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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
Malignant Neoplasms
|
0.050 |
Biomarker
|
group |
BEFREE |
GPR81 is a lactate receptor recently identified in adipose and muscle cells that has not been investigated in cancer.
|
24928781 |
2014 |
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 |
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 |
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 |
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 |
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 |
Neoplasm Metastasis
|
0.050 |
Biomarker
|
phenotype |
BEFREE |
Cells in which GPR81 was silenced showed a dramatic decrease in growth and metastasis.
|
24928781 |
2014 |
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 |
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 |