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Molecular modelling studies were performed on the hDHFR inhi
2020-07-13
Molecular modelling studies were performed on the hDHFR inhibitors identified (1, 11, 13, 14, 16, 25 and 32) to explore the structural basis of the interaction between the mentioned compounds and the human enzyme. The docking studies were performed using the X-ray crystallographic structure of the h
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br NADH and NADPH Turnover and the
2020-07-13
NADH and NADPH Turnover and the Putative Role of Alternative NAD(P)H Dehydrogenases Still very little is known about the metabolic function of external and internal alternative NADH:UQ oxidoreductases, and almost nothing is known about the mechanisms underlying their metabolic regulation, especia
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Cysteine protease activities have been suggested
2020-07-13
Cysteine protease activities have been suggested to be important for Giardia’s pathogenesis [[11], [12], [13],16,18,19,21,28,29,35]. Recently several giardial CPs were shown to be released during host cell interactions [9,10]. The three major released CPs have recently been shown to be involved in t
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br P Y receptor structure br Pharmacology Several
2020-07-13
P2Y receptor structure Pharmacology Several subtype selective compounds have been developed in recent years (Jacobson and Müller, 2016; Rafehi and Müller, 2018). These compounds are helpful tools for analyzing the roles of P2Y receptor subtypes in physiology and pathophysiology. The present ar
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A cocktail approach can detect the
2020-07-13
A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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br Conclusion In vivo pharmacokinetic studies showed
2020-07-13
Conclusion In vivo pharmacokinetic studies showed that dasatinib monohydrate pretreatment significantly decreased the blood level of CsA in rats, which was most probably due to the induction of CYP3A2 isoenzymes. The nilotinib pre-treatment had no significant effects on cyclosporine pharmacokinet
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Several extragenic cot ts suppressors
2020-07-13
Several extragenic cot-1 (ts) suppressors have been identified. Among them, cytoplasmic dynein, dynactin, and nuclear distribution mutants of N. crassa, as well as an additional gene gul-1 (NCU01197), have been shown to have genetic interactions with cot-1 (Bruno et al., 1996, Seiler et al., 2006, T
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The following are the supplementary data related
2020-07-11
The following are the supplementary data related to this article. Acknowledgments Introduction Drug-resistant epilepsy (DRE) occurs in approximate 30% of patients who suffer from epilepsy [1]. Temporal lobe epilepsy (TLE) is one of the most common partial seizures and the common cause of DRE
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br Materials and methods br
2020-07-11
Materials and methods Results Discussion COX-2-mediated production of PGE2 is involved in cell growth and metastasis of many cancers. Previous studies indicated that COX-2 was overexpressed in many cancer tissues and that PGE2 increased cancer cell growth, a process that could be suppressed
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mk 801 DGK is highly expressed in
2020-07-11
DGKδ is highly expressed in skeletal muscle [7], which is a primary target of insulin for glucose disposal [14]. Notably, Chibalin et al. reported that DGKδ contributes to hyperglycemia-induced peripheral insulin resistance and that decreased protein levels of DGKδ in skeletal muscle attenuated gluc
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br E E backside interaction The
2020-07-10
E3–E2 backside interaction The E2 possesses an important regulatory interface which is termed its backside as it is opposite to the catalytic cleft that bears the active-site cysteine forming the thioester with SUMOD. This backside site interacts noncovalently with a scaffold SUMOB and was origin
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The combination of brequinar and fluorouracil FU has been
2020-07-10
The combination of brequinar and 5-fluorouracil (5-FU) has been evaluated to assess whether brequinar-induced uridine depletion would improve 5-FU activity. In cells, 5-FU is metabolized into FdUMP and inhibits thymidylate synthetase, which catalyzes the formation of thymidine monophosphate from deo
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The following is the supplementary data
2020-07-10
The following is the supplementary data related to this article. Funding This work was supported by departmental funding to Prof. Mühl. Funding derived from the State of Hessia to the Institute of General Pharmacology and Toxicology at the pharmazentrum frankfurt (Head: Prof. Josef Pfeilschifter
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To characterize Ea and S DC AC electrical parameters will
2020-07-10
To characterize Ea and γ·S, DC/AC electrical parameters will be determined from MIL standard measurements in a temperature range of −55 to +200°C. It is therefore necessary also to characterize the junction temperatures and hot points by infra-red or electrical method. The accelerated aging, represe
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Another potential source of variable affinities is inherent
2020-07-10
Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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