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Consistent with our previous study Gao et al b
2021-04-28
Consistent with our previous study (Gao et al., 2018b; Wu et al., 2018), we found that TCB-2 disrupted both pup preference and home-cage maternal behavior. Based on the findings that 4-h pup Alsterpaullone sale (a technique presumably increases maternal motivation) failed to attenuate the TCB-2-ind
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Cy5 NHS ester br Materials and methods br Results br Discuss
2021-04-28
Materials and methods Results Discussion DNA-PKcs and the Ku heterodimer (Ku70 and Ku80) constitute the DNA-PK complex, which is a serine/threonine kinase. DNA-PK phosphorylates H2AX and other substrates, such as main NHEJ factors (Artemis, XRCC4, and DNA ligase IV) [4]. Therefore, DNA-PK
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Over the past decade targeting DNA repair proteins has
2021-04-28
Over the past decade, targeting DNA repair proteins has emerged as an effective tool to enhance chemosensitivity of malignant cells [9]. However, identification and selection of the proper target of DNA repair pathways is critical to increase cytotoxic activity of chemotherapeutic agents in cancer c
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As DNA methylation plays a critical
2021-04-28
As DNA methylation plays a critical role in organismic development and human diseases, the interest in DNA methyltransferases is constantly increasing. Extensive studies on the repertoires of dnmts genes have indicated increasing dnmts members in eukaryotes (Goll and Bestor, 2005; Ponger and Li, 200
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Transduction of cellular signals by G
2021-04-27
Transduction of cellular signals by G protein-coupled receptors (GPCRs) is stringently regulated to prevent the deleterious effects of unrestrained GPCR signaling. The rapid termination of signaling mediated by agonist-occupied GPCRs is referred to as homologous desensitization and involves the foll
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Flexible alignment of isopropylphenylaminobenzimidazole with
2021-04-27
Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead Neuropeptide Y 13-36 (porcine) 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well a
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WM refers to the storage of information
2021-04-27
WM refers to the storage of information in the context of processing, and coordination of elements into new structures (Oberauer, Süß, Wilhelm, & Wittman, 2003). Concerning the impact of WM on ISV facets, a strong negative association between WM and ex-Gaussian tau, suggesting that improved WM perfo
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br Materials and methods br Results and discussion br Conclu
2021-04-27
Materials and methods Results and discussion Conclusions In this study, we have investigated the possibility that hierarchical phosphorylation by CK2 may play a role in cellular signal transduction. Hierarchical phosphorylation by CK2 requires multiple consensus determinants with specific s
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br Experimental br Declaration of interest br
2021-04-27
Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR h2 receptor antagonist library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound w
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br Materials and methods br Results
2021-04-27
Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen
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Although the presence of calcium in RHA P
2021-04-27
Although the presence of calcium in RHA-P active site is confirmed by the homology modeling, some additional observations can be made following the metal depletion and reconstitution experiments performed on RHA-Phis. EDTA-treated RHA-Phis recovers its activity in the presence of divalent cations su
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The nuclear receptor NR superfamily of ligand regulated tran
2021-04-27
The nuclear receptor (NR) superfamily of ligand regulated transcription factors has proven to be a rich source of targets for the development of therapeutics for a wide range of human diseases. The NR3B subfamily known as the estrogen-related receptor (ERRα[NR3B1], ERRβ[NR3B2] and ERRγ[NR3B3]) regul
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While previously reported optimizations on compound focused
2021-04-27
While previously reported optimizations on latrunculin focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to explore new
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Based upon these findings on portions A
2021-04-27
Based upon these findings on portions A and B, novel scaffolds of EP4 antagonist, and (R & R=()-Me; =Cl; R=H), shown in , were identified. We next focused on optimizing portion C of these scaffolds. We utilized for an alternative synthesis of nicotinamide scaffold , which is quite effective for
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AZD4547 Interestingly anti inflammatory actions for sPLA V
2021-04-27
Interestingly, anti-inflammatory actions for sPLA2-V were also described in mice a few years ago in a model of autoimmune complex mediated arthritis [148]. A novel mechanism was delineated, whereby sPLA2-V promotes phagocytosis of immune complexes by macrophages to ameliorate inflammation in autoimm
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