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Tacrine an aminoacridine derivative Fig A was the first
2024-10-31
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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Because of its role in tumor growth proliferation and
2024-10-31
Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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As shown in B the recombinant human LOX nM
2024-10-31
As shown in B, the recombinant human 15-LOX-1 (30nM) showed a time-dependent increase in fluorescent signal, and signal development was almost completed within 20min in the presence of 50μM arachidonic NGB 2904 and 5μM DHR. For both purified enzyme and cell lysates, the enzyme activities disappeared
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Almorexant receptor Another heroic set of studies combining
2024-10-30
Another heroic set of studies combining retrodialysis with electrophysiological recording at two distinct brain sites further indicated that the estradiol-induced increase in auditory-evoked firing in NCM also enhanced the selectivity of auditory-evoked responses in the downstream sensorimotor nucle
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Mitochondria are key organelles involved in the
2024-10-30
Mitochondria are key organelles involved in the mechanism of apoptosis (Xiong et al., 2014), and loss of ΔΨm is an important marker associated with mitochondrial dysfunction and cell death. We found that Mino induced ΔΨm impairment and nuclear fragmentation in Jurkat ST 2825 in a concentration-depe
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Long term blood pressure regulation is linked to renal
2024-10-30
Long term blood pressure regulation is linked to renal function through the mechanisms of pressure natriuresis (Evans et al., 2005), which has been shown to be modulated by the RAS (Hall et al., 1999). Key components of the RAS are expressed throughout the kidney, and are implicated in renal excreto
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It has been largely demonstrated that several clinico
2024-10-30
It has been largely demonstrated that several clinico-pathological factors influence ovarian cancer patients' prognosis, including residual tumor at primary cytoreductive surgery, FIGO stage, tumor grading, cancer histology and performance status [3,4]. Nevertheless, the recent awareness achieved in
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There are some limitations and further experiments that are
2024-10-30
There are some limitations and further experiments that are required. First, to our surprise, measurement of the cardiomyocyte cross-sectional area in Akt1−/−/iAkt2 KO mice showed comparable areas to WT mouse despite of reduced heart weight. In addition to measuring cardiomyocyte cross-sectional are
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br Translational Considerations Targeting the AHR Pathway Mo
2024-10-30
Translational Considerations Targeting the AHR Pathway Modulating AHR function offers exciting therapeutic potential in host immunity and inflammation. However, the emerging concept of AHR function in a cell type-specific manner, combined with differences between AHR activation in cell culture in
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Perhaps the discovery of this linkage has served to
2024-10-30
Perhaps the discovery of this linkage has served to catapult much of the work on ABCA1, leaving its family member in need of a relationship with a defined human pathology. In this regard, there is by now a quite mature literature that suggests that ABCA2 may have been overlooked in terms of its impo
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In this article we have outlined the
2024-10-30
In this article, we have outlined the increasing, as yet still circumstantial evidence that the 6TM domains of bacterial ACs might operate as receptors for as yet unknown ligands. Intriguingly, several architectural arguments are also applicable to the 6TM domains of mammalian membrane-bound ACs (mA
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Adenosine is an endogenous nucleoside that plays pivotal
2024-10-30
Adenosine is an endogenous nucleoside that plays pivotal roles in different physiological and pathophysiological processes by triggering specific cell-surface receptors both in the CGS 35066 and in the periphery. The adenosine receptors (ARs) are four different subtypes of G protein-coupled recepto
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pkc inhibitor Interestingly a homolog of C
2024-10-29
Interestingly, a homolog of C. elegans acr-23 is present in the A. suum pkc inhibitor (Jex et al., 2011). However, A. suum is not susceptible to monepantel treatment in vivo (Tritten et al., 2011). Our research seeks to advance knowledge on the mode of action of monepantel on nAChRs from Clade III (
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br Viral manipulation of host factors to oppose
2024-10-29
Viral manipulation of host factors to oppose anti-viral autophagy To escape or manipulate autophagy, some viruses developed strategies that are based on the recruitment of host-cell endogenous factors. The non-enveloped double-stranded DNA virus adenovirus is rapidly endocytosed after attachment.
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The mitochondrial protein AIF was
2024-10-29
The mitochondrial protein AIF was the first caspase-independent death effector. AIF can induce caspase-independent chromatin condensation and large-scale DNA fragmentation to approximately 50 KB. AIF that is released to cytoplasm can mediate apoptosis when special extracellular signals trigger the o
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