hypothalamic G protein-coupled receptor for BigLEN, a neuropeptide involved in feeding. Proceedings of the National Academy of Sciences of the United States of America. 2013, 110(40), 16211-16216. PubMed ID: 24043826
   
   

   This article’ s results demonstrate that GPR171 is the BigLEN receptor and that the BigLEN-GPR171 system plays an important role in regulating responses associated with feeding and metabolism in mice.

GPR171 Preparation Options

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