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In HepG cells compound showed inhibition
2023-09-13
In HepG2 cells, vorinostat showed inhibition of total lipid syntheses with an IC of 8μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditions, compound
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br Conflict of interest statement br
2023-09-13
Conflict of interest statement Acknowledgments Introduction Cellular responses to genotoxic stress in eukaryotic cells are coordinated by members of the phosphoinositide kinase related protein kinase (PIKK) family. Two members of this family, Ataxia–Telangiectasia mutated (ATM) and ATM and
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To elucidate whether membrane fluidity changes could impact
2023-09-13
To elucidate whether membrane fluidity changes could impact on signaling pathways, we examined the effects of Rh2 on the activation of Akt, a lipid raft-associated protein kinase, which promotes cell survival and blocks the apoptotic pathways. Upon pretreatment with 5 mM MβCD and in the absence of R
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Kim et al found that hydroxydopamine
2023-09-12
Kim et al. (2013) found that 6-hydroxydopamine (6-OHDA) promoted the atrophy of dopaminergic neurons associated with the activation of poly (ADP-ribose) polymerase (PARP), the translocation of apoptosis inductor factor (AIF) and the depletion of ATP. An increase in p-AMPK and pS6K (upstream kinase o
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Sixth significant progress has been made during the last few
2023-09-12
Sixth, significant progress has been made during the last few years regarding the molecular mechanisms underlying the activation of AMPK and this should aid to develop more potent and specific compounds. Information from crystallographic structures combined with computer-based drug design hold promi
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Cy3-UTP receptor One of the specifications of the NIA AA res
2023-09-12
One of the specifications of the NIA-AA research framework was that it Cy3-UTP receptor be applicable in two distinct research contexts—interventional trials and observational research. In many if not most modern AD interventional trials, individuals are selected for inclusion with the aid of biomar
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br Discussion To our knowledge this is
2023-09-12
Discussion To our knowledge, this is the first case report that demonstrates the presence of a novel T1151K ALK mutation in a patient with disease progression after crizotinib and then ceritinib. As early as 2011, Zhang et al. identified T1151K among other resistance mutations to crizotinib in Ba
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br Conclusions br Introduction During numerous physiological
2023-09-12
Conclusions Introduction During numerous physiological processes, aldehydes are generated from a variety of endogenous and exogenous precursors including amino acids, carbohydrates, and lipids [1]. Most aldehydes are highly reactive and cytotoxic due to the strong electrophilic nature of the t
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br Acknowledgements Dr Paul J Gasser is supported
2023-09-12
Acknowledgements Dr. Paul J. Gasser is supported by the National Institutes of Health (grant number R01DA032895), and the Charles E. Kubly Mental Health Research Center. Dr. Christopher A. Lowry is supported by the National Institutes of Health (grant number R21 MH116263), the Department of the N
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Small RhoGTPases are single domain nucleotide dependent bina
2023-09-12
Small RhoGTPases are single-domain nucleotide-dependent binary switches that act as highly-tuned regulators in signal transduction [1]. The cycling between active GTP-bound and inactive GDP-bound forms allows RhoGTPases to bind to or to dissociate from downstream effectors, respectively [2]. Guanine
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CGP 53353 Toxicity is the main reason for
2023-09-12
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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br Materials and methods br Results
2023-09-12
Materials and methods Results Discussion Fluoride can readily penetrate cellular membranes and seriously damage the structure and physiological function of cells (Zhou et al., 2015). Several studies have shown that excessive fluoride can decrease the viability of cells and that the growth o
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There is a delicate balance between ROS generation and scave
2023-09-12
There is a delicate balance between ROS generation and scavenging by the protective antioxidant defenses in the cell. Antioxidant systems present in the Enasidenib include enzymes like superoxide dismutase (SOD), catalases, glutathione peroxidases (GPxs) and peroxiredoxins (PRxs) (Fig. 3) [38]. SOD
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Pralatrexate In recent years the higher lipophilicity
2023-09-12
In recent years, the ‘higher lipophilicity’-thus-‘better performance’ tenet, derived from the polar paradox theory applied to micro-structured media, was challenged by novel and unexpected experimental results. In particular, the synthesis of many complete series of fatty Pralatrexate esters of nat
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In humans the superior safety
2023-09-11
In humans, the superior safety profile of lipid-associated formulations is characterized by decreased acute infusion-related reactions and dose-related nephrotoxicity, allowing the administration of larger doses and therefore similar efficacy with fewer administrations. In vitro studies and human cl
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