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G protein-coupled receptors (GPCRs, or GPRs), such as GPR81, contain 7 transmembrane domains and transduce extracellular signals through heterotrimeric G proteins.[supplied by OMIM, Feb 2005].. Additionally we are shipping G Protein-Coupled Receptor 81 Antibodies (100) and many more products for this protein.
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lactate can induce GPR81-independent metabolic changes that modulate macrophage pro-inflammatory activation.
GPR81 expression increased during gestation, and peaked near labor. GPR81 is expressed in the uterus with high expression in myometrium. GPR81 mediates inflammation in the laboring uterus.
Results indicate that lactate may aggravated ischemic brain injury by activating GPR81 and inhibition of GPR81 protects against ischemia-induced cell death via an antiapoptosis pathway
Description of a GPR81 selective agonist with in vivo efficacy, inhibiting lipolysis without flushing.
Lactate negatively regulates TLR induction of the NLRP3 (show NLRP3 Proteins) inflammasome and production of IL1beta (show IL1B Proteins), via ARRB2 (show ARRB2 Proteins) and GPR81 in liver and pancreatic injury.
chronic obesity reduces GPR109A and GPR81 expression in the adipose tissue, while acute in vitro LPS treatment increases expression of GPR109A in adipocytes and macrophages.
Inflammation decreases the expression of GPR81 in adipose tissue
An autocrine lactate loop mediates insulin (show INS Proteins)-dependent inhibition of lipolysis through GPR81.
GPR81 couples to the Gi signaling pathway
Data show that siRNA-mediated knockdown (show PPARG Proteins)of PPARgamma in differentiated 3T3-L1 adipocytes showed a significant decrease in Gpr81 protein expression.
Activation of GPR81 decreases intracellular cAMP levels and inhibits PKA activity, leading to activation of TAZ (show TAZ Proteins) and upregulation of PD-L1 (show CD274 Proteins). This study reveals a critical role for lactate in the immune checkpoint pathway and an unexpected function of TAZ (show TAZ Proteins) in tumor evasion of the T-cell-mediated immune response.
Lactate receptor/HCAR1 expression in cervical carcinoma cells may contribute to the modulation of cellular DNA repair mechanisms.
HCA1/3 are necessary for breast cancer cells to balance lipid/fatty acid metabolism.
HCAR1 and monocarboxylate transporters activity is required for the L- and D-lactate-mediated enhancement of DNA repair and of HeLa cell survival.
Data support that GPR81 is important for cancer cell regulation of lactate transport mechanisms.
demonstrated that the C165-E166-S167-F168 motif at the second extracellular loop is critical for GPR81 function, and the conserved six Cys (show DNAJC5 Proteins) residues at the extracellular regions are necessary for GPR81 function
GPR81 with relatively restricted expression in the adipose tissues functions as a receptor for lactate and can mediate an anti-lipolytic effect of lactate.
Data show that the coordinated PPARgamma (show PPARG Proteins)-mediated regulation of the GPR81, GPR109A and GPR109B presents a novel mechanism by which TZDs may reduce circulating free fatty acid levels and perhaps ameliorate insulin (show INS Proteins) resistance in obese patients.
G protein-coupled receptors (GPCRs, or GPRs), such as GPR81, contain 7 transmembrane domains and transduce extracellular signals through heterotrimeric G proteins.
G protein-coupled receptor 81
, G-protein coupled receptor 81
, hydroxycarboxylic acid receptor 1
, G protein-coupled receptor 104
, G-protein coupled receptor 104
, T-cell activation G protein-coupled receptor
, hydroxy-carboxylic acid receptor 1
, lactate receptor 1