HCAR1, hydroxycarboxylic acid receptor 1, 27198

N. diseases: 26; N. variants: 0
Source: ALL
Disease Score gda Association Type Type Original DB Sentence supporting the association PMID PMID Year
CUI: C0027651
Disease: Neoplasms
Neoplasms
0.070 Biomarker group BEFREE These compounds showed pronounced selectivity towards the cytosolic human (h) isoforms such as the hCA I, II and VII rather than the membrane tumor associate hCA IX. 31693947 2020
CUI: C0017601
Disease: Glaucoma
Glaucoma
0.070 Biomarker disease BEFREE The physiologically important and off-target cytosolic isoform hCA I was weakly inhibited by most of the newly synthesized sulfonamides while the glaucoma associated isoform hCA II was moderately inhibited with K<sub>I</sub>s spanning in low nanomolar range (K<sub>I</sub> = 8.0 nM-0.903 μM). 31539777 2019
CUI: C0017601
Disease: Glaucoma
Glaucoma
0.070 Biomarker disease BEFREE Most of these compounds exhibited excellent activity against all these isoforms. hCA I was inhibited with <i>K<sub>i</sub></i>s in the range of 50.8-966.8 nM, while the glaucoma associated hCA II was inhibited with <i>K<sub>i</sub></i>s in the range of 6.5-760.0 nM. 31237458 2019
CUI: C0017601
Disease: Glaucoma
Glaucoma
0.070 Biomarker disease BEFREE These compounds were tested for the inhibition of four human (h) isoforms, hCA I, II, IX, and XII, involved in pathologies such as glaucoma (CA II and XII) or cancer (CA IX/XII). 31112841 2019
CUI: C0017601
Disease: Glaucoma
Glaucoma
0.070 Biomarker disease BEFREE The ureido benzenesulfonamides incorporating triazinyl moieties were investigated as inhibitors of four selected physiologically relevant human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, namely, hCA I, II, IX, and XII which are involved in various diseases such as glaucoma, epilepsy, obesity and cancer. 30312866 2019
CUI: C0027651
Disease: Neoplasms
Neoplasms
0.070 Biomarker group BEFREE Novel sulfonamidoindole-based hydrazones with a 2-(hydrazinocarbonyl)-3-phenyl-1<i>H</i>-indole-5-sulfonamide scaffold were synthesized and tested in enzyme inhibition assays against the tumor-associated carbonic anhydrase isoforms, hCA IX and XII, and the off-targets, hCA I and II. 31083645 2019
CUI: C0017601
Disease: Glaucoma
Glaucoma
0.070 Biomarker disease BEFREE The obtained 1,3-diaryltriazene-substituted sulfonamides were investigated as inhibitors of four selected human carbonic anhydrase (CA, EC 4.2.1.1) isoforms (hCA I, hCA II, hCA VII and hCA IX) are involved in various diseases such as glaucoma, epilepsy, retinitis pigmentosa, cancer, obesity, etc. 29462772 2018
CUI: C0017601
Disease: Glaucoma
Glaucoma
0.070 Biomarker disease BEFREE The cytosolic isoform hCA I was inhibited with K<sub>i</sub>'s ranging between 53.2 nM and 7.616 μM whereas the glaucoma associated cytosolic isoform hCA II was inhibited with K<sub>i</sub>'s in the range 21.8 nM-0.807 μM. 29571155 2018
CUI: C0017601
Disease: Glaucoma
Glaucoma
0.070 Biomarker disease BEFREE Some of these sulfonamides showed effective inhibitory action (in the nanomolar range) against the cytosolic isoform hCA II and the transmembrane, tumor-associated one hCA IX, making them interesting candidates for preclinical evaluation in glaucoma or various tumors in which the two enzymes are involved. hCA I and IV were on the other hand less inhibited by these sulfonamides, with inhibition constants in the micromolar range. 28161252 2017
CUI: C0027651
Disease: Neoplasms
Neoplasms
0.070 Biomarker group BEFREE GPR81 and GPR91 are tumor promoters, and increased production of lactate and succinate as their agonists drives tumorigenesis by enhancing signaling via these two receptors. 28512002 2017
CUI: C0027651
Disease: Neoplasms
Neoplasms
0.070 Biomarker group BEFREE Overall, these 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. 27765922 2016
CUI: C0027651
Disease: Neoplasms
Neoplasms
