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The effects of C on
2021-12-13
The effects of C646 on the NF-κB pathway could be explained by the role for p300 that has been described in the regulation of the NF-κB pathway [5]. For instance, acetylations of the p65 NF-κB subunit on lysines 218, 221 and 310 are mediated by the HATs p300 and PCAF [11] and increase transcriptiona
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Following our initial observation of
2021-12-13
Following our initial observation of an unexpected increase in the maximal rates of cGMP formation by NO-stimulated sGC in the presence of cytosolic PCA preparations [15], we attempted to purify, identify and characterize the responsible protein(s). The purification protocol described in the present
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br For some time it was
2021-12-13
For some time, it was known that membrane-bound guanylate cyclases (GCs) of photoreceptor Ozanimod australia in the retina respond to changes in the [Ca]. Lolley and Racz observed that synthesis of cyclic GMP (cGMP) was stimulated at only low [Ca], concluding that Ca has an inhibitory effect on
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In the present study we focused on a
2021-12-13
In the present study, we focused on a role of the C-terminal segment in GCAP2 using two chimeric proteins, in which the C-terminal segment of GCAP2 was either replaced by the corresponding sequence of recoverin (chimera GR) or transferred into recoverin (chimera RG). We have monitored Ca-dependent c
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KJ Pyr 9 br Ketone body metabolism and neuronal excitability
2021-12-13
Ketone body metabolism and neuronal excitability One of the best examples of the close connection between metabolism and neuronal excitability is illustrated by the effect of ketone bodies on epileptic seizures. One third of patients suffering from epileptic seizures do not respond to conventiona
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LPC OMe LPC LPC and OMe LPC were shown
2021-12-13
LPC 14:0, 2-OMe-LPC 14:0, LPC 16:0 and 2-OMe-LPC 16:0 were shown to be most potent stimulators of intracellular calcium flux in the β cell model, which is one of key processes leading to insulin exocytosis. Yet, species with myristoyl residue initiate calcium influx through voltage-gated 4-iodo-SAHA
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An alternative approach to improving pharmacokinetic
2021-12-13
An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl
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NG,NG-dimethyl-L-Arginine hydrochloride Elimination of the Q
2021-12-13
Elimination of the Q234–R244 bridge significantly affected the protein NG,NG-dimethyl-L-Arginine hydrochloride but had little effect on its activity at a permissive temperature, which may seem contrary to the known functional importance of this motif in Fpg. However, since the mutants fully or part
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Functional studies based on patch clamp electrophysiology pr
2021-12-13
Functional studies based on patch-clamp electrophysiology provide additional information on the active state of GlyR α1. Current-voltage measurements from single Shikonin in outside-out patches at symmetric 145-mM chloride concentration yielded a unitary conductance of 86 pS for the main open state
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ICH induced striatal lesion produced a reduction
2021-12-13
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 pka of alcohol transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain isch
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There are additional implications of subunit alterations in
2021-12-13
There are additional implications of α2-subunit alterations in the hippocampus. P has anticonvulsant activity (Herzog, 1995, Herzog et al., 1997, Herzog et al., 2012, Reddy et al., 2001, Reddy, 2010). These actions result from the metabolic conversion of P to GABA-A receptor-modulating, antiseizure
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Piroxicam belongs to the oxicam
2021-12-13
Piroxicam belongs to the oxicam family of NSAIDs and a special attention has been drawn to this drug because of its multifunctional potential [5], [27], [28]. Chemically, piroxicam (4-hydroxy-2-methyl-N-2-pyrimidyl-2H-1,2-benzothiazine-3-carboxyamide) is an enolic 2×Taq PCR Master Mix(with dye) wit
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The C terminal regions in both FGF and FGF define
2021-12-13
The C-terminal regions in both FGF19 and FGF21 define their KLB interaction [15], [16], [23], [25]. However, less than 40% identity in comparative alignment of C-terminal sequences for these two proteins (Table 1) suggests that their interaction with KLB may require higher-order association with oth
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Compounds were tested for GPR
2021-12-13
Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO ghrelin receptor transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure act
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It raises a question about origin of
2021-12-13
It raises a question about origin of the sensitivity to Ca of both FBPase isozymes. Was the ancestral vertebrate FBPase inhibited by calcium similarly to the liver isozyme? And is the high sensitivity of FBP2 a new evolutionary feature of warm-blooded vertebrates? Additionally, since subcellular lo
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