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For the current studies we used
2020-03-25
For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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In the present study we investigated
2020-03-25
In the present study, we investigated the deeper role of eNOS in the pathogenesis of nasal polyps and analyzed the influence of 1,8-cineol on nasal polyp gene and protein expression of eNOS in vitro. Different studies dealt with the localization and expression of eNOS in nasal polyps and nasal mucos
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A summary of the drug CDK hydrophobic hydrogen
2020-03-24
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 beta lactamase the same value [77], which facilitates comparisons among diff
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Given the excellent in vitro pharmacology
2020-03-24
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic hmg-coa reductase functionality of 1. Acetonitrile 49 was found to have a good balance of DG
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There is literature precedence for the metabolic
2020-03-24
There is literature precedence for the metabolic activation of the methylene carbons adjacent to the ring oxygen(s) of dioxanes and benzopyrans resulting in ring-opened electrophilic carbonyl species. Based on the potential for this metabolic pathway being operative with , a steric block approach wa
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Cyclosporine NEORAL Oral Solution Novartis is an immunosuppr
2020-03-24
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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PHA 543613 hydrochloride Introduction Excessive exposure to
2020-03-24
Introduction Excessive exposure to ultraviolet (UV) irradiation from the sun injures human skin, which might lead to premature aging and skin pathologies [1], [2]. Chronic exposure to UV (especially ultraviolet-B, UVB) irradiation could profoundly affect the skin epidermis, interfering with the ker
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The cholinergic system has been shown to play a
2020-03-24
The cholinergic system has been shown to play a role in regulation of the inflammatory response [13] as well as in the influence of the metabolism of PCa cells [14]. The reduced activity of cholinesterase (ChoE) and the consequent increased amount of FSLLRY-NH2 has been shown to lead to a cholinerg
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The first example of a broadly
2020-03-23
The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth
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valdecoxib NMR was employed for the determination of un liga
2020-03-23
NMR was employed for the determination of un-ligated domain 1 structure of DDR2 receptor. The collagen-binding site on the same was identified by cross saturation experiment and mutagenesis [40]. Birgit leitinger identified the binding site of collagen with DDR2 receptor, which was three spatially a
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At the cellular level TGF has been involved in the
2020-03-23
At the cellular level, TGF-β1 has been involved in the formation of invadosomes (Mandal et al., 2008, Varon et al., 2006). Invadosomes are actin-based structures involved in matrix degradation and cell invasion through metalloproteinases (MMP) activity (Linder et al., 2011). Invadosomes, constitutiv
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br Cyclin dependent kinases control more
2020-03-23
Cyclin-dependent kinases control more than cell cycle CDKs’ roles conducting the concert of NVP-ADW742 was first revealed in the context of the tumor suppressor Rb, phosphorylation of which by CDK4 or CDK6 inactivates it loosing the transcription factor E2F [1], [12], [15]. Discovery of other cyc
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To ascertain separation of the distinct enzymatic activities
2020-03-23
To ascertain separation of the distinct enzymatic activities found in this protein preparation following separation on the HAP column, a rigorous quantitative analysis was conducted on the nickel–agarose elution and HAP FT pools of protein. For these analyses, each pool of protein was dialyzed in th
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NMR was employed for the determination
2020-03-23
NMR was employed for the determination of un-ligated domain 1 structure of DDR2 receptor. The collagen-binding site on the same was identified by cross saturation experiment and mutagenesis [40]. Birgit leitinger identified the binding site of collagen with DDR2 receptor, which was three spatially a
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br Conclusions The present study demonstrated that CuE posse
2020-03-23
Conclusions The present study demonstrated that CuE possesses strong hepatotoxicity. CuE is not only a mechanism-based inhibitor of human CYP3A4, but also inhibits P-gp activity in vitro. In whole animal studies, CuE induces CYP3A and P-gp after a long-term treatment but inhibits the activities o
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