0.070 Biomarker group BEFREE These sulfonamides were investigated as inhibitors of the human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms hCA I and II (cytosolic isozymes), as well as hCA IX and XII (trans-membrane, tumor-associated enzymes). 26875933 2016
CUI: C0027651
Disease: Neoplasms
Neoplasms
0.070 AlteredExpression group BEFREE Examination of tumors resected from patients with pancreatic cancer indicated that 94% (148 of 158) expressed high levels of GPR81. 24928781 2014
CUI: C0027651
Disease: Neoplasms
Neoplasms
0.070 Biomarker group BEFREE A tumor growth delay assay was performed using murine syngeneic tumors; one radioresistant tumor, HCa-I and one radiosensitive tumor, MCa-K. 20657160 2010
CUI: C0027627
Disease: Neoplasm Metastasis
Neoplasm Metastasis
0.050 Biomarker phenotype BEFREE Highly expressed G protein-coupled receptor 81 (GPR81), a receptor for lactate, is emerging as a critical regulator of tumor growth and metastasis. 31666207 2020
CUI: C0006826
Disease: Malignant Neoplasms
Malignant Neoplasms
0.050 Biomarker group BEFREE These compounds were tested for the inhibition of four human (h) isoforms, hCA I, II, IX, and XII, involved in pathologies such as glaucoma (CA II and XII) or cancer (CA IX/XII). 31112841 2019
CUI: C0006826
Disease: Malignant Neoplasms
Malignant Neoplasms
0.050 Biomarker group BEFREE The ureido benzenesulfonamides incorporating triazinyl moieties were investigated as inhibitors of four selected physiologically relevant human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, namely, hCA I, II, IX, and XII which are involved in various diseases such as glaucoma, epilepsy, obesity and cancer. 30312866 2019
CUI: C1306459
Disease: Primary malignant neoplasm
Primary malignant neoplasm
0.050 Biomarker group BEFREE These compounds were tested for the inhibition of four human (h) isoforms, hCA I, II, IX, and XII, involved in pathologies such as glaucoma (CA II and XII) or cancer (CA IX/XII). 31112841 2019
CUI: C1306459
Disease: Primary malignant neoplasm
Primary malignant neoplasm
0.050 Biomarker group BEFREE The ureido benzenesulfonamides incorporating triazinyl moieties were investigated as inhibitors of four selected physiologically relevant human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, namely, hCA I, II, IX, and XII which are involved in various diseases such as glaucoma, epilepsy, obesity and cancer. 30312866 2019
CUI: C0006826
Disease: Malignant Neoplasms
Malignant Neoplasms
0.050 Biomarker group BEFREE As such, these three metabolite receptors play a critical role in cancer and represent a new class of drug targets with selective antagonists of GPR81 and GPR91 for cancer treatment and agonists of GPR109A for cancer prevention. 28512002 2017
CUI: C0006826
Disease: Malignant Neoplasms
Malignant Neoplasms
0.050 Biomarker group BEFREE The lactate receptor, also known as hydroxycarboxylic acid receptor 1 (HCAR1/GPR81), plays a vital role in cancer biology. 29151072 2017
CUI: C0027627
Disease: Neoplasm Metastasis
Neoplasm Metastasis
0.050 Biomarker phenotype BEFREE Recently, hydroxycarboxylic acid receptor 1 (HCAR1) was shown to drive lactate-dependent enhancement of cell survival and metastasis in pancreatic and breast cancers. 28258841 2017
CUI: C0027627
Disease: Neoplasm Metastasis
Neoplasm Metastasis
0.050 Biomarker phenotype BEFREE Recently, HCAR1 was reported to enhance metastasis, cell growth, and survival of pancreatic, breast, and cervical cancer cells. 29151072 2017
CUI: C0027627
Disease: Neoplasm Metastasis
Neoplasm Metastasis
0.050 Biomarker phenotype BEFREE Through its transporters (MCTs) and receptor (GPR81), lactic acid plays a key role in multiple cellular processes, including energy regulation, immune tolerance, memory formation, wound healing, ischemic tissue injury, and cancer growth and metastasis. 29021365 2017
CUI: C1306459
Disease: Primary malignant neoplasm
Primary malignant neoplasm
0.050 Biomarker group BEFREE The lactate receptor, also known as hydroxycarboxylic acid receptor 1 (HCAR1/GPR81), plays a vital role in cancer biology. 29151072 2017