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Dabrafenib Although effects of low concentrations of
2023-10-30
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major Dabrafenib α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-esterase-inhibiti
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Drug resistance development often involves structurally
2023-10-30
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 apoptosis are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associated
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We conclude that Tetrapleura tetraptera fruits extract
2023-10-30
We conclude that Tetrapleura tetraptera fruits extract possess antiplasmodial activity and the results of this study justifies and confirms the traditional usage of this plant as malarial remedy. Acknowledgement Introduction The phylum apicomplexa comprises of nearly 5000 species, most of whi
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Finally impaired endothelial integrity culminates
2023-10-27
Finally, impaired endothelial integrity culminates in an increased plasma protein concentration in the interstitial space, and thus accumulation of fluid in the ECM, favoring the swelling of the face and limbs [2] mainly. Concurrently with this systemic change, there is intense activation of coagula
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AMPK is a cellular energy sensor that is
2023-10-27
AMPK is a cellular energy sensor that is phosphorylated in response to high intracellular ADP levels to increase GLUT4 translocation into the cell, and subsequently, increase intracellular glucose levels to provide substrate to replenish ATP levels [25]. In metabolic syndrome, sequestration of plasm
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The excellent safety profile of solanezumab and encouraging
2023-10-27
The excellent safety profile of solanezumab and encouraging trends in the exploratory analyses in mild AD led to its inclusion in two secondary prevention trials, which are continuing in the hope that earlier intervention may yield more substantial benefit. The A4 study (NCT02008357) started in Febr
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(S)-Methylisothiourea sulfate There are several reports prov
2023-10-27
There are several reports providing evidences that functional and mechanistic connection between Sirt1 and LKB1/AMPK in metabolic regulation [26], [32], [33]. It has been reported that the deacetylation of LKB1 by Sirt1 is one of the determining factors of the subcellular localization of LKB1. In ag
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Inhibition of autophagy has been shown to alleviate
2023-10-27
Inhibition of autophagy has been shown to alleviate neuronal damage after cerebral ischemia, both in cell culture and rodent models (Koike et al., 2008, Li et al., 2015, Wang et al., 2016, Zhang et al., 2014, Zheng et al., 2014). Therefore, blockage of autophagy is a potential target for prevention
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Liao and van Linden et al
2023-10-27
Liao [47] and van Linden et al. [48] divided the gap between the N-terminal and C-terminal lobes into a front cleft or pocket, a gate area, and a back cleft. The back pocket corresponds to the gate area and the back cleft. The front cleft includes the Gly-rich loop, the hinge, the linker connecting
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Retigabine dihydrochloride synthesis Most of the identified
2023-10-27
Most of the identified aldose reductase inhibitors possess undesirable effects like poor pharmacokinetic properties, hypersensitivity and Steven-Johnson Syndrome [1]. However, the main side effect is the lack of selectivity relative to aldehyde reductase (ALR1, EC 1.1.1.2). ALR1 plays the important
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There is a growing literature on ABCA expression in human
2023-10-27
There is a growing literature on ABCA2 expression in human biopsies, where it has been described as a potential biomarker of leukemias. In childhood T-cell acute lymphoblastic leukemia, ABCA2 and ABCA3 were expressed at high levels, which upon treatment with methotrexate, vinblastine and doxorubicin
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In particular we focused our attention
2023-10-27
In particular, we focused our attention on beta2 adrenergic receptors, since their commercial inhibitors are effective in lowering IOP, the primary indication of glaucoma. The hypotensive action of a commercial sequence of beta2 adrenergic receptor siRNA was tested in rabbits. The results confirmed
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In addition to the above
2023-10-27
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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Further investigations were concerned to study the mechanism
2023-10-27
Further investigations were concerned to study the mechanisms by which GABA modulates adenosine-mediated effects in hippocampal tissue. From these results it can be concluded that endogenous GABA exerts an inhibitory effect through GABAA receptors via a predominant adenosine-mediated action and this
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Introduction Microdialysis is an in vivo
2023-10-27
Introduction Microdialysis is an in vivo-technique which allows continuous sampling of small molecular weight substances (such as neurotransmitters, metabolites and neuropeptides) from the extracellular space of different tissues or organs, e.g. brain, muscle or skin. While the implantation of the
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