Overview
- Peptide CSKSSIDGANRSQR, corresponding to amino acid residues 319-332 of mouse GPR81 (HCAR1) (Accession Q8C131). Intracellular, C-terminus.
Western blot analysis of rat kidney (lanes 1 and 3) and rat liver (lanes 2 and 4) lysates:1, 2. Anti-GPR81/HCAR1 Antibody (#AHR-011), (1:200).
3, 4. Anti-GPR81/HCAR1 Antibody, preincubated with GPR81/HCAR1 Blocking Peptide (#BLP-HR011) (#BLP-HR011).
Western blot analysis of mouse kidney lysate (lanes 1 and 3) and mouse liver membrane (lanes 2 and 4):1, 2. Anti-GPR81/HCAR1 Antibody (#AHR-011), (1:200).
3, 4. Anti-GPR81/HCAR1 Antibody, preincubated with GPR81/HCAR1 Blocking Peptide (#BLP-HR011) (#BLP-HR011).
Expression of HCAR1 in mouse hippocampus.Immunohistochemical staining of perfusion-fixed frozen mouse brain sections with Anti-GPR81/HCAR1 Antibody (#AHR-011), (1:200), followed by goat anti-rabbit-AlexaFluor-488. A. HCAR1 immunoreactivity (green) appears in hippocampal blood vessels (horizontal arrows) and astrocytes (vertical arrows). B. Pre-incubation of the antibody with GPR81/HCAR1 Blocking Peptide (BLP-HR011), suppressed staining. Cell nuclei are stained with DAPI (blue).
Expression of HCAR1 in mouse parietal cortex.Immunohistochemical staining of perfusion-fixed frozen mouse brain sections with Anti-GPR81/HCAR1 Antibody (#AHR-011), (1:200), followed by goat anti-rabbit-AlexaFluor-488. A. HCAR1 immunoreactivity (green) appears in cortical blood vessels (horizontal arrows) and astrocytes (vertical arrows). B. Pre-incubation of the antibody with GPR81/HCAR1 Blocking Peptide (BLP-HR011), suppressed staining. Cell nuclei are stained with DAPI (blue).
- Liu, C. et al. (2009) J. Biol. Chem. 284, 2811.
- Wallenius, K. et al. (2017) JCI Insight 2, e92564.
- Li, G. et al. (2014) PLoS One 9, e93041.
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- Roland, C.L. et al. (2014) Cancer Res. 74, 5301.
- Kuei, C. et al. (2011) Mol. Pharmacol. 80, 848.
GPR81 is an orphan G-protein-coupled receptor that belongs to a family of hydroxy-carboxylic acid (HCA) receptors. Its endogenous ligand is L-lactate, a metabolite produced when glycolysis exceeds the capacity to oxidize pyruvate1,2.
In addition to being a by-product of metabolism, lactate plays a role in insulin signaling, particularly in insulin mediated anti-lipolytic effects. Likewise, GPR81 is mostly expressed in adipose tissues and its activation results in inhibition of lipolysis and reduced hydrolysis of triglycerides to glycerol and fatty acids, suggesting that GPR81 may be an attractive drug discovery target for metabolic disorders4.
Beyond the control of adipocyte lipolysis, GPR81 is also involved in neuronal signaling, regulation of blood flow to the retina. The receptor is overexpressed in several cancer types where it appears to play a role in the adaptation to the ischemic tumor microenvironment5.
GPR81, like all other G protein coupled receptors, consists of seven transmembrane domains, in addition it possesses a highly conserved Cys-Glu-Ser-Phe motif in the second extracellular loop, essential for its function and six Cys residues at the extracellular domains that potentially form three disulfide bonds6.
Anti-GPR81/HCAR1 Antibody (#AHR-011) is a highly specific antibody directed against an epitope of the mouse protein. The antibody can be used in western blot analysis. It has been designed to recognize HCAR1 from rat and mouse samples. The antibody will not recognize human GPR81.
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