|
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 |
|
Primary malignant neoplasm
|
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 |
|
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 |
A tumor growth delay assay was performed using murine syngeneic tumors; one radioresistant tumor, HCa-I and one radiosensitive tumor, MCa-K.
|
20657160 |
2010 |
|
Alzheimer's Disease
|
0.010 |
Biomarker
|
disease |
BEFREE |
As a result, the novel menthol sulfamate and menthol carbonyl sulfamate derivatives can be promising Alzheimer's disease drug candidates and novel hCA I and hCA II enzymes inhibitors.
|
30255953 |
2018 |
|
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 |
|
Primary malignant neoplasm
|
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 |
|
Amyotrophic Lateral Sclerosis
|
0.010 |
Biomarker
|
disease |
BEFREE |
As the physiological function hCA I is poorly understood, and it was recently shown to be involved in the pathogenesis of cerebral malaria and amyotrophic lateral sclerosis, selective and effective inhibitors may be useful as tools or drugs for better understanding this abundant isoform.
|
28318894 |
2017 |
|
Neoplasm Metastasis
|
0.050 |
Biomarker
|
phenotype |
BEFREE |
Cells in which GPR81 was silenced showed a dramatic decrease in growth and metastasis.
|
24928781 |
2014 |
|
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 |
|
Retinal Diseases
|
0.010 |
Biomarker
|
group |
BEFREE |
Herein, we show that GPR81, localized predominantly in Müller cells, governs deep vascular complex formation during development and in ischemic retinopathy.
|
31220454 |
2019 |
|
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 |
|
Pancreatic carcinoma
|
0.010 |
AlteredExpression
|
disease |
BEFREE |
In vivo, GPR81 expression levels correlated with the rate of pancreatic cancer tumor growth and metastasis.
|
24928781 |
2014 |
|
Malignant neoplasm of pancreas
|
0.010 |
AlteredExpression
|
disease |
BEFREE |
In vivo, GPR81 expression levels correlated with the rate of pancreatic cancer tumor growth and metastasis.
|
24928781 |
2014 |
|
Disorder of eye
|
0.010 |
Biomarker
|
group |
BEFREE |
Interesting inhibitory activities were observed against all these isoforms. hCA I, an isoform involved in several eye diseases was inhibited moderately with K<sub>I</sub>s in the range of 191.8-904.2 nM, hCA II, an antiglaucoma drug target was highly inhibited by the new sulfonamides, with K<sub>I</sub>s in the range of 0.75-8.8 nM. hCA IX, a tumor-associated isoform involved in cancer progression and metastatic spread was potently inhibited by the new sulfonamides, with K<sub>I</sub>s in the range of 2.3-87.3 nM, whereas hCA XII, and antiglaucoma and anticancer drug target, was inhibited with K<sub>I</sub>s in the range of 6.1-71.8 nM.
|
28965419 |
2017 |
|
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 |
|
Epilepsy
|
0.030 |
Biomarker
|
disease |
BEFREE |
Most screened sulfonamides showed high potency in inhibiting hCA II, widely involved in glaucoma, epilepsy, edema, and other pathologies (K<sub>i</sub>s in the ranging from 6.32 ± 0.06 to 128.93 ± 23.11 nM). hCA I was inhibited with K<sub>i</sub>s in the range of 6.80 ± 0.10-85.91 ± 7.57 nM, whereas AChE in the range of 60.79 ± 3.51-249.55 ± 7.89 nM.
|
31129502 |
2019 |
|
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 |
|
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 |
|
Malignant neoplasm of breast
|
0.020 |
Biomarker
|
disease |
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 |
|
Breast Carcinoma
|
0.010 |
Biomarker
|
disease |
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 |
|
Diabetes
|
0.010 |
AlteredExpression
|
disease |
BEFREE |
Potentially novel GPR81 agonists were identified that suppressed fasting plasma free fatty acid levels in rodents and in addition improved insulin sensitivity in mouse models of insulin resistance and diabetes.
|
28978803 |
2017 |
|
Diabetes Mellitus
|
0.010 |
AlteredExpression
|
group |
BEFREE |
Potentially novel GPR81 agonists were identified that suppressed fasting plasma free fatty acid levels in rodents and in addition improved insulin sensitivity in mouse models of insulin resistance and diabetes.
|
28978803 |
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 |
|
Malignant neoplasm of breast
|
0.020 |
Biomarker
|
disease |
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 |