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Two additional hydrogen bonds are formed by the substituted
2021-03-22
Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th
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br Loss of Chk sensitizes cells
2021-03-22
Loss of Chk 1 sensitizes inno-206 to hypoxia/reoxygenation In contrast to Chk 2, studies have identified Chk 1 as being phosphorylated in an ATR-dependent manner at residue serine 345 during hypoxia [18]. More recently, siRNA mediated inhibition of Chk 1 signaling was found to sensitize cells exp
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One possible pitfall of using
2021-03-22
One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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The Kaempferia parviflora extract met the
2021-03-22
The Kaempferia parviflora extract met the criteria for a non-competitive interaction with CYP1A1 based on the decrease of Vmax and unchanged Km. The high Ki value and low IC50, as well as the high Km value was indicative of the weakness of the interaction between the Kaempferia parviflora extract an
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br Conclusions When the authors joined the
2021-03-22
Conclusions When the authors joined the field of oxysterol analysis around the turn of the century, oxysterols and cholestenoic acids were mostly considered as uninteresting intermediates of cholesterol metabolism. Some oxysterols had been shown to have biological activity, but the most studied o
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Given the excellent in vitro pharmacology
2021-03-22
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic Cholera Toxin mg functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT
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Herein we report the expression of shrimp Cdk
2021-03-22
Herein we report the expression of shrimp Cdk-2 in hepatopancreas, gills and muscle, finding higher expression in hepatopancreas and gills and lower expression in muscle. No significant changes due to hypoxia and hypoxia reoxygenation were detected on the expression of Cdk-2 in hepatopancreas and gi
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br Conclusion br Conflict of interest br Acknowledgments The
2021-03-22
Conclusion Conflict of interest Acknowledgments The authors extend their appreciation to the Deanship of Scientific Research at King Saud University for funding the work through the research group project No. RGP-120. Introduction Methods Results Conclusions Introduction Pat
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With a favorable spectrum of
2021-03-22
With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
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Some of the psychoactive actions of nicotine
2021-03-22
Some of the psychoactive actions of nicotine are mediated by the nigrostriatal and mesolimbic pathways (Di Chiara, 2000, Di Chiara et al., 2004). The nigrostriatal pathway originates in the dopaminergic neurons located in the substantia nigra and terminates in the putamen and nucleus caudatus which
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Finally the recent work to define the microcircuitry of the
2021-03-22
Finally, the recent work to define the microcircuitry of the central amygdala and the role of specific cell populations in fear conditioning can stand as a useful model for advances in preclinical alcohol research. To date, the role of the amygdala in alcohol-related behaviors, and reward-related be
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Introduction The carnitine choline acyltransferase family is
2021-03-22
Introduction The carnitine/choline acyltransferase family is a family of enzymes that play diverse roles, ranging from (the regulation of) Guanethidine Sulfate and fuel metabolism in mitochondria and peroxisomes to the generation of the neurotransmitter acetylcholine. In mammals, this family consis
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Yang et al investigatedPsoralidin a coumestan derivative
2021-03-22
Yang et al. investigatedPsoralidin 39, a coumestan derivative isolated from the seed of Psoralea corylifolia, regarding its effects on IR-induced pulmonary inflammation. Psoralidin 39 inhibited the IR-induced COX- 2 expression and PGE(2) production through regulation of PI3K/Akt and NF-κB pathway. A
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The small molecule d mannuronic
2021-03-22
The small molecule β-d-mannuronic AT7519 synthesis (M2000), patented (DE-102016113018.4), has been tested as an anti-inflammatory and a novel immunosuppressive agent in various experimental models such as animal models of immune complex glomerulonephritis, nephrotic syndrome, multiple sclerosis and
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The repeat sequence TTAGGG of telomere
2021-03-22
The repeat sequence “TTAGGG” of telomere could be directly recognized by TERF1. TERF1 is indispensable for the maintenance of telomere Fmoc-Arg(Pbf)-OH mg structure and integrity (Tan et al., 2017). Trf1 genetic depletion in vivo induces a persistent DNA damage response and telomere uncapping, which
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