APLNR Membrane Protein Introduction

Introduction of APLNR

APLNR (also known as APLNR and APJ) was first discovered in 1993 as an angiotensin receptor-like receptor due to its sequence similarity with the angiotensin AT1 receptor. However, it does not bind angiotensin II and in 1998 the apelin (APLN) was identified as the endogenous ligand of APLNR. APLN is a peptide hormone and it modulates various signaling pathways in different cell types upon binding to APLNR. APLNR consists of 380 amino acids and it belongs to the class A G-protein-coupled receptor (GPCR) family. APLNR is widely expressed in the human organism including the central nervous system (CNS), heart, lung, kidney, pancreas, and placenta.

Functions of APLNR Membrane Protein

The APLN/APLNR system is found to be involved in a lot of physiological processes. Firstly, it is notably expressed in hypothalamus where it participates in the regulation of fluid homeostasis, food intake, and glucose metabolism. APLNR stimulation or inhibition in the CNS may have consequences on behavior (memory, food, and water intake) and physiology (neuroprotection, pain, metabolism). Moreover, it is well recognized that apelin signaling is involved in the peripheral regulation of cardiovascular function, playing a critical role in physiological and pathological angiogenesis. Furthermore, the apelin-APJ system has been extensively described as a major factor involved in energy metabolism. As a result, the dysregulation of apelin signaling is associated with the development and progression of different diseases including diabetes, obesity, cardiovascular diseases, and cancer. Given the broad range of pathophysiological actions of APLN/APLNR system, APLNR represents a promising target for pharmacological agent design.

Fig.1 Metabolic effects of APLN and its main signaling targets. (Bertrand, 2015)

Applications of APLNR Membrane Protein in Literature

1. Sekerci R., et al. Apelin/APJ expression in the heart and kidneys of hypertensive rats. Acta Histochemica. 2018, 120(3). PubMed ID: 29395316
   
   

   This article measured the expression of apelin and apelin receptor in the heart and kidney tissue of hypertensive rats. The results were thought to be used for experimental or clinical studies related to hypertension and apelin.

2. Różycka M., et al. Apelin and apelin receptor at different stages of corpus luteum development and effect of apelin on progesterone secretion and 3β-hydroxysteroid dehydrogenase (3β-HSD) in pigs. Animal Reproduction Science. 2018, 192:251-260. PubMed ID: 29576467
   
   

   This study investigated the gene expression and immunolocalization of apelin and its receptor in corpora lutea (CL) in pigs. The results suggested potential auto/paracrine regulation by apelin in the luteal phase of the estrous cycle and confirmed the involvement of apelin receptor and AMPKα kinase in apelin activity in CL.

3. Hall C., et al. Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growth. Cancer Letters. 2017, 386:179. PubMed ID: 27894959
   
   

   This study studied the apelin receptor in cholangiocarcinoma (CCA) and investigated if inhibition of the apelin/APLNR axis could inhibit CCA growth using an apelin receptor antagonist, ML2221. The conclusion was that inhibition of this system decreases CCA growth.

4. Besserer-Offroy É., et al. The hypotensive effect of activated apelin receptor is correlated with β-arrestin recruitment. Pharmacological research. 2018, 131: 7-16. PubMed ID: 29530600
   
   

   This study investigated the signaling pathways through which apelin exerts its hypotensive action. The results showed that the β-arrestin recruitment potency was involved in the hypotensive efficacy of activated apelin receptor.

5. Rak A., et al. Expression of apelin and apelin receptor (APJ) in porcine ovarian follicles and in vitro effect of apelin on steroidogenesis and proliferation through APJ activation and different signaling pathways. Theriogenology. 2017, 96:126. PubMed ID: 28532828
   
   

   This study investigated the expression of apelin and APJ in ovarian follicles of different sizes from mature pigs. The results suggested that apelin appeared to regulate ovarian follicular functions via APJ activation and different signaling pathways.

APLNR Preparation Options

Investigations of membrane protein structure, function, and drug discovery stem from their solubilization, purification, and reconstitution. Our versatile membrane protein production platform presents multiple reconstitution systems for our clients to obtain their target proteins in functional formats. See Magic™ Membrane Protein Production Service for more information. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-APLNR antibody development services.

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Creative Biolabs pursues to provide reconstituted APLNR proteins that are most suitable for your research goals. Please feel free to contact us for more detailed information.

Reference

1. Bertrand C, et al. (2015). Apelin and energy metabolism. Front Physiol. 6, 115.

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