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MTT results show that both pancreatic cell
2021-04-02
MTT results show that, both pancreatic cell lines were quite sensitive to camptothecin (CPT), a well known topoisomerase I poison. Interestingly, CPT does not show any selectivity over cancer cell lines probably due to the duplication times for cancerous (MIA PaCa-2) and immortalized healthy (HPDEC)
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Another question concerns the mechanism of
2021-04-02
Another question concerns the mechanism of PC reduction during the phosphate starvation response. There are at least three main mechanisms of PC depletion: suppression of PC synthesis due to substrate exhaustion, downregulation of PC synthase expression by suppression of gene transcription or intens
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The instructive precedent for galectin phosphorylation is hu
2021-04-02
The instructive precedent for galectin phosphorylation is human galectin-3 (hGal-3). Its serine modification by protein kinase CK1 in the N-terminal tail is relevant for nuclear export during the course of apoptosis regulation and contact formation with the neural cell adhesion molecule L1 , , , . T
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In conclusion our findings suggested that EP receptor activa
2021-04-01
In conclusion, our findings suggested that EP4 receptor activation triggers apoptosis in B-cell lymphoblasts. Our results also showed that EP4 receptor engagement inactivates NF-κB, which, in turn, sensitizes Ramos melatonin receptor agonist to apoptosis induced by chemotherapeutic agents. EP4 rece
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Whichever interactions are formed between the
2021-04-01
Whichever interactions are formed between the DS domains and the collagen ligand, they are expected to lead to structural changes within the DDR dimer that are propagated across the cell membrane to result in DDR autophosphorylation (Noordeen et al., 2006). Tight coupling of the extracellular confor
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During the host response to inflammation inflammatory
2021-04-01
During the host response to inflammation, inflammatory mediators, including release of pro-inflammatory cytokines, have been associated with altered content, expression, and activity of CYP450 enzymes, consequently leading to alterations in the metabolism and elimination of certain drugs. The losses
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The attachment of ubiquitin to RTKs such
2021-04-01
The attachment of ubiquitin to RTKs, such as EGFR, mediates efficient delivery through the endosome-lysosome system for proteolysis. In this way, RTK degradation enables cessation of signal transduction. A recent siRNA screen identified a number of USPs that can significantly modulate EGFR levels an
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The UPP broadly involves proteolysis in biochemical processe
2021-04-01
The UPP broadly involves proteolysis in biochemical processes and is a potential target for cancer therapy. The UPP degrades unfolding or damaged proteins by an ATP-dependent mechanism (Ciechanover, Elias, Heller, Ferber, & Hershko, 1980). It also plays an important role in PPDA regulation, DNA dam
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Upstream Stimulatory Factor USF binding to the E box is
2021-04-01
Upstream Stimulatory Factor (USF) binding to the −65 E-box is required for the regulation of FAS promoter activity in fasting/feeding [97], [98]. DNA-PK are identified as a USF-interacting protein [99]. In response to feeding/insulin, the transient double-stranded DNA breaks occurred during the tran
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br Conclusions br Acknowledgements br Introduction Liver
2021-04-01
Conclusions Acknowledgements Introduction Liver cancer was the fifth most common cancer and the second leading cause of cancer-related death worldwide [1]. Most of primary liver cancers (70–90%) occurring worldwide are hepatocellular carcinoma (HCC) [2]. Persistent hepatitis B virus (HBV) i
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br Regulation of DGK activity Activation
2021-04-01
Regulation of DGK activity Activation of the DGKs is complex and unique for each DGK isotype. In most cases, DGKs must translocate to a membrane compartment to access DAG. However, translocation does not necessarily activate the enzyme [57]. In addition, DGK activity can be modified by other cofa
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Next the BE obtained for the different complexes
2021-04-01
Next, the BE obtained for the different complexes were evaluated. From the BE obtained from our MD simulations, a very good binder can be differentiated from a very weak binder (−11.85 kcal/mol for MTX vs. −6.74 and −3.61 kcal/mol for compounds 14b and 15c, respectively) but ligands with similar bin
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Preparation of the regioisomeric pyridooxazepinones and
2021-04-01
Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and Tarafenacin sale chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a 1
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br Significance Ubl post translational modifications
2021-03-30
Significance Ubl post-translational modifications are potential targets for developing novel therapeutics for life-threatening diseases, such as c-Myc- and KRas-driven cancers that lack targeted therapy. However, only a few drugs are available to target these modifications. This lack of drugs hig
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Results from experiments in model systems have
2021-03-30
Results from experiments in model systems have suggested that the DPRs translated from the HRE of C9ORF72 are toxic and play a role in disease pathogenesis (reviewed in Taylor et al. (2016)). Although the DPRs are present in neurons and glia in various regions of the central nervous system (CNS) ear
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