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Activating GSK signaling to inhibit
2020-07-14

Activating GSK3β signaling to inhibit PK signaling during ischemia/reperfusion (I/R) is protective of WM ischemic injury. Glycogen synthase kinase (GSK3), which was the first substrate identified for AKT [44], is inhibited by AKT phosphorylation at positions S9 and S21 [45]. When GSK3β is active, it
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Protein kinase casein kinase CK comprises a family of highly
2020-07-14

Protein kinase casein kinase 1 (CK1) comprises a family of highly related, constitutively active serine/threonine protein kinases (reviewed by [15]). CK1 is involved in controlling a wide variety of different cellular events including protein turnover [16], [17], nuclear import [18] and the cellular
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The reaction of chitosan with DVS should take place primaril
2020-07-14

The reaction of chitosan with DVS should take place primarily through a nucleophilic attack of the vinyl sulfone groups to the amino groups in chitosan [39,50], although its hydroxyl groups can also be involved, as it happens when using agarose [35]. These reactions create very stable secondary amin
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Pyrazolopyrimidines are bioisostere of purine
2020-07-13

Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase Manidipine 2HCl [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour an
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Finally the identification of predictive biomarkers of
2020-07-13

Finally, the identification of predictive biomarkers of response will also allow the more recently discovered CDK inhibitors to be explored in particular genetically-defined contexts, for example by building on recent observations that KRAS mutant tumors are highly sensitive to CDK1 inhibition, and
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Given a disruption of membrane internalization and
2020-07-13

Given a disruption of membrane internalization and an increase in synaptic glutamate receptors in CPG2 knockdown neurons, one might expect an increase in dendritic spine size as membrane continues to be inserted into the spines during receptor exocytosis. However, we observed the opposite phenotype,
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BRCC is the catalytic subunit responsible for
2020-07-13

BRCC36 is the catalytic subunit responsible for the majority of K63-Ub-specific DUB activity in the cytoplasm and in the nucleus as part of two distinct macromolecular assemblies characterized by the presence of either of the MPN– pseudo DUB proteins KIAA0157 or Abraxas (Cooper et al., 2009, Dong et
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br Future perspectives Understanding how peptides are degrad
2020-07-13

Future perspectives Understanding how peptides are degraded, particularly those which may be therapeutically useful, such as GLP-1, has proved to be invaluable in providing a rationale for the development of a novel class of therapeutic agents. However, while DPP-4 plays an important role in the
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Although the formation and toxicity of DPC is theoretically
2020-07-13

Although the formation and toxicity of DPC is theoretically acceptable, it is difficult to evaluate the specific role of DPC and its repair enzyme MGMT in the cytotoxic and mutagenic effects because DPCs are estimated to constitute only 1%–3% of total DNA damage when rat 4 are exposed to bis-electr
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br Protein acetylation Several reports show that MTX
2020-07-13

Protein acetylation Several reports show that MTX is able to induce acetylation of histones and other proteins. Extensive studies have established that histone acetylation is primarily associated with gene activation. Acetylation occurs at lysine residues on the amino-terminal tail of the protein
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To be a qualified non specific CYP inhibitor
2020-07-13

To be a qualified non-specific CYP inhibitor used as an in vitro or in vivo screening tool to distinguish CYP involvement in the overall metabolism, a complete inhibition of the entire metabolism catalyzed by CYPs in a simple experiment is desired. Based on our results, 100 μM atipamezole can comple
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Accordingly we prepared three compounds and
2020-07-11

Accordingly, we prepared three compounds (, , and ) as shown in . Condensation of commercially available cmv virus with glycine methyl ester gave amide . A Friedel–Crafts reaction between compound and 4-methyl valeryl chloride in the presence of aluminum chloride mainly produced undesired compou
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br Acknowledgments br Introduction br Endothelin receptors S
2020-07-11

Acknowledgments Introduction Endothelin receptors Shortly after the discovery of ET‐1, two types of seven transmembrane G protein‐coupled receptors were cloned called endothelin receptor A (ETA) (Arai et al., 1990) and ETB (Sakurai et al., 1990). The affinity of the ETA receptor for ET-3 is
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64c The biological significance of DNA ligases
2020-07-11

The biological significance of DNA ligases is attributed to their function in DNA replication, recombination and/or DNA repair [1], [2]. In vertebrates, three different DNA ligases I, III and IV are recognized. DNA ligase I is essential for the Okazaki fragments’ ligation during lagging-strand DNA s
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Thus RhoA mediated inhibition of
2020-07-11

Thus RhoA-mediated inhibition of DGKθ is a well-characterized pathway, conserved from C. elegans to mammalian tissues, which enables G-protein coupled receptors to regulate the extent and kinetics of DAG-mediated signaling by fine tuning DGK enzymatic activity. Acknowledgments Introduction Ce
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