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Classical DHFR inhibitors such as methotrexate MTX
2021-04-17
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino L 006235 residues as well as hydrophobic in
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In a study on the time course of
2021-04-17
In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve
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We further correlated OPRK and
2021-04-17
We further correlated OPRK1 and OPRM1 methylation levels with individual characteristics in Xinjiang Han and Uygur controls. Partial correlation analyses showed that OPRK1 methylation was positively correlated with age in Uygur male controls (r=0.72, p=0.001, adjusted by body mass index (BMI), gluco
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System Analysis and Modeling In this work
2021-04-16
System Analysis and Modeling - In this work, a three-level hierarchical modeling – composed by combinatorial and state-space models – is used: (1) First, failure rates () of TMS servers subsystem units are estimated through continuous Markov chains; (2) Then, the single server 3'-O-(2-nitrobenzyl)-2
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T7 High Yield Cy5 RNA br Conflict of interest statement br A
2021-04-16
Conflict of interest statement Acknowledgements Introduction Spending their last days on earth having already lost many cognitive functions remains a major fear of elderly people. Although during the last century their lifespans increased, the so-called “old-age diseases” became more and mo
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br Acknowledgements br Introduction Protein tyrosine phospho
2021-04-16
Acknowledgements Introduction Protein–tyrosine phosphorylation, catalyzed by protein–tyrosine kinases and protein–tyrosine phosphatases, has a pivotal role in the regulation of a wide variety of cellular processes. Similar numbers of tyrosine kinases and tyrosine phosphatases are encoded by th
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Acidosis has lethal consequences but alkalosis due
2021-04-16
Acidosis has lethal consequences, but alkalosis (due to chloride depletion, potassium depletion, and excess mineralocorticoid) is not tolerated as well (Luke and Galla, 2012). In this regard, efforts to restore pH to normal physiological level, in the most benign way should be the goal of researcher
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On the opposite side sPLA X has
2021-04-16
On the opposite side, sPLA2-X has also been implicated in the pathology of cancer [167,168]. Human sPLA2-X induces lipid droplet formation in Ras-driven MDA-MB-231 triple-negative breast cancer RWJ 56110 and promotes their survival during nutrient stress. It acts through the products of its enzymat
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br Material and methods br Results br Discussion A
2021-04-16
Material and methods Results Discussion A. fumigatus utilizes several virulence factors that facilitate its establishment in human hosts. Among these factors, the best known are hydrolytic enzymes such as proteases and phospholipases, toxins, melanine and catalases that neutralize the react
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hqn australia In conclusion this study indicated that
2021-04-16
In conclusion, this study indicated that D. tripetala and A. melengueta extracts inhibited CYP 3A enzyme both in vitro and in vivo. Although these inhibitions may appear to be weak from the US FDA classification point of view, caution must be applied in the concurrent use of herbal preparations cont
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br Conflicts of interest br Acknowledgements This work was s
2021-04-16
Conflicts of interest Acknowledgements This work was supported by the Swiss National Science Foundation No 31003A-179400 to AO. We thank Dr. Thierry Langer, University of Vienna and Inte:Ligand GmbH, for providing the LigandScout Software, and Dr. Daniela Schuster, Paracelsus Medical Universit
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These studies established IAP proteins as dimeric
2021-04-16
These studies established IAP proteins as dimeric RING E3 ligases, but did not account for the essential role of dimerization. In IAPs and related E3s, such as RNF4 and MDM2, dimerization not only depends on contacts from the core RING domain but also residues N- and C-terminal to the RING domain (B
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The modification of proteins with the small amino acid
2021-04-16
The modification of proteins with the small 76-amino Carbenoxolone disodium protein ubiquitin (Ub) plays a central role in many key cellular processes. Ubiquitylation of a target protein requires the concerted action of a cascade of three enzymes (Figure 1). The ubiquitin-activating enzyme (E1) cata
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br Acknowledgments Studies in the Tomkinson
2021-04-16
Acknowledgments Studies in the Tomkinson laboratory on DNA ligase III are supported by research grants from the National Institutes of Health (P01 CA92584 and ES12512 to AET), a grant from the V Foundation and the University of New Mexico Cancer Center. Introduction Ionizing radiation (IR) as
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Predictions of enzyme topology for
2021-04-15
Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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