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br Acknowledgements This work was
2021-05-14
Acknowledgements This work was supported by the National Institute of Neurologic Disorders and Stroke (U54 HD061222, 1K23 NS107646-01, and 1K12NS089417-01), Rocky Mountain Rett Association, International Foundation for CDKL5 Research, the Ponzio Family Chair in Neurology Research, and NHMRC Senio
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br CXCR The CXC receptor and CXCR and
2021-05-14
CXCR1/2 The CXC receptor 1 and 2 (CXCR1 and CXCR2) have been well characterised in vertebrates. In mammals and birds, the two receptors are shared by the ELR+ CXC ligands, namely the CXCL8 family members that have proinflammatory roles in recruitment of neutrophils, monocytes and macrophages to s
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Several studies have described the role of NP
2021-05-14
Several studies have described the role of NP in vRNP nuclear export. For example, leptomycin B (LMB), an inhibitor of the CRM1 nuclear export signal (NES) binding domain (Kudo et al., 1999), inhibits nuclear export of vRNP and NP, but not NEP or M1, in virally infected or transfected clearly (Elto
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br Acknowledgements We are grateful
2021-05-14
Acknowledgements We are grateful to the National Natural Science Foundation of China (Grant Nos. 21571033 and 81503099) and the New Drug Creation Project of the National Science and Technology Major Foundation of China (Grant No. 2015ZX09101032) for financial aids to this work. The research was a
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All of these experiments in GM matter injury
2021-05-14
All of these experiments in GM matter injury models have identified an array of signaling mechanisms that are potentially important. First, Kim et al. proposed that CK2 acts as a negative modulator of NADPH oxidase [55]. Then Blanquet et al. [50] found that increased CK2 correlated with inhibition o
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Therapeutic options targeting intrahepatic resistance are
2021-05-14
Therapeutic options targeting intrahepatic resistance are very limited. Theoretically, the NO-cGMP pathway may be influenced at several sites. Yet, most strategies did not reach clinical practice or yielded disappointing results, such as activators of soluble guanylate cyclase [14], NO releasing der
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The highest concentrations from several tens to often
2021-05-14
The highest concentrations (from several tens to often hundreds or thousands ng/L) are reported in animal farm flush water, and associated runoffs and lagoons in China and in the U.S. Lower concentrations are reported in WWTP influents and effluents. In WWTP influent waters DRO, LNG, NET and PRG hav
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In summary we have identified a series
2021-05-14
In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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Cytidine 5-triphosphate The development and activation of T
2021-05-14
The development and activation of T Cytidine 5-triphosphate play an important role in the progression of atherosclerosis. As for activation and differentiation of T cells, TCR signalling pathway is pivotal. ZAP70 plays a crucial role in formulation of TCR–microclusters, initiation of TCR signalling
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br Target enzyme attributes and substrate peptide selection
2021-05-14
Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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br Materials and methods br Results br Discussion PYR
2021-05-13
Materials and methods Results Discussion PYR-41 inhibits UBE1 activity that catalyses an initial step in the ubiquitination reaction. In the present study, we examined the role of this enzyme in sperm-egg fusion by inhibiting UBE1 enzymatic activity in eggs. Our results suggest that PYR-41
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br Common features of TdT pol and pol TdT pol
2021-05-13
Common features of TdT, pol μ and pol λ TdT, pol μ and pol λ remain in a closed conformation throughout their catalytic cycle, contrary to pol β [24•, 53, 54•]. One possible explanation for this observation is that they have traded fidelity (which requires open-to-closed transition) for a very ti
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Like compound substitution on compound
2021-05-13
Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226.
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br Introduction In mammals there
2021-05-13
Introduction In mammals there are ten known isoforms of the enzyme diacylglycerol kinase (DGK), as well as gene splice variants. Enzymes of this family all have a homologous active site but differ widely in their molecular mass, mechanisms of activation and biological function (Shulga et al., 201
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Besides by substrate and product KSTDs may also
2021-05-13
Besides by substrate and product, Δ1-KSTDs may also be inhibited by other steroids. N. simplex ATCC 6946 Δ1-KSTD was strongly inhibited non-competitively by dicortinone (60), a steroidal dimer, and by bis-1-dehydrodicortinone, with values of 0.7 and 0.75 μM, respectively. This enzyme was also inhib
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