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Glycogen synthase kinase GSK is an evolutionarily
2021-09-07
Glycogen synthase kinase-3β (GSK-3β) is an evolutionarily conserved serine/threonine kinase that plays multifaceted role in diverse cellular and neurophysiological processes [8]. GSK-3β is regulated by inhibitory serine and stimulatory tyrosine phosphorylation on Ser9 and Tyr216 respectively [9]. Dy
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The manuscript provides mechanistic insights into the suppre
2021-09-07
The manuscript provides mechanistic insights into the suppression of EGFR, BCRP, PKM2, and other cancer biomarkers in response to pharmacological inhibition of GPR55 with MNF and CID (Fig. 7). Firstly, inactivation of ERK has been previously demonstrated following treatment of PANC-1 ha 47 mg with
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For the study described herein
2021-09-07
For the study described herein, analogues of CID1792197 (2) were selected for exploration. There are a variety of reasons for this decision. First, the synthetic approach, described hereafter, is modular in nature to rapidly enable the independent modification of either end of the molecule. Second,
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br Materials and methods br Results Using
2021-09-07
Materials and methods Results Using an 84 gene Th1-Th2-Th3 cytokine profile, 17 genes were significantly up-regulated in PBMC one week post-marathon compared to pre-marathon samples (Table 1). Eight genes were down-regulated among various subjects but none consistently enough to achieve statis
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Fig summarizes the underlying mechanism of SB
2021-09-07
Fig. 7 summarizes the underlying mechanism of SB on inhibiting inflammation and maintaining epithelium barrier integrity in the TNBS-induced colitis model. Our findings not only explained the protective effect of SB on colon health, but also provided evidence that GPR109A likely constitutes a valid
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Limited efforts were made to exploit
2021-09-07
Limited efforts were made to exploit the naturally-occurring antigen-specific Treg for ex vivo expansion. This study sets up a reproducible protocol for the expansion of insulin-specific Treg isolated from NOD mice. These cyclic adenosine monophosphate exhibited higher suppressive capacity compared
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Pifithrin-μ receptor Selective pharmacological inhibition of
2021-09-07
Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i
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br Materials and methods br Results br Discussion To
2021-09-07
Materials and methods Results Discussion To the best of our knowledge, the current study presented the first evidence that GPR40, also named FFAR1, played an essential role in bone formation and mediated DMH-1 induced osteogenic effect via Wnt/β-catenin signaling. We found that dose–respon
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The fine interplay among post
2021-09-07
The fine interplay among post-translational modifications and intersection with other pathways, such as PI3K–AKT, has a crucial role in the regulation of GLI activity and in the generation of their repressor forms 40, 41, 42. In addition to β-TrCP, for example, other E3 ligases belonging to the real
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Doxofylline br Conclusion and future directions GS is
2021-09-06
Conclusion and future directions GS is an important therapeutic target for the treatment of Alzheimer's disease. Its structure and function have been studied during the last years to understand the substrate cleavage mechanism to modulate the Aβ42 peptide production. The recent elucidation of GS
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Cys loop GABA receptors are well studied targets
2021-09-06
Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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AZ191 australia We tested formyl MYVKWPWYVWL which we had pr
2021-09-06
We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a max
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VS strategies have been building
2021-09-06
VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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br Results br Discussion In this study six new
2021-09-06
Results Discussion In this study, six new T30695 variants were synthesized with the acyclic R or S glycerol linker instead of Rifabutin unit at 4, 8 or 12 T residue. Based on our previous studies on TBA-GQ, this type of modification should provoke local changes in GQ conformations in the fina
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br Conclusion br Acknowledgements This
2021-09-06
Conclusion Acknowledgements This study was supported by the China Postdoctoral Science Foundation (No.2015M581817), the National Research Council of Science and Technology Support Program (2015BAD03B05-06), and the Priority Academic Program Development of Jiangsu Higher Education Institutions
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