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br Conclusions br Conflicts of interest br Acknowledgements
2023-09-18
Conclusions Conflicts of interest Acknowledgements This work was supported by Ege University Research Fund [BAP, 14-ECZ-030, 2016]. Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, sp
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exemplifies three of the compounds investigated in the selec
2023-09-18
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC CHIR-98014 australia 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 p
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Earlier studies showed that exposure of
2023-09-18
Earlier studies showed that exposure of cells to IR caused ATM-dependent phosphorylation of 53BP1, as judged by electrophoretic mobility shift [24], [25], [26]. To date, the only known in vivo 53BP1 phosphorylation site(s) are Ser25 and possibly Ser29 [27]. In the course of our studies, we noticed t
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Second the choice of the PAABD
2023-09-18
Second, the choice of the PAABD is critical for an efficient and sensitive biosensor. The sequence of the PAABD should present high affinity and efficient recognition of the phosphorylated substrate, as opposed to poor affinity for the unphosphorylated substrate, and should display a fully reversibl
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It has been reported that trehalose
2023-09-16
It has been reported that trehalose shows beneficial effects in a mouse model of several neurodegenerative diseases [21], [22], [23]. There are also reports showing that trehalose can improve the impaired cognitive and learning ability and reduced Aβ deposit in hippocampus of APP/PS1 transgenic mice
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Some members from the AAAP family namely the
2023-09-16
Some members from the AAAP family, namely the AUX1 and the LAX proteins, transport auxin instead of amino acids [48]. While there is some structural relationship between IAA and Trp, the substrate recognition characteristics seem different for these proteins: the auxins do not have any amino group o
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br Results br Discussion By using
2023-09-16
Results Discussion By using an unbiased proteomic screen for xCT binding partners, followed by functional validation, we have made the surprising discovery that mTORC2 regulates amino blue nitro sale metabolism in tumor cells by phosphorylating serine 26 of the cystine-glutamate antiporter xC
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Gratifyingly compound also demonstrated improved
2023-09-16
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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AHR mediated MMP upregulation has been shown in response
2023-09-16
AHR-mediated MMP1 upregulation has been shown in response to tobacco smoke [32]. Tobacco smoke contains various AHR ligands such as benzo[a]pyrene. Both benzo[a]pyrene [15] and FICZ [13] are high-affinity ligands for AHR and upregulate CYP1A1 and CYP1B1. FICZ is rapidly degraded by CYP1A1 [20], [33]
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Despite these efforts to prevent oxidative metabolic
2023-09-15
Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of
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In terms of the ring B C
2023-09-15
In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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br Discussion One binding site MB Fig is located
2023-09-15
Discussion One binding site, MB327-1 (Fig. 4) is located in the extracellular domain between the γ and α subunits. MB327 adopts an extended conformation in the MB327-1 site and is oriented parallel to the channel. The second putative binding site, MB327-2 (Fig. 4) is situated deep inside the chan
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br Antioxidative stress and anti inflammation Oxidative stre
2023-09-15
Antioxidative stress and anti-inflammation Oxidative stress is a major cause of reduced endothelial NO bioavailability in hypertension, and inflammatory response is thought to play an important role in these processes (Blake and Ridker, 2001, Landmesser et al., 2006). Reactive oxygen species (ROS
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An AXL decoy receptor with
2023-09-15
An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer cl 2 and a murine breast cancer cell line in grafting assays in mice. The
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In considering the roles of these enzymes
2023-09-15
In considering the roles of these enzymes in normal physiology, given the importance of GLUT4-dependent glucose uptake and glucose-dependent fatty N6-Cyclopentyladenosine synthesis synthesis for systemic metabolic homeostasis (Herman and Kahn, 2006, Herman et al., 2012), deletion of Acly in adipocyt
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