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The liposomes as a FDA approved drug delivery carrier have
2021-05-11
The liposomes, as a FDA-approved drug delivery carrier, have been widely utilized for drug delivery [32], [33], [34]. Liposomes are defined as self-assembled vesicles, which are composed of one or multiple concentric lipid bilayers and enclose an aqueous core. The advantages of utilizing liposomes a
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br Materials and methods br Results and discussion br Conclu
2021-05-11
Materials and methods Results and discussion Conclusions Codon-optimized MGSK-Lys-C was expressed at a high level in an optimized expression system as inclusion bodies. The Lys-C activity reached its maximum with about 9340 nkat/Lculture under standard (chemical) refolding conditions. The r
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It has been reported that the
2021-05-11
It has been reported that the ECD of DDRs require dimerization and/or oligomerization for binding to collagen.,, Here, we have established using SPR that antibody-mediated oligomerization of DDR2-Fc significantly enhances its binding to immobilized collagen type 1. Our results are consistent with ea
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br Materials and Methods br Results
2021-05-11
Materials and Methods Results Discussion Viral infection of eukaryotic Conessine sale activate signaling pathways both via specific interaction with pattern recognition receptors (TLRs, RIG-I, MDA5) and more nonspecific mechanisms such as accumulation of newly synthesized viral glycoprotei
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br Results br Discussion In this paper we present insights
2021-05-11
Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 Donitriptan hydrochloride via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selec
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To ascertain separation of the distinct enzymatic
2021-05-11
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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br Acknowledgments Grant support was provided by
2021-05-11
Acknowledgments Grant support was provided by the Leading Academic Discipline Projects of Shanghai Municipal Education Commission (J5028) (J50201) to Dr. Mi, the China National Science Foundation Project (81072076) to Dr. Mi, the China National Science Foundation Project (31000349) to Dr. Shen, a
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P has three subfamilies CYP CYP and
2021-05-11
P450 has three subfamilies (CYP1, CYP2, and CYP3), which contribute largely to the oxidative biotransformation of xenobiotics that include most drugs, dietary chemicals, and environmental pollutants. The CYP1 enzymes have great importance in the bioactivation of mutagens and its isoforms are capable
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The on target in vitro pharmacology of was then
2021-05-10
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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br Thermodynamic modeling br Selection of data The solutes w
2021-05-10
Thermodynamic modeling Selection of data The solutes were selected based on the set of data needed to evaluate the CPA-EoS for prediction of their solubility in CO2 + cosolvent, as shown in Fig. 1. Critical temperatures, melting temperatures and enthalpies of fusion of the solutes are required
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Coumarins also known as benzopyran ones are a family of
2021-05-10
Coumarins also known as benzopyran-2-ones are a family of nature-occurring lactones first isolated from Tonka beans in 1820. They are an important class of oxygen containing heterocycles widely found in nature, so much so that they have been routinely employed as herbal remedies since early days. Ov
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Interestingly from our consensus SBVC protocol
2021-05-10
Interestingly, from our consensus SBVC protocol only few compounds (less than 150) have been scored with a full ‘ consensus’. That means that these compounds appear in the top 5% of the database when ranked by every scoring function independently. After visual inspection, we have realized that two
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Tacrine amino tetrahydroacridine I Fig was the first AChEI t
2021-05-10
Tacrine (9-amino-1,2,3,4-tetrahydroacridine) (I, Fig. 1) was the first AChEI to be approved by the Food and Drug Administration (FDA) for the treatment of AD [25], [26], [27], [28]. However, despite its good AChE inhibitory activity, tacrine was far from ideal due to its low bioavailability and shor
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Berner et al used a meta analysis to
2021-05-10
Berner et al used a meta-analysis to show that sildenafil resulted in an effect of 9.65-point improvement. Tadalafil could be pooled into an effect of 8.52-point improvement, and vardenafil showed an effect of 7.50-point improvement. In our present studies, 200 mg udenafil resulted in an effect of 8
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Initially studies of GPCRs predominantly assessed the signal
2021-05-10
Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re
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