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The on target in vitro
2020-02-25

The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the su
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Transduction of cellular signals by G protein coupled recept
2020-02-25

Transduction of cellular signals by G protein-coupled receptors (GPCRs) is stringently regulated to prevent the deleterious effects of unrestrained GPCR signaling. The rapid termination of signaling mediated by agonist-occupied GPCRs is referred to as homologous desensitization and involves the foll
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The different diagnostic outcomes of the two assays are
2020-02-25

The different diagnostic outcomes of the two assays are also dependent on the used stimuli. The QuantiFERON-CMV assay targets CD8 + T N6-Cyclopentyladenosine sale by using peptides whereas the T-Track-CMV targets CD4+ and CD8 + T cells by stimulation with two viral proteins [18]. In our study, a sp
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Multivariate models take interactions between cytokines into
2020-02-25

Multivariate models take interactions between cytokines into account and were used to accurately distinguish samples from different time points in pregnancy. The distinction accuracy did not increase with increasing time between the gestational time points, indicating that the cytokine development d
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br Chagas disease and HAT drug
2020-02-25

Chagas disease and HAT drug R&D Drug R&D for Chagas disease and HAT has historically relied on serendipitous findings achieved using low-technology approaches. The absence of biotechnology tools associated and the very limited understanding of the biomolecular processes of the parasites are among
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Furthermore our sample preparation uses a simple isolation
2020-02-25

Furthermore, our sample preparation uses a simple isolation procedure. Numerous CYP450 phenotyping methods employed extensive extraction procedures for sample preparation such as dual liquid extraction or solid phase extraction which are costly and time consuming [10], [17], [18], [19], [20], [23],
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br Materials and methods br Results br Discussion DAS
2020-02-25

Materials and methods Results Discussion DAS and nilotinib, as the second potent, oral generation TKIs, bind to both the active and inactive conformation of the ABL1 kinase domain, have been found to be effective in treating patients with IM resistant or intolerant CML-CP, and inhibit all t
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(±)-CPSI 1306 synthesis br Acknowledgment We thank Prof
2020-02-25

Acknowledgment We thank Professor Yuh-Chang Sun for providing helpful advice and the Ministry of Science and Technology of the Republic of China for financial support (grants MOST ). Introduction Past century has witnessed a tremendous increase in life expectancy of the human population, achi
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Our knowledge of DDR induced signaling
2020-02-25

Our knowledge of DDR-induced signaling pathways is still fragmentary. In particular, we do not know which signaling effectors interact with the phosphorylated receptors and how different effectors are linked to the control of specific cellular functions. The DDRs are at the interface between RTKs an
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The lack of robust immunocompetent animal models permissive
2020-02-25

The lack of robust immunocompetent animal models permissive for HCV makes it hard to assess if the quantity and quality of vaccine-induced immunity is sufficient to confer protection. Thus, it is difficult to predict to what extent antibody responses induced by current vaccination approaches, includ
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br Materials and methods br Results br
2020-02-25

Materials and methods Results Discussion We recently detected phosphorylation of tyrosine Y102 in BPV-1 E2 and reported that FGFR3 binds to E2 and limits E1 dependent viral DNA replication (Culleton et al., 2017, Xie et al., 2017). In the current study, we addressed the potential role of ot
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Hedamycin isolated from Streptomyces griseoruber
2020-02-25

Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of AZD 8055 (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure 3(c)). He
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Previous studies from our lab looked at
2020-02-25

Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to ide
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br Results and discussion br Conclusion In the current study
2020-02-24

Results and discussion Conclusion In the current study, a series of novel ‘open-chain’ classes of E. coli PDHc E1 inhibitors, N-acylhydrazone pyrimidine derivatives A, B, and C were designed and synthesized. As novel ThDP analogs, all A displayed moderate to powerful inhibitory activity with I
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A range of inhibitors were therefore
2020-02-24

A range of inhibitors were therefore synthesized containing either carboxylic Paclitaxel or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively (). Analysis
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