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Various compounds have been designed to inhibit aldose
2023-08-18
Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic Kaempferol moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a po
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In silico docking analysis performed in
2023-08-18
In silico docking analysis performed in the current study indicated that TCDD strongly binds to AhR-LBD. Moreover, the formation of the TCDD/AhR-LBD complex was confirmed experimentally with the use of EMSA. We found that 10nM TCDD after 2 hours of incubation not only bound to the AhR in the porcine
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The AhR molecule is composed of
2023-08-18
The AhR molecule is composed of multiple functional domains [38]. In the N-terminal end, the AhR contains bHLH domain which is involved in DNA binding, dimerization with ARNT and association with chaperone proteins. The PAS domain, which is situated next to the bHLH domain consists of two structural
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br Acknowledgements Dr Paul J Gasser is supported
2023-08-18
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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br Material and methods br Results br
2023-08-18
Material and methods Results Discussion GRK2 activity has increasingly been shown to contribute to the progression of numerous diseases and organ dysfunction [5], [6]. For instance, a large body of work over the last two decades has identified GRK2 as a major regulator of cardiac dysfunctio
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The presence of different LO splice variants
2023-08-18
The presence of different 5-LO splice variants was first demonstrated in human RS-1 tumour cells and in dimethyl sulfoxide-differentiated HL-60 cells [40] and a correlation between the 5-LO splicing pattern and the malignancy of the brain tumours was found. Later, other splice variants were identif
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What can we learn about the anticancer
2023-08-18
What can we learn about the anticancer therapeutic efficacy of Aurora kinase inhibitors from our experience with the Bcr-Abl inhibitors and the long term clinical consequence of their use in treating leukemias? As discussed, all Aurora kinase inhibitors developed to date are ATP-competitive inhibito
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br Results and discussion br Conclusion A series of aminoben
2023-08-18
Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen nor-Binaltorphim
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ATP citrate lyase ACLY is
2023-08-18
ATP citrate lyase (ACLY) is a cytosolic enzyme that catalyzes the generation of acetyl-CoA from citrate [15]. Acetyl-CoA is the building block for the biosynthesis of fatty acids and cholesterol, and also serves as a substrate of the acetylation reaction of various molecules, including histones and
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Receptor Subtypes and Their Function Critical Appraisal Larg
2023-08-18
Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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We designed SSOs that block APP
2023-08-17
We designed SSOs that block APP exon 17 splicing and induce the production of an alternatively spliced APP mRNA lacking exon 17 (APPΔex17). APPΔex17 mRNA encodes an APP protein isoform that lacks 49 Compstatin including the γ-secretase cleavage sites that give rise to the toxic, AD-associated Aβ42
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In summary we identified a novel
2023-08-17
In summary, we identified a novel MLPH-ALK fusion in AST with discordant results of ALK IHC. In order not to overlook ALK-rearranged AST with rare fusion partners on IHC screening, a sensitive IHC method is preferable. Introduction Lung cancer remains the leading cause of cancer related deaths w
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br Aldehyde sensors to monitor substrate
2023-08-17
Aldehyde sensors to monitor substrate levels Previous efforts to ameliorate metabolic diseases frequently relied on biochemical methods which could measure the levels of toxic substrates in 2-Deoxycytidine or bodily fluids (blood and serum or plasma, urine, cerebrospinal fluid). Therapeutic effo
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In addition to it we also showed that glycine increases
2023-08-17
In addition to it, we also showed that glycine increases miR-301a expression which directly binds to PTEN 3′UTR target sites [13]. Glycine confers neuroprotection through microRNA-301a/PTEN signaling in rats cortical neurons in oxygen deprivation model [13]. Substantial studies indicate that inhibit
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Adiponectin also works on AdipoR inducing extracellular
2023-08-17
Adiponectin also works on AdipoR1, inducing extracellular Ca2+ influx necessary for activation of Ca2+/calmodulin-dependent protein kinase kinase (CaMKK)β, AMPK (Fig. 1). This step is then followed by activation of SirT1 and increased expression and decreased acetylation of PPARγ coactivator (PGC)-1
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