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Targeting MCTs is likely to have dramatic effects on
2021-09-29

Targeting MCTs is likely to have dramatic effects on lactate-dependent metabolic symbiosis described in the previous paragraphs. A plethora of MCT inhibitors have been described, including α-cyano-4-hydroxycinnamate (CHC) [59], organomercurials [60], stilbene disulfonates [60], and other second-gene
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The manuscript provides mechanistic insights into the suppre
2021-09-29

The manuscript provides mechanistic insights into the suppression of EGFR, BCRP, PKM2, and other cancer biomarkers in response to pharmacological inhibition of GPR55 with MNF and CID (Fig. 7). Firstly, inactivation of ERK has been previously demonstrated following treatment of PANC-1 DL-TBOA recepto
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Glycine regulates several brain functions and glycine transp
2021-09-29

Glycine regulates several brain functions and glycine transporters significantly contribute in such processes. In previous work we reported calpain sensitive regions in N-terminal domains of GlyT1a and GlyT1b (Baliova and Jursky, 2005). Here we show that distal part of glycine transporter GlyT1C-ter
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As discussed above both endogenous and exogenous
2021-09-29

As discussed above, both endogenous and exogenous lesions can lead to adverse health effects [43]. Damaged nucleobases can block DNA replication which is often lethal to cells [44]. The effectiveness of DNA restoration by DNA glycosylases should be closely monitored to gain an insight of the functio
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br Conflict of interest br Funding br Acknowledgements br
2021-09-29

Conflict of interest Funding Acknowledgements Introduction to SLC6 transporters The solute carrier (SLC) 6 family of membrane proteins perform the Na+-coupled symport of amino acids and amino nigericin derivatives into cells throughout the body. Disrupting neurotransmitter SLC6-mediated
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ICH induced striatal lesion produced
2021-09-29

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino Cytarabine transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia
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br Materials and methods br Results
2021-09-29

Materials and methods Results Conclusions We developed a glutamate biosensor with chitosan as a matrix for the immobilization of the enzyme glutamate oxidase on the surface of a platinum electrode. Our miniaturized biosensor of 50 µm in diameter can be applied for monitoring glutamate in vi
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Here we studied the effects of BZ flurazepam FZ at
2021-09-29

Here we studied the effects of BZ flurazepam (FZ) at high doses in acute and chronic settings of tolerance and dependence in GluR-A−/− mice (Zamanillo et al., 1999). We used measurements in which the phenomenon of “learning while intoxicated” should play only a minor role in order to find out the si
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LbGlcK and the HsHxKIV d glucose
2021-09-29

LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key biotin-LC-LC-tyramide binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, s
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Although encoded by a single gene
2021-09-29

Although encoded by a single gene, GR displays considerable heterogeneity through the combined effects of alternative mRNA splicing, alternative translation initiation, and complex post-translational modification. Differential expression of the various GR isoforms may contribute to tissue-specific f
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In conclusion we have shown
2021-09-29

In conclusion, we have shown that AKR1D1 regulates glucocorticoid availability and GR activation and therefore represents a key pre-receptor regulator of hormonal action in human liver. However, there are additional questions that need to be addressed including dissecting the broader role of AKR1D1
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In conclusion a novel series of
2021-09-28

In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen STF-62247 had a remarkable effect on the GPR40 agonistic activity.
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depicts the synthesis of series
2021-09-28

depicts the synthesis of series with a four-step sequence. First, the commercially available 4-hydroxybenzaldehyde () was condensed with 2-bromoethanol through Mitsunobu reaction to give the key intermediate (). Next, conventional nucleophilic substitution reaction with the privileged structures (
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br Acknowledgements The authors have
2021-09-28

Acknowledgements The authors have no ethical conflicts to disclose. The authors have no conflicts of interest to declare. This work was funded by the Research Council of Lithuania. Introduction This paper studies whether there is a causal influence of the risk-taking incentives provided by op
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The present findings demonstrate for
2021-09-28

The present findings demonstrate for the first time in immature rats that hippocampal infusion of ET-1 results in a rapid and long-lasting decrease in regional cerebral blood flow (rCBF) and oxygen saturation (pO2). These data are in accord with the results of studies and adult animals, which have s
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