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br Potential endogenous agonists of GPR The
2021-11-18
Potential endogenous agonists of GPR35 The first endogenously produced chemical that was shown to be able to activate GPR35 was the tryptophan metabolite kynurenic Betaine sale [8]. When human GPR35 was expressed along with a mixture of promiscuous and chimeric G proteins 9, 10 (Box 1) in CHO ce
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Previously we have shown that the natural
2021-11-17
Previously, we have shown that the natural flavonoid compounds that possess C-4 ketone group and C-5 hydroxy group, such as baicalein, luteolin, myricetin and quercetin, effectively inhibit human GLO I. Considering our interest in inhibitors of GLO I and based on the rationale mentioned above, struc
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Excessive extracellular glutamate may induce excitotoxic neu
2021-11-17
Excessive extracellular glutamate may induce excitotoxic neuronal damage in disorders of the CNS (Schwartz et al., 2003). EAATs are considered to contribute to prevention of excitotoxicity by glutamate uptake. Our data revealed that expression levels of membrane EAAT proteins in astrocytes are much
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Caffeine decreased EAAT and EAAT expression levels
2021-11-17
Caffeine decreased EAAT1 and EAAT2 Eltrombopag Olamine levels in P2 fraction, as well as [3H]d-aspartate uptake; however, as soon as caffeine is removed from incubation, [3H]-d-Aspartate uptake is recovered to control levels, eliminating the possibility of caffeine as a cell death inducer. In resu
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br GluR A knockout mice
2021-11-17
GluR-A knockout mice Genetically modified, adult mice lacking the GluR-A AMPA receptor subunit exhibit fast synaptic transmission in the hippocampus, mediated by the receptors formed from the remaining AMPA receptor subunits GluR-B and GluR-C (Sommer et al., 1991), but are deficient in a rapidly
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Although encoded by a single gene GR displays considerable h
2021-11-17
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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After initial optimization of the distances we
2021-11-17
After initial optimization of the distances we obtained the structure iG shown schematically in Fig. 1. This is the telomeric fragment of chromosome with the noncanonical structures of i-motif and G-quadruplex placed symmetrically in the middle of the duplex. Obviously, we consider the situation whe
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Current studies have identified five
2021-11-17
Current studies have identified five orphan G protein-coupled receptors (GPCRs) that can be activated by free fatty acids (FFAs), GPR40, GPR41, GPR43, GPR84, and GPR120. Short-chain fatty acids (FAs) are specific agonists of GPR41 and GPR43 [21] and middle-chain FAs agonize GPR84 [22]. Long-chain FAs
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Senger et al performed a retrospective review of patients wi
2021-11-17
Senger et al. performed a retrospective review of 17 patients with ICH on dabigatran or rivaroxaban who received 4F-PCC. Eight patients had a traumatic Hydroxy Bupropion injury (TBI) and nine patients had a spontaneous ICH. Nine patients had a devastating outcome, including severe neurologic defici
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Several observations about structure activity relationships
2021-11-17
Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic Emodepside class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage
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br Materials and methods br Results
2021-11-17
Materials and methods Results Discussion The development of HCC is a multistep process involving the accumulation of multiple genetic and epigenetic alterations that lead to the activation of oncogenes and inactivation of tumor suppressor genes [20]. Frequent intrahepatic or pulmonary metas
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br Results br Discussion In this study
2021-11-17
Results Discussion In this study, six new T30695 variants were synthesized with the acyclic R or S glycerol linker instead of gaba receptor unit at 4, 8 or 12 T residue. Based on our previous studies on TBA-GQ, this type of modification should provoke local changes in GQ conformations in the
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We reveal that the four well known
2021-11-17
We reveal that the four well known vertebrate families of KAT enzymes (GNAT, MYST, P300/CBP, Basal transcription factor/nuclear receptor co-activator) seem to be conserved (Karmodiya et al., 2014; Roth et al., 2001; Sheikh & Akhtar, 2018) in the mangrove rivulus, together with Camello, a potential n
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Of what interest is the link between
2021-11-16
Of what interest is the link between GSNOR and NO in the plant response to Fe deficiency? On the one hand, NO acts as an important signal to help plants accommodate Fe deficiencies; on the other hand, surplus NO is indeed a harmful RNS that induces severe S-nitrosylation-related damage at a higher s
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To apply the recently developed GPR ligands to
2021-11-16
To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the BRD-9424 and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this end, the pr
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