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As a sort of proof of concept some clinical
2020-08-03
As a sort of proof of concept, some clinical trials have shown that the down-regulation of the exposure to estrogens, either by using selective estrogen receptors modulators (SERM) or by abrogating the production of estrogens with aromatase inhibitors (AI), relates with a reduction in the risk for b
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br Introduction It has become increasingly
2020-08-03
Introduction It has become increasingly apparent that seemingly identical cells in a population can actually be a heterogenous mixture differing at genome, transcriptome, and/or proteome levels. Analysis of this heterogeneity among cells within a population is critical to provide deeper understan
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br Acknowledgments Research on radical SAM activating
2020-08-03
Acknowledgments Research on radical SAM activating enzymes in the Broderick laboratory is supported by the National Institutes of Health (GM54608). 6-Tuliposides (Pos), the major secondary metabolites in tulip (), are glucose esters of 4-hydroxy-2-methylenebutanoate and (3)-3,4-dihydroxy-2-met
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Future DHODH targeted therapy may be improved by identifying
2020-08-03
Future DHODH-targeted therapy may be improved by identifying patient populations that will be responsive to DHODH inhibition. The recent decrease in the cost of genomic profiling makes effective personalized medicine increasingly feasible and may be used to develop and test biomarkers that predict D
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Over the past decade an increasing number of small molecule
2020-08-03
Over the past decade, an increasing number of small-molecule DGAT-1 inhibitors had been developed with variable structural types.13, 14, 15 Most (Fig. 1) share a privileged structure with the heteroaryl-linker-acid, which is based on compounds 1 and 2 described in the early patents of Japan Tobacco
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brucine As hydrophobic residues make up
2020-08-03
As hydrophobic residues make up almost 40% of all the residues in the DGAT1 proteins [74] (Fig. 2a and c), they presumably play an important role in facilitating the reaction. While it is clear that alterations within the Sit1 motif, especially of the critical tyrosine (Y), alter binding to oleoyl-C
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As it was recently found native
2020-08-03
As it was recently found [28], native α-synuclein interacts with anion-binding groove between O and R (or P and Q) subunits of GAPDH which comprises NAD+-binding pocket and active site (Fig. 2A). In all 10 simulations, α-synuclein bound to this region of GAPDH (Fig. 2D, E). The following GAPDH resid
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DDRs a novel subfamily of
2020-08-03
DDRs, a novel subfamily of receptor tyrosine kinases, were discovered during the search for tyrosine kinase proteins expressed in human malignancies 5, 6. DDRs can modulate cell responses such as adhesion, migration, differentiation, survival and proliferation, in response to the changes in the amou
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As the IC substitution pattern trimethoxybenzene was found
2020-08-01
As the IC261 substitution pattern (2,4,6-trimethoxybenzene) was found to be important for the activity, it was systematically varied into 2,3,4- and 3,4,5-trimethoxybenzene (, ). These two derivatives also exert a significant k145 in total Aβ. Although the o-positions of (Aβ=54%, Aβ=72%, Aβ=65%) are
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jlk br Materials and methods br Results br Discussion
2020-07-31
Materials and methods Results Discussion The study assessed the in vitro and in vivo effects of D. tripetala and A. melengueta extracts on CYP450 3A isoenzyme. The result indicated inhibitory activity of the extracts on the enzyme. Some constituents of herbal extracts have been shown to alt
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While a number of studies have helped elucidate the
2020-07-31
While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub Thiolutin specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-RING interface in governing subst
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For C NNC Abi Dargham
2020-07-31
For [11C]NNC 112, Abi-Dargham et al. performed a test-retest study using arterial input function and kinetic modelling using the 2-tissue compartment model (2TCM) [30], evaluating a range of different outcomes measures. The test-retest variability for most parameters were similar for striatal and co
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In conclusion our results show
2020-07-31
In conclusion, our results show that the interaction between the level of hearing loss and the COMT Val158Met polymorphism can increase the susceptibility to the clinical manifestation of tinnitus. We demonstrated that the PHC becomes involved in tinnitus in patients with hearing loss that are Met c
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In this study we examined the role
2020-07-31
In this study we examined the role of a well characterized genetic polymorphism in the COMT gene in mediating cognitive antipsychotic treatment effects in first episode psychosis (FEP). We considered catechol-O-methyltransferase (COMT) to be a potentially important baseline consideration in a pharma
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The structures of OGT substrate complexes
2020-07-30
The structures of OGT substrate complexes showed that peptide backbones of glycosylation and cleavage substrates are superimposable (Figure 2b right panel). Combined with biochemical evidence consistent with a reaction mechanism involving a glutamyl ester, the structural evidence suggested that HCF-
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