| High Glucose Levels Promote Switch to Synthetic Vascular Smooth Muscle Cells via Lactate/GPR81. | High Glucose Levels Promote Switch to Synthetic Vascular Smooth Muscle Cells via Lactate/GPR81.
Yang J, Gourley GR, Gilbertsen A, Chen C, Wang L, Smith K, Namenwirth M, Yang L., Free PMC Article | 02/15/2024 |
| Activation of GPR81 aggravated intestinal ischemia/reperfusion injury-induced acute lung injury via HMGB1-mediated neutrophil extracellular traps formation. | Activation of GPR81 aggravated intestinal ischemia/reperfusion injury-induced acute lung injury via HMGB1-mediated neutrophil extracellular traps formation.
Yili S, Xinyi D, Kerui F, Kun C, Yang Y, Zhang L, Hu K., Free PMC Article | 11/6/2023 |
| History and Function of the Lactate Receptor GPR81/HCAR1 in the Brain: A Putative Therapeutic Target for the Treatment of Cerebral Ischemia. | History and Function of the Lactate Receptor GPR81/HCAR1 in the Brain: A Putative Therapeutic Target for the Treatment of Cerebral Ischemia.
Colucci ACM, Tassinari ID, Loss EDS, de Fraga LS. | 08/19/2023 |
| The lactate receptor GPR81 is predominantly expressed in type II human skeletal muscle fibers: potential for lactate autocrine signaling. | The lactate receptor GPR81 is predominantly expressed in type II human skeletal muscle fibers: potential for lactate autocrine signaling.
Nordström F, Liegnell R, Apró W, Blackwood SJ, Katz A, Moberg M. | 02/25/2023 |
| Insights into the regulation of podocyte and glomerular function by lactate and its metabolic sensor G-protein-coupled receptor 81. | Insights into the regulation of podocyte and glomerular function by lactate and its metabolic sensor G-protein-coupled receptor 81.
Grochowalska K, Pikul P, Piwkowska A. | 12/3/2022 |
| Activation of lactate receptor HCAR1 down-modulates neuronal activity in rodent and human brain tissue. | Activation of lactate receptor HCAR1 down-modulates neuronal activity in rodent and human brain tissue.
Briquet M, Rocher AB, Alessandri M, Rosenberg N, de Castro Abrantes H, Wellbourne-Wood J, Schmuziger C, Ginet V, Puyal J, Pralong E, Daniel RT, Offermanns S, Chatton JY., Free PMC Article | 08/20/2022 |
| Lactate receptor HCAR1 regulates cell growth, metastasis and maintenance of cancerspecific energy metabolism in breast cancer cells. | Lactate receptor HCAR1 regulates cell growth, metastasis and maintenance of cancer‑specific energy metabolism in breast cancer cells.
Jin L, Guo Y, Chen J, Wen Z, Jiang Y, Qian J., Free PMC Article | 07/16/2022 |
| The lactate sensor GPR81 regulates glycolysis and tumor growth of breast cancer. | The lactate sensor GPR81 regulates glycolysis and tumor growth of breast cancer.
Ishihara S, Hata K, Hirose K, Okui T, Toyosawa S, Uzawa N, Nishimura R, Yoneda T., Free PMC Article | 05/7/2022 |
| Rare and potentially pathogenic variants in hydroxycarboxylic acid receptor genes identified in breast cancer cases. | Rare and potentially pathogenic variants in hydroxycarboxylic acid receptor genes identified in breast cancer cases.
McGuire Sams C, Shepp K, Pugh J, Bishop MR, Merner ND., Free PMC Article | 04/23/2022 |
| Transcriptomic and functional studies reveal miR-431-5p as a tumour suppressor in pancreatic ductal adenocarcinoma cells. | Transcriptomic and functional studies reveal miR-431-5p as a tumour suppressor in pancreatic ductal adenocarcinoma cells.
Haugen ØP, Khuu C, Weidemann HM, Utheim TP, Bergersen LH. | 03/19/2022 |
| HCAR1/MCT1 Regulates Tumor Ferroptosis through the Lactate-Mediated AMPK-SCD1 Activity and Its Therapeutic Implications. | HCAR1/MCT1 Regulates Tumor Ferroptosis through the Lactate-Mediated AMPK-SCD1 Activity and Its Therapeutic Implications.
Zhao Y, Li M, Yao X, Fei Y, Lin Z, Li Z, Cai K, Zhao Y, Luo Z. | 11/13/2021 |
| Effects of GPR81 silencing combined with cisplatin stimulation on biological function in hypopharyngeal squamous cell carcinoma. | Effects of GPR81 silencing combined with cisplatin stimulation on biological function in hypopharyngeal squamous cell carcinoma.
Jia Q, Xu O, Wang J, Dong J, Ren X, Jia X, Shan C., Free PMC Article | 04/24/2021 |
| Heterogeneous ozone effects on the DNA methylome of bronchial cells observed in a crossover study. | Heterogeneous ozone effects on the DNA methylome of bronchial cells observed in a crossover study.
