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Increased knowledge about CRC pathogenesis has provided new
2020-01-21
Increased knowledge about CRC pathogenesis has provided new and remarkable treatments beyond the classical options of surgery, radiation and chemotherapy [11]. Despite these advances, chemotherapy remains the most important element of anti-cancer therapy. Chemotherapy, when initiated, is generally e
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Cytochromes P CYP are a superfamily of hemoproteins containi
2020-01-21
Cytochromes P450 (CYP 450) are a superfamily of hemoproteins containing a heme cofactor, which are widely distributed in animals, plants and microbes (Hannemann et al., 2007). CYP450 exhibits a variety of biological functions including biotransformation of drugs, detoxification of endogenous and xen
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Moreover a ligand for fusin has recently been
2020-01-21
Moreover, a ligand for fusin has recently been found: the lymphocyte chemoattractant stromal-derived factor-1 (SDF-1) binds to CHO dpp-4 inhibitors transfected with fusin and promotes secondary messenger production (Bleul et al., 1996; Oberlin et al., 1996). A new name, CXCR-4, has been proposed fo
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Next we evaluated the therapeutic potential of compound usin
2020-01-21
Next, we evaluated the therapeutic potential of compound () using the mouse model of collagen-induced arthritis (CIA model), which is the pathological model for RA. Consequently, oral once-daily dosing of 3 mg/kg reduced the overall progression of the clinical score, including inflammation and bone
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With the narrow SAR of the tail
2020-01-21
With the narrow SAR of the tail favouring the ortho sulfone group, we examined the remaining position open to substitution at the pyrazole 3-position, in an attempt to at least moderate the excessive human PPB (). Lipophilic groups in this position maintained huge shifts in potency in the absence or
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After repeated intermittent exposure to a psychostimulant an
2020-01-21
After repeated, intermittent exposure to a psychostimulant an augmentation of drug response to motor activity is commonly observed, a phenomenon known as behavioral sensitization (Kalivas and Stewart, 1991, Steketee and Kalivas, 2011). On the other hand, several reports have pointed out that stress
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Alternatively procedural factors may have contributed to the
2020-01-21
Alternatively, procedural factors may have contributed to the conflicting results. For instance, in order to have a more circumscribed area of drug diffusion, a volume of 0.05μl was injected in experiment 1b, which is four times lower than the one used in the mentioned plus-maze investigation. Besid
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Another question concerns the mechanism of PC reduction
2020-01-21
Another question concerns the mechanism of PC reduction during the phosphate starvation response. There are at least three main mechanisms of PC depletion: suppression of PC synthesis due to substrate exhaustion, downregulation of PC synthase expression by suppression of gene transcription or intens
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The proposed FDIR technique is presented in the following fo
2020-01-21
The proposed FDIR technique is presented in the following format: Section 2 contains a survey of typical orbits of interest with regard to the lcq environment found in them, which is contrasted with a LEO orbit. Additionally, how the requirements for the satellite system can be estimated is presente
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br COTSget based Architectures This section describes how ou
2020-01-21
COTSget-based Architectures This section describes how our COTSget-based architectures are defined. We use a design inspired by MDE to build a Domain-Specific Language (DSL) of the architecture, as can be seen in the metamodel of Fig. 3. This metamodel defines the abstract syntax of our DSL and i
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Dose response analysis Fig can be performed on
2020-01-21
Dose response analysis (Fig. 2) can be performed on Ruxolitinib phosphate in culture, in tissue, in animals or even in patients. Many different responses can be measured, including mRNA levels, reporter gene activity, gene product (e.g. enzyme) activity or even physiological functions such as inhibi
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br Additional CDKs with a
2020-01-20
Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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It is interesting that of
2020-01-20
It is interesting that of the control groups, female TG controls only had significantly higher MB-COMT protein than non-TG male controls (Supplemental Table 9, P = 0.005), while these two groups have almost equal expression of S-COMT protein (8.54- vs. 8.34-fold) and their COMT enzyme activity is al
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br Materials and methods br Results br Discussion
2020-01-20
Materials and methods Results Discussion Inflammatory signalling and in particular the arachidonic Go 6983 cascade have been suggested as targets for disease modification, optimization of the therapeutic response, and even restoration of pharmacosensitivity (Potschka, 2010). Recently, we d
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Within the X CX PX RX motif of several prokaryotic
2020-01-20
Within the X1CX3PX5RX7 motif of several prokaryotic FGE substrates, the residues of X3, X5, and X7 are variably found as mixtures of alanine, glycine, threonine, or serine residues [26], [27]. The docked model of our identified HCTPRRP motif revealed that position X1 (H1) and position X7 (P7) were n
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