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br Reaction mechanism The dissimilarity between monofunction
2021-12-27
Reaction mechanism The dissimilarity between monofunctional and bifunctional glycosylases is that the monofunctional glycosylases removes the substrate base, leaving an intact AP site while the bifunctional glycosylases have an additional lyase activity. This intrinsic lyase activity is present i
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Xie et al b reported that the combination of
2021-12-27
Xie et al. (2009b) reported that the combination of diagnostic ultrasound impulses and cyclic RGD-bearing MBs targeted for GP IIb/IIIa resulted in the successful recovery of epicardial and microvascular blood flow in swine models with acute thrombotic occlusion. It is well known that the stability o
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We noticed that the spontaneous
2021-12-27
We noticed that the spontaneous openings of the D97R α1 GlyR appeared to be quite similar to those elicited by a maximally-effective glycine concentration on wildtype GlyR; both generated similar open and shut dwell-time histograms, both exhibited openings grouped into clusters with Popen values gre
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br Acknowledgments This work was funded by NIH Grant R
2021-12-27
Acknowledgments This work was funded by NIH Grant 2R01 MH066958 (JGT) and NSF CAREER award IOS- 1053716 (NV). We thank Dr. Greti Aguilera for the generous gift of the GRE-Luciferase construct and Dr. Louis Muglia for the generous gift of the GR-GFP construct. Introduction Prostate cancer (PCa
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In Solloway and colleagues reported that mice with alpha cel
2021-12-27
In 2015, Solloway and colleagues reported that mice with alpha cell hyperplasia due to inactive hepatic glucagon receptor signaling may most likely be caused by amino AZD-3463 sale dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of rapamycin
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The effects of GHS R
2021-12-27
The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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Optimization of the tetrahydroindazole series led to the dis
2021-12-24
Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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The release of FBPase and aldolase from
2021-12-24
The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle Clofibric Acid australia was about 6–7 times high
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Sirolimus rapamycin and everolimus both
2021-12-24
Sirolimus (rapamycin) and everolimus, both of which are mTOR inhibitors, are released by commonly used first- and second-generation DES. Considering the relatively high rates of the target vessel failure with currently available DES [12,14,16,45,46], there is a need for a novel drug strategy that pr
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In summary we have designed and explored
2021-12-24
In summary, we have designed and explored synthetic routes towards novel acylsulfamoyl benzoxaborole-based HCV NS3 protease inhibitors. Interestingly, the resulting, unoptimized P1–P3 and P2–P4 macrocyclic inhibitors were equipotent in an enzyme assay and somewhat less potent in replicon assays, com
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It is extremely difficult to predict a
2021-12-24
It is extremely difficult to predict a plausible conformer of hsGCαβ heterodimer with right orientation of multiple domains. Even though the template identities in case of dimeric domains were not high enough but still we modelled the entire heterodimeric structure of hsGCαβ with a reasonable and ju
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monoamine oxidase inhibitor Glutathione transferases EC also
2021-12-24
Glutathione transferases (EC 2.5.1.18; also referred to as glutathione S-transferases, GSTs) are ubiquitous and promiscuous enzymes that catalyze various kinds of reactions involving a wide variety of substrates that are toxic and chemically reactive (Angelucci et al., 2005). The primary function of
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Compound was synthesized in a racemic fashion
2021-12-24
Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position (
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SAR around amino derivative revealed
2021-12-24
SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-po
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Uracil DNA glycosylase UDG is a highly conserved damage repa
2021-12-24
Uracil-DNA glycosylase (UDG) is a highly conserved damage repair enzyme which can specifically recognize and excise uracil residue within the DNA sequences and actuate the DNA 1-Oleoyl lysophosphatidic acid sodium salt excision repair (BER) pathway which keeps the maintenance of genomic integrity a
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