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The activation of P Rs modulates the activity
2023-05-24
The activation of P1Rs modulates the activity of many ion channels and receptors (Sebastião and Ribeiro, 2009) and the recent detection of P1Rs at the postsynaptic level of the adult NMJ (Garcia et al., 2014) makes potentially possible an adenosine-mediated modulation of the nicotinic MPTP hydrochlo
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In the late s Solvay Pharmaceuticals discontinued the Phase
2023-05-24
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Structure activity relationships biochemical metabolic and m
2023-05-24
Structure–activity relationships [23], [24], [25], [26], biochemical [24], [25], [26], [27], [28], [29], [30], [31], metabolic [19], [27], [28], [29], [30], [31], and molecular [32] investigations have demonstrated that the substrate specificity, as well as other characteristics of T. gondii adenosi
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A key step in the ADAR reaction is the
2023-05-24
A key step in the ADAR reaction is the formation of the adenosine covalent hydrate with a tetrahedral center at C6. The nucleoside analog 8-azanebularine (box in Fig. 6), with its relatively high propensity to form a covalent hydrate, is useful as an adenosine replacement in ADAR2 substrates to trap
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In an attempt to complete the overview
2023-05-24
In an attempt to complete the overview of resistance mechanisms in Spanish codling moth populations, the aims of the present work were to assess the actual occurrence of AChE and kdr mutations in codling moth field populations from different pome fruit-growing areas of Spain, concurrently with the f
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Additionally regulation of GPCR heteromerization by specific
2023-05-24
Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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The exact etiology of BPH is not completely understood howev
2023-05-24
The exact etiology of BPH is not completely understood, however this pathology has been associated with elevated Caspase-9 Colorimetric Assay Kit receptor levels of the androgen DHT (10). Thus, a valuable strategy in BHP treatment is the reduction of DHT (10) levels, by inhibiting its biosynthetic
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In plants altered expression of
2023-05-24
In plants, altered expression of Aurora kinases results in impaired meiotic divisions followed by the formation of aneuploid or polyploid progenies [21]. This observation is interesting from an evolutionary point of view because it can be assumed that, during evolution, the influence of biotic and a
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exemplifies three of the compounds investigated in the
2023-05-24
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC The Bufalin as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation products
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As noted above yeasts particularly S cerevisiae Frey and
2023-05-19
As noted above, yeasts, particularly S. cerevisiae (Frey and Röhm 1978; Trumbly and Bradley 1983), produce APs, but these are intracellular enzymes located in the vacuolar compartment, with the exception of aminopeptidase II. About 40% of aminopeptidase II activity is detected as external enzyme, li
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In addition to plasma membrane sites OCT
2023-05-17
In addition to plasma membrane sites, OCT3 was also observed associated with endomembranes, including mitochondrial membranes, with particularly strong expression in the outer nuclear membranes of both neurons and astrocytes (Gasser et al., 2017), indicating that, in addition to regulating extracel
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br Introduction Psychostimulant abuse and addiction remain a
2023-05-17
Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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By promoting bundling and processive elongation of
2023-05-17
By promoting bundling and processive elongation of MRS 1220 australia filaments and inhibiting association of capping protein with filament barbed ends, Ena/VASP family proteins contribute to the dynamics of lamellipodia and filopodia [41] and maintenance of focal adhesions and tight junctions [42,
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Previously we described that cadmium induces a more
2023-05-17
Previously, we described that cadmium induces a more pronounced, but not selective, cell death on primary cholinergic neurons from basal forebrain (Del Pino et al., 2014). Degeneration of septal cholinergic neurons from basal forebrain, as happens in AD, results in memory deficits (Scheiderer et al.
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br Experimental procedure br Funding The
2023-05-17
Experimental procedure Funding The present study was supported by the Grant Russian Foundation for basic research (project no. 16-04-01517). Introduction 5-HT, a monoaminergic neurotransmitter, is synthesised from l-tryptophan catalysed by the enzymes tryptophan hydroxylase (Tph) and aroma
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