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br Results br Discussion Adaptive drug resistance is
2019-12-17
Results Discussion Adaptive drug resistance is a major challenge to the clinical success of cancer therapies. Incomplete inhibition of oncogenic signaling allows survival of “drug-tolerant” tumor cells, which persist in that state for variable periods before acquiring additional genetic mutati
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In conclusion we designed novel E inhibitors
2019-12-17
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,
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Plasminogen is composed of five N terminal kringle domains a
2019-12-17
Plasminogen is composed of five N-terminal kringle domains and a C-terminal serine protease domain. The kringle domains have an affinity to lysine and binding of plasminogen with its receptors is dependent on its lysine interacting kringle domains [10], [28]. In the current report, we show that enol
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In conclusion we demonstrate that
2019-12-17
In conclusion we demonstrate that infection of salmon cells with ISAV induce the main branches of the cellular UPR machinery, but also one of its main negative regulators, GADD34. This is probably important for maintaining translation of interferon and interferon stimulated genes (ISGs), keeping ISA
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br A brief introduction to DUBs The reversal
2019-12-17
A brief introduction to DUBs The reversal of ubiquitin conjugation of targeted proteins relies on deubiquitinating Terbinafine synthesis (DUBs), which catalytically cleave single Ub or poly-ubiquitin chains from proteins. The human genome encodes approximately 100 potential DUBs which can be cla
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N Cyclopentylmethyl analog exhibited fold
2019-12-16
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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br Discussion Although DNA has
2019-12-16
Discussion Although DNA has a limited chemical stability it has long been known that DNA in blood stains may remain relative stable for weeks, months, or even years at ambient temperature,1, 2, 3, 4, 5, 6 and samples (e.g., reference samples) that have been transferred to a matrix, e.g., FTA® pap
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Some mechanistic experiments performed in the early s
2019-12-16
Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects Annexin V-Cy5 Apoptosis Kit synthesis from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-indu
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Although it is believed that CYP
2019-12-16
Although it is believed that CYP induction is regulated in humans in principle in the same fashion as in animals, some species differences in CYP3A enzymes induction were observed. Rifampicin is known to be a potent inducer of CYP3A4 in human hepatocytes, whereas pregnenolone-16α-carbonitrile (PCN)
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Mechanistically GW treatment modulated cytokine expression w
2019-12-16
Mechanistically, GW2580 treatment modulated cytokine expression within the kidney. We noted a decrease in the levels of TNF, MCP-1, IL-1β, IL-27, and GM-CSF in GW2580 treated mice. Decreased levels of these proinflammatory cytokines likely contributed to the attenuated proteinuria and improved renal
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Acknowledgments br PGD is an
2019-12-16
Acknowledgments PGD is an arachadonic acid-derived prostaglandin produced in large quantities when asthmatic lung tissues are challenged by allergens. PGD contracts the airway tissue as well as stimulating an inflammatory response. PGD was also found to be the ligand for a second receptor, DP2 (
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Cardiogenesis is enhanced with timely applicati http www ape
2019-12-16
Cardiogenesis is enhanced with timely application of Wnt pathway activators and inhibitors. A combination of Wnt/β-catenin signaling pathway activators such as CHIR99021 and inhibitors such as IWP-2 and IWR-1 have been found to be highly efficient cardiomyocyte differentiation protocols [27], [28].
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br Conclusion In conclusion our findings do not
2019-12-16
Conclusion In conclusion, our findings do not suggest that HT is an important determinant of future AD risk and are in line with a recent Cochrane review stating that HT is not indicated for preventing dementia or cognitive decline in postmenopausal women [13]. Contributors Conflict of inte
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Omaveloxolone Given that dimethylamine substitution was tole
2019-12-16
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated Omaveloxolone amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). The
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For these reasons molecules of the ET
2019-12-16
For these reasons, molecules of the ET family and in particular ET-1 are considered useful factors in the evaluation of malignancy and in consequence, in the prognosis for several forms of neoplasia, such as ovarian (Bagnato et al., 2005), prostate (Nelson et al, 1995, Nelson et al, 1996), colorecta
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