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Several highly potent CysLT receptor antagonists with large
2019-08-22
Several highly potent CysLT1 receptor antagonists with large structural nisin have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thiazoles. O
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Finally the identification of predictive biomarkers of respo
2019-08-22
Finally, the identification of predictive biomarkers of response will also allow the more recently discovered CDK inhibitors to be explored in particular genetically-defined contexts, for example by building on recent observations that KRAS mutant tumors are highly sensitive to CDK1 inhibition, and
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br Effects of estradiol outside the
2019-08-21
Effects of estradiol outside the nucleus are often mediated by classical estrogen receptors Today, it is widely accepted that steroid hormones can signal in ways that do not rely on receptors acting in the nucleus, including activation of receptors localized to the cellular membrane. Rapid effect
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cAMP mediated signaling pathways are important for maintaini
2019-08-21
cAMP-mediated signaling pathways are important for maintaining metabolic homeostasis, and the effects of the glucagon/catecholamine–cAMP–PKA axis on energy balance have been well documented [20]. For example, herpes simplex virus 1 of the PKA 2β regulatory subunit (RIIβ) in mice leads to increased
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Introduction CYP is a superfamily of heme
2019-08-21
Introduction CYP450 is a superfamily of heme-containing monooxygenases, many of which are expressed in the liver, and they are significant phase-I 5959 in drug metabolism and detoxification. There are three subfamilies (CYP1, CYP2 and CYP3) that are mainly involved in the metabolism of drugs in bot
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TRAF and TRAF were initially identified as
2019-08-21
TRAF1 and TRAF2 were initially identified as tumor necrosis factor receptor 2 (TNRF2)-associated components, TRAF4 was overexpressed in breast carcinoma cells, whereas TRAF3, TRAF5 and TRAF6 were discovered by their interaction with specific domains in the cytoplasmic tails of trans-membrane recepto
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HCV has evolved mechanisms to
2019-08-21
HCV has evolved mechanisms to evade humoral immune responses including high functional flexibility and variability of immunogenic portions of its envelope proteins. The highest sequence variability occurs in the first 27 Diclofenac Sodium of the N-terminus of E2, which is referred to as the hyperva
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br Discussion The biochemical separation of exonuclease acti
2019-08-21
Discussion The biochemical separation of exonuclease activity from DNA-PK dependent endonuclease activity reported in this manuscript is consistent with genetic separation of Artemis enzymatic activity. Mutations in the protein which result in disruption of endonuclease activity have no effect on
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Oxamic acid A range of inhibitors were therefore synthesized
2019-08-21
A range of inhibitors were therefore synthesized containing either carboxylic Oxamic acid 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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Calcium dependence of CaM target interaction
2019-08-21
Calcium dependence of CaM/target interaction was analyzed using a titration matrix in which both Ca2+ and CaM concentrations were changed. This gave us access to different parameters characterizing the interaction and namely to the number of bound Ca2+ required for the interaction to occur. Our app
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Interestingly selective ETA blockade increased cutaneous
2019-08-20
Interestingly, selective ETA blockade increased cutaneous blood flow as measured by laser Doppler fluxmetry. This is a measure of total blood flow in the different vessels in the skin including venules, Lamivudine as well as arterioles. This finding is in accordance with the previous demonstration
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Identification of the drug to be used as first
2019-08-20
Identification of the drug to be used as first-step antihypertensive treatment has always been, and remains, a matter of debate. The decision wihich drug (or drug combination) to choose as first-line therapy depend on many variables such as coexisting metabolic disorders, obesity, presence of subcli
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br Methods br Discussion In
2019-08-20
Methods Discussion In a recent survey among 2625 high risk patients on atorvastatin, 10.5% of patients achieved an LDL-target of DBM 1285 dihydrochloride level for improvement of acceptance and adherence to effective lipid lowering therapy are warranted to maximize the benefits of standard t
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NF B is a family of protein mediators
2019-08-20
NF-κB is a family of protein mediators that regulate various innate and adaptive immune responses [29,30]. The NF-κB family consists of the following five proteins: c-Rel (Rel); p65 (RelA); RelB; p50(NF-κB1); and p52(NF-κB2). It has been confirmed that NF-κB is activated by TNF family cytokines, suc
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Cyclosporine NEORAL Oral Solution Novartis is an immunosuppr
2019-08-20
Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na
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