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The GABA A receptors containing the subunit are
2022-05-16
The GABA-A receptors containing the δ subunit are crucial for the mediation of non-synaptic inhibition in the dentate gyrus; thus, the decreased expression of the δ subunit may suggest a decrease in the inhibitory tone and an increase in the neuronal excitability. Moreover, the GABA-A receptors cont
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br Materials and methods br Results br Discussion Zn
2022-05-16
Materials and methods Results Discussion Zn2+ is an extremely abundant transition metal in the synaptic vesicles of hippocampal glutamatergic mossy fibers and remains a key factor in the modulation of neuronal plasticity (Assaf and Chung, 1984). Disruption of Zn2+ homeostasis is associated
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br Experimental br Results and discussion br
2022-05-16
Experimental Results and discussion Conclusion In conclusion, four bisnaphthalimides have been investigated for their potential G-quadruplex binding. The compounds 3a, 3b and 5b display high affinity for telomeric and oncogenic G-quadruplexes. On the other hand, 5a only show high affinity f
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OCA has recently been approved for the treatment of
2022-05-16
OCA has recently been approved for the treatment of patients with PBC and is under study for diseases such as NASH, PSC and biliary atresia [30], [49]. Up to now, the beneficial effects of OCA have been related to its anti-cholestatic, anti-inflammatory and anti-fibrotic properties. We have here rep
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Compared to a large database of
2022-05-16
Compared to a large database of NSCLC samples matched for disease type, many of the frequently altered genes were similar to those seen in this series of FGFR fusion-positive samples; however, there were notable exceptions. As expected, alterations in known NSCLC drivers (KRAS and EGFR) were signifi
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Our previous study had shown that silencing
2022-05-16
Our previous study had shown that silencing FFAR1 expression weakened the action of PIO in increasing insulin secretion in lipotoxic β enfuvirtide [6]. Resent research found that PIO promoted insulin secretion by upregulating FFAR1 [17]. Therefore, we presumed that FFAR1 may be involved in the anti
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br Results br Discussion Our studies
2022-05-16
Results Discussion Our studies highlight MUFAs as key lipid modulators of both non-apoptotic and apoptotic cell death. Recent studies show that a more mesenchymal phenotype, de-differentiation, and acquired resistance to targeted inhibitors, can all promote a ferroptosis-sensitive cell state (
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In the FARM motifs of GGPPSs hydrophobic amino acids are
2022-05-16
In the FARM motifs of GGPPSs, hydrophobic FITC, Fluorescein isothiocyanate receptor are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta C
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In the Joint United Nations
2022-05-16
In 2015, the Joint United Nations Program on HIV/AIDS (UNAIDS) proposed that by 2020, 90% of people living with HIV should be aware of their HIV status, as the first part of 90-90-90 strategy to end AIDS epidemic. Early detection of HIV allows initiating care for proper treatment, which impacts in m
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KL 001 br To explore further the functional
2022-05-16
To explore further the functional impact of the similarity of the UTY and KDM6A proteins, the FANTOM5 human dataset was analysed to determine whether or not the genes were expressed at the same time in the same tissues (which would suggest that they are controlled by the same regulators) or with o
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The stability and function of the HIF
2022-05-16
The stability and function of the HIF-1α protein are affected by many post-translational modifications (PTMs), including hydroxylation, acetylation, ubiquitination and SUMOylation [[29], [30], [31]]. It has been shown that HIF-1α stability is regulated by LSD1 [25]; in particular, the Set9 histone m
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Compound containing dimethylglutarimide P cap P propyl group
2022-05-13
Compound containing, dimethylglutarimide P-cap, P propyl group, α-methylbenzyl urea resulted in inhibitor with much improved binding (=0.064μM) and EC=0.3μM. This was an aza-peptide analog with an EC comparable to our first generation clinical candidate . Analog was evaluated for its selectivity
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Several studies have found that GPR possesses a
2022-05-13
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Probenecid expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (R
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br Materials and methods br Results br Discussion br
2022-05-13
Materials and methods Results Discussion Disclosures Author contributions Acknowledgements Introduction Diabetes mellitus is one of the fastest growing chronic diseases worldwide, with an estimated prevalence of 382 million patients, of which about 90% have type 2 diabetes melli
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Consistent with previous reports of an association between i
2022-05-13
Consistent with previous reports of an association between increased accumulation of cAMP and GLP-1 secretion [25, 44, 45], we hypothesized that Oleoyl-LPI may regulate GPR119 activation and secretion of GLP-1 secretion through the cAMP/PKA/CREB pathway. Pharmacological inhibition of PKA by H-89 was
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