AVPR2 Membrane Protein Introduction

Introduction of AVPR2

The AVPR2 is a member of the 7 membrane domain family of G protein-coupled receptors (GPCRs) and is a protein that acts receptor for vasopressin. The activity of the AVPR2 receptor is mediated by the G_s type of G proteins, which stimulates adenylate cyclase. It activates the G_s protein via its third intracellular loop i3 and part of its proximal C-terminal region to produce its renal antidiuretic effect. AVPR2 is predominantly expressed on the basolateral membrane of the distal convoluted tubule and collecting ducts of the kidney.

Basic Information of AVPR2
Protein Name	Vasopressin V2 receptor
Gene Name	AVPR2
Aliases	AVPR V2, Antidiuretic hormone receptor, VR2 Renal-type arginine vasopressin receptor
Organism	Homo sapiens (Human)
UniProt ID	P30518
Transmembrane Times	7
Length (aa)	371
Sequence	MLMASTTSAVPGHPSLPSLPSNSSQERPLDTRDPLLARAELALLSIVFVAVALSNGLVLA ALARRGRRGHWAPIHVFIGHLCLADLAVALFQVLPQLAWKATDRFRGPDALCRAVKYLQM VGMYASSYMILAMTLDRHRAICRPMLAYRHGSGAHWNRPVLVAWAFSLLLSLPQLFIFAQ RNVEGGSGVTDCWACFAEPWGRRTYVTWIALMVFVAPTLGIAACQVLIFREIHASLVPGP SERPGGRRRGRRTGSPGEGAHVSAAVAKTVRMTLVIVVVYVLCWAPFFLVQLWAAWDPEA PLEGAPFVLLMLLASLNSCTNPWIYASFSSSVSSELRSLLCCARGRTPPSLGPQDESCTT ASSSLAKDTSS

Functions of AVPR2 Membrane Protein

The major role of this receptor is the regulation of the body water homeostasis. Binding of antidiuretic hormone arginine-vasopressin (AVP) to this receptor stimulates the recruitment of selective water channels (aquaporins), which allow reabsorption of renal tubular water and concentration of urine. The AVPR2 is involved in several pathophysiological conditions. For instance, mutations in the human AVPR2 result in X-linked nephrogenic diabetes insipidus (NDI). Moreover, this receptor is also involved in states of excessive reabsorption of renal water, which is shared by several diseases, such as liver cirrhosis, congestive heart failure, and the syndrome of inappropriate release of AVP (SIADH).

AVPR2 Membrane Protein-Introduction Fig.1 Vasopressin-2 receptor with its seven transmembrane helices. (Zietse, 2009)

Applications of AVPR2 Membrane Protein in Literature

1. Shuang., et al. Synthesis and biological evaluation of novel phenothiazine derivatives as non-peptide arginine vasopressin V2 receptor antagonists. Chinese Chemical Letters. 2015, 26(5): 627-630.

This study synthesized a series of novel phenothiazine derivatives and evaluated their arginine vasopressin receptor antagonist activity. Several compounds with promising binding affinity to V2 receptors were recognized as potent AVP V2 antagonist candidates.

2. El B R., et al. Antagonism of vasopressin V2 receptor improves albuminuria at the early stage of diabetic nephropathy in a mouse model of type 2 diabetes. Journal of Diabetes & Its Complications. 2017, 31(6): 929-932. PMID: 28412033

This study investigated the role of the V2 receptor in type 2 diabetes using male obese diabetic db/db mice. The results showed that vasopressin contributed to albuminuria and glomerular hyperfiltration via the V2 receptor.

3. Balázsfi D., et al. Restoration of peripheral V2 receptor vasopressin signaling fails to correct behavioral changes in Brattleboro rats. Psychoneuroendocrinology. 2015, 51(51): 11-23. PMID: 25278460

Using wild-type and vasopressin-deficient male Brattleboro rats, this article investigated whether correction of the peripheral symptoms of congenital absence of vasopressin corrected the behavioral alterations. The results showed that vasopressin was involved in the development of affective disorders through central mechanisms.

4. Erdélyi L S., et al. Mutation in the V2 vasopressin receptor gene, AVPR2, causes nephrogenic syndrome of inappropriate diuresis. Kidney International. 2015, 88(5): 1070-1078. PMID: 26131744

This study investigated the I130N mutation in the V2 receptor gene causing a nephrogenic syndrome of inappropriate antidiuresis (NSIAD).

5. Bolignano D., et al. Aquaretic inhibits renal cancer proliferation: Role of vasopressin receptor-2 (V2-R). Urol Oncol. 2010, 28(6): 642-647. PMID: 19217806

Using a culture model of CAKI-2 and A498 cancer cells, this study aimed to verify if renal carcinoma cells also express V2-R and whether receptor activation modulates their proliferation.

AVPR2 Preparation Options

Considering the importance of the AVPR2 in health and disease and the difficulty to study GPCRs in vivo, Creative Biolabs now offers various robust reconstitution forms for the structural and functional studies of this membrane protein in vitro. Aided by our versatile Magic™ Membrane Protein platform, we can always provide you with a suitable format for a given protein. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-AVPR2 antibody development services.

Creative Biolabs’ mission is to provide our customers with the best quality membrane targets for their brilliant studies and discovery projects. To learn more about our services please contact us directly or send us an inquiry.

Reference

Zietse, R., et al. (2009). Current and future treatment options in SIADH. Ndt Plus. 2(Suppl 3), iii12-iii19.

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