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Finally considering the encouraging inhibitory and selectivi
2020-03-25
Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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To simulate the inhibition of the enzyme by organophosphorus
2020-03-25
To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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The need for dedicated DAPT updates is
2020-03-25
The need for dedicated DAPT updates is well justified by the large amount of data and new information generated in the field over the past few years. As expected, the ACC/AHA and ESC updates contain large areas of overlap as well as some differences. Differences were largely explained by the differe
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The T cell receptor TCR pathway
2020-03-25
The T cell receptor (TCR) pathway is associated with T cell activation and differentiation. When specific antigen peptides are recognized by the TCR, lymphocyte-specific protein tyrosine kinase (lck) phosphorylates the immune-receptor tyrosine-based activation motifs (ITAMs) of the TCR-CD3 complex a
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After activation AKT phosphorylates target proteins involved
2020-03-25
After activation, AKT phosphorylates target proteins involved in cell growth, metabolism and survival (Manning and Cantley, 2007). For example, AKT phosphorylates the pro-apoptotic protein BAD, preventing it from binding to and inactivating Bcl-xL in mitochondria (Datta et al., 1997). In turn, Bcl-x
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Fmoc-Cys(Trt)-ol The liposomes as a FDA approved drug delive
2020-03-25
The liposomes, as a FDA-approved drug delivery carrier, have been widely utilized for drug delivery [32], [33], [34]. Liposomes are defined as self-assembled vesicles, which are composed of one or multiple concentric lipid bilayers and enclose an aqueous core. The advantages of utilizing liposomes a
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In terms of its protease activity MME has a broad
2020-03-25
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other SAG supplier australia of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degrade
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Since the aggregation of neurotoxic forms of A plays a
2020-03-24
Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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In contrast T bet downregulated the
2020-03-24
In contrast, T-bet downregulated the expression of Tfh functional molecules, CD40L, ICOS, and IL-21; accordingly, T-bet overexpression abrogated the helper function of IL-12-stimulated CD4+ T cells. Thus, T-bet seems more involved in the downregulation of the helper functions than in the differentia
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In the present study we used linagliptin
2020-03-24
In the present study, we used linagliptin, one of the commercially available DPP-4 inhibitors, because it has more long-lasting inhibition of DPP-4 activity than other drugs of this class. We hypothesized that linagliptin may interact with intercellular components, not only with DPP-4 on the plasma
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P has three subfamilies CYP CYP
2020-03-24
P450 has three subfamilies (CYP1, CYP2, and CYP3), which contribute largely to the oxidative biotransformation of xenobiotics that include most drugs, dietary chemicals, and environmental pollutants. The CYP1 enzymes have great importance in the bioactivation of mutagens and its isoforms are capable
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Magnetic interactions between metal ions are
2020-03-24
Magnetic interactions between metal ions are usually described by superexchange via intermediate ligands. Although the general principles of the superexchange mechanism are essentially the same for d and f ions, calculations of exchange parameters for lanthanides are more difficult than for transiti
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Epitope analyses of AT AA and ET AA indicate that
2020-03-24
Epitope analyses of AT1-AA and ET-AA indicate that the Aurora Kinase Inhibitor III of both autoantibodies are located at the second extracelluar loop of both receptors. The specific epitopes for both autoantibodies are similar to what was reported previously in a cohort of patients from Brazil [6]
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A summary of the drug CDK hydrophobic
2020-03-23
A summary of the drug-CDK2/6/9 hydrophobic (Φ), hydrogen-bonding (H), and polar-bonding (P) interactions based upon the KLIFS residue numbers is provided in Table 5. The KLIFS system gives comparable residues from different mgmt inhibitor the same value [77], which facilitates comparisons among dif
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Social interaction is known to be the main
2020-03-23
Social interaction is known to be the main source of stress in human beings (Dickerson and Kemeny, 2004, Tamashiro et al., 2005). An animal model of social stress should closely mimic real-life situations in human life (Neisewander et al., 2012); in this context, social defeat in an agonistic encoun
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