Bind MC, Rubin DB, Cardenas A, Dhingra R, Ward-Caviness C, Liu Z, Mirowsky J, Schwartz JD, Diaz-Sanchez D, Devlin RB., Free PMC Article | 01/16/2021 |
| The lactate receptor GPR81 promotes breast cancer growth via a paracrine mechanism involving antigen-presenting cells in the tumor microenvironment. | The lactate receptor GPR81 promotes breast cancer growth via a paracrine mechanism involving antigen-presenting cells in the tumor microenvironment.
Brown TP, Bhattacharjee P, Ramachandran S, Sivaprakasam S, Ristic B, Sikder MOF, Ganapathy V. | 11/28/2020 |
| Monocarboxylate transporters in cancer. | Monocarboxylate transporters in cancer.
Payen VL, Mina E, Van Hée VF, Porporato PE, Sonveaux P., Free PMC Article | 11/21/2020 |
| Activation of GPR81 can rescue oscillatory shear stress -induced reduced expression of the key atheroprotective transcription factor KLF2. | Activation of GPR81 by lactate inhibits oscillatory shear stress-induced endothelial inflammation by activating the expression of KLF2.
Sun Z, Han Y, Song S, Chen T, Han Y, Liu Y. | 07/11/2020 |
| The transcriptional response of GPR81 to lactate is mediated by Signal transducer and activator of transcription 3 (STAT3). | A lactate-induced Snail/STAT3 pathway drives GPR81 expression in lung cancer cells.
Xie Q, Zhu Z, He Y, Zhang Z, Zhang Y, Wang Y, Luo J, Peng T, Cheng F, Gao J, Cao Y, Wei H, Wu Z. | 07/11/2020 |
| The novel role of HCAR1 in development of chemoresistance in cervical carcinoma HeLa cells via ABCB1 transporter up-regulation. | The lactate receptor (HCAR1/GPR81) contributes to doxorubicin chemoresistance via ABCB1 transporter up-regulation in human cervical cancer HeLa cells.
Wagner W, Kania KD, Blauz A, Ciszewski WM. | 07/7/2018 |
| Findings identify GPR81 as a tumor-promoting receptor in breast cancer progression and suggest a novel mechanism that regulates GPR81-dependent activation of the PI3K/Akt signaling axis in tumor microenvironment. | G-protein-coupled receptor 81 promotes a malignant phenotype in breast cancer through angiogenic factor secretion.
Lee YJ, Shin KJ, Park SA, Park KS, Park S, Heo K, Seo YK, Noh DY, Ryu SH, Suh PG., Free PMC Article | 02/24/2018 |
| Activation of GPR81 decreases intracellular cAMP levels and inhibits PKA activity, leading to activation of TAZ and upregulation of PD-L1. This study reveals a critical role for lactate in the immune checkpoint pathway and an unexpected function of TAZ in tumor evasion of the T-cell-mediated immune response. | Tumor cell-derived lactate induces TAZ-dependent upregulation of PD-L1 through GPR81 in human lung cancer cells.
Feng J, Yang H, Zhang Y, Wei H, Zhu Z, Zhu B, Yang M, Cao W, Wang L, Wu Z. | 10/28/2017 |
| Lactate receptor/HCAR1 expression in cervical carcinoma cells may contribute to the modulation of cellular DNA repair mechanisms. | Stimulation of lactate receptor (HCAR1) affects cellular DNA repair capacity.
Wagner W, Kania KD, Ciszewski WM. | 08/5/2017 |
| HCA1/3 are necessary for breast cancer cells to balance lipid/fatty acid metabolism. | Hydroxycarboxylic acid receptors are essential for breast cancer cells to control their lipid/fatty acid metabolism.
Stäubert C, Broom OJ, Nordström A., Free PMC Article | 05/28/2016 |
| HCAR1 and monocarboxylate transporters activity is required for the L- and D-lactate-mediated enhancement of DNA repair and of HeLa cell survival. | L- and D-lactate enhance DNA repair and modulate the resistance of cervical carcinoma cells to anticancer drugs via histone deacetylase inhibition and hydroxycarboxylic acid receptor 1 activation.
Wagner W, Ciszewski WM, Kania KD., Free PMC Article | 03/12/2016 |
| Description of a GPR81 selective agonist with in vivo efficacy, inhibiting lipolysis without flushing. | Identification of a novel GPR81-selective agonist that suppresses lipolysis in mice without cutaneous flushing.
Sakurai T, Davenport R, Stafford S, Grosse J, Ogawa K, Cameron J, Parton L, Sykes A, Mack S, Bousba S, Parmar A, Harrison D, Dickson L, Leveridge M, Matsui J, Barnes M. | 01/31/2015 |
| Data support that GPR81 is important for cancer cell regulation of lactate transport mechanisms. | Cell surface lactate receptor GPR81 is crucial for cancer cell survival.
Roland CL, Arumugam T, Deng D, Liu SH, Philip B, Gomez S, Burns WR, Ramachandran V, Wang H, Cruz-Monserrate Z, Logsdon CD., Free PMC Article | 01/24/2015 |