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We used the lead compound
2024-07-29
We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system. E
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The downstream targets of ATR involved in mediating human te
2024-07-26
The downstream targets of ATR involved in mediating human telomerase recruitment have not yet been identified. Under stalled fork conditions, activated ATR is able to phosphorylate and activate ATM (Stiff et al., 2006, and Figures 4C and 4D); whether this Bax channel blocker of ATM participates in a
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Several structural classes of ASK inhibitors mostly from
2024-07-26
Several structural px12 of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead revealed
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CORT induced hippocampal damage has been implicated
2024-07-26
CORT-induced hippocampal damage has been implicated in depression, aging and long-term glucocorticoid therapy. Therefore, finding a drug that can protect hippocampal neurons from the adverse effects of CORT could have significant clinical benefits. In this regard, we tested the potential protective
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br Materials and methods br
2024-07-26
Materials and methods Results A first series of experiments explored whether the Ampkα1 isoform is involved in the regulation of cardiac Pkcζ. To this end, HL-1 cardiomyocytes were transfected with a construct encoding constitutively active Prkaa1T183D (CAα1) or with the empty vector as contro
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br MADS box proteins in
2024-07-26
MADS box proteins in plants, a flourishing family In contrast to animals, homeotic genes in plants do not code for homeodomain-containing proteins, but rather, in almost all cases, for MADS domain proteins. The sequencing of the genome of Arabidopsis thaliana revealed more than 100 putative MADS
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Fish aminopeptidases from Alaska Pollack roe
2024-07-26
Fish aminopeptidases from Alaska Pollack roe and tuna pyloric caeca have been reported on [12,13]. More recently, we described the purification of a leucine aminopeptidase from the skeletal muscle of the common carp [14], red sea bream [15] and a lysine aminopeptidases from Japanese flounder [16]. T
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A key building block in MT SGL
2024-07-26
A key building block in MT-SGL is the computation of the proximal operator in (12) when is the multi-task sparse group lasso regularizer given byFor MT-SGL, the iterates x ≡ Θ are matrices, and the proximal operator is computed at z ≡ Z = Θ + α(Θ − Θ). For the loss function L(·) corresponding to Gau
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Growing evidence indicates that GRKs can
2024-07-26
Growing evidence indicates that GRKs can exert different effects within the cell depending on the stimulus, cell type, and localization [97], [121]. In this sense, we were the first to demonstrate a mitochondrial localization for GRK2 [122], later confirmed by other investigators [123], establishing
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Based on the improved characteristics of the
2024-07-25
Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun
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BQ-788 sodium salt sale Based on the observation that antips
2024-07-25
Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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exemplifies three of the compounds investigated in
2024-07-25
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC Fmoc-Lys(Dnp)-OH 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 produ
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The protective role of HMW HA in
2024-07-25
The protective role of HMW-HA in inflammatory diseases and pulmonary damage led us to investigate whether PM2.5-induced ALI could be attenuated by HMW-HA and the underlying mechanisms. In this study, we used a rat model to evaluate the effect of HMW-HA on pulmonary histology, lung inflammation, oxid
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Despite these conflicting data about COX ER correlations a l
2024-07-25
Despite these conflicting data about COX-2/ER correlations, a large body of evidence supports that elevated COX-2 expression in breast cancer is a constant feature of high stage disease and a predictor of worse outcome. Upregulation of COX-2 protein has been identified in approximately 40% of cases
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Bran is a byproduct of flour milling
2024-07-25
Bran is a byproduct of flour milling, typically utilized as a valuable component of animal feeds. Because of its attractive technological and health-promoting properties, it topotecan has also been increasingly used in food manufacturing as a source of dietary fiber. Indeed, with the growing intere
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