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For the SAR optimization of the right
2021-02-12
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic DOI hydrochloride receptor moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introdu
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In the preclinical evaluation of CRF receptor antagonists ef
2021-02-11
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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Flavonoids are most common and
2021-02-11
Flavonoids are most common and widely distributed group of natural phenolic compounds synthesized by plants that have varied effects on mammalian cell systems (Kumar and Pandey, 2013). Several studies demonstrate that flavonoids might be potent inhibitors of several protein kinases involved in vario
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The results of physical parameters of the prepared samples
2021-02-11
The results of physical parameters of the prepared samples are summarized in Table 2. The equivalent diameter ranged from 1.09 to 1.14 mm, which is within the required size distribution of 0.8–1.25 mm. A slight increase in size is probably caused by increasing the thickness of the second coat. To d
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br Discussion EFTs are sarcomas with
2021-02-11
Discussion EFTs are sarcomas with almost undifferentiated histologic features, consequently their differentiation from other small, blue, round cell tumors may be difficult. Substantial intracellular Pexidartinib on PAS stain is a useful diagnostic feature. The addition of CD99 and FLI1 immunohi
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br Physiological roles for EPAC isoforms vascular
2021-02-10
Physiological roles for EPAC isoforms: vascular function The effects of cAMP on limiting vascular endothelial cell (VEC) inflammation and vascular smooth muscle cell (VSMC) proliferation have been well documented 36, 37, 38. However, recent work has demonstrated that several key effects of cAMP i
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Many studies have documented that enolase acts as a plasmino
2021-02-10
Many studies have documented that enolase acts as a plasminogen-binding protein and this interaction is involved in the tissue invasion and pathogenicity of the causative agents (Almeida et al., 2004; Avilan et al., 2000; Marcilla et al., 2007; Mundodi et al., 2008; Vanegas et al., 2007). Furthermo
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In the current study we have elucidated an intrinsic
2021-02-10
In the current study, we have elucidated an intrinsic mechanism by which PD-1 signaling maintains Foxp3 in Tbet+iTreg and iTreg cells. The data presented here demonstrate that PD-1 can inhibit a functional nuclear pool of active asparaginyl endopeptidase (AEP), an endo-lysosomal protease previously
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VU590 hydrochloride The potent estrogen EE induced a
2021-02-10
The potent VU590 hydrochloride EE2 induced a decrease in CYP2C11 activity (reduction in 2α-OH and 16α-OH testosterone) and protein at the 200 ppb dose and in this respect was similar to nonylphenol and genistein. This result agrees qualitatively with the results of Hallstrom et al. (1996) who expos
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The EGFR belongs to the ErbB family of receptor tyrosine
2021-02-10
The EGFR belongs to the ErbB family of receptor tyrosine kinases (RTKs), comprised of four members: EGFR (ErbB1, HER1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4) [24]. HER receptors are activated by a group of epidermal growth factor (EGF) ligands and undergo homo- or hetero-dimerization during th
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Structural characterization of A S Given the
2021-02-10
Structural characterization of A1S_0222. Given the low specific activity of our protein preparations and the considerable problems to concentrate the protein to levels above 2.5 mg/mL, we employed SAXS to structurally characterize and generate a low-resolution model of A1S_0222 in solution. Fig. 5 a
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This hydrophobic biphenyl tail gave good binding affinity fo
2021-02-10
This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC pten inhibitor was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interactions which w
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br Acknowledgement br Introduction Recent developments in ca
2021-02-10
Acknowledgement Introduction Recent developments in cancer immunotherapies have demonstrated durable responses, suggesting that effective immunotherapy would hold promise to improve patient outcome (Gunturu et al., 2013; Hodi et al., 2003; Lutz et al., 2011; Ribas et al., 2009). However, attem
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Considering all these facts in the present study
2021-02-10
Considering all these facts, in the present study, we investigated the effects of two highly selective CRF receptor 2 antagonists (antisavaugine-30, ASV-30; and astressin-2B, AST-2B) on anxiety behavior in rats. The rationale for such an experimental approach was based on the premise that fear and s
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Although CK phosphorylated Msn as
2021-02-10
Although CK2 phosphorylated Msn4 as well as Msn2 (Fig. 1A), the two CK2-dependent phosphorylation sites in Msn2 are not conserved in Msn4. Thus, Msn2 and Msn4 might be differently regulated by CK2-dependent phosphorylation. Msn2 and Msn4, which have 41% identity and similarity in size and amino PD 1
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