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The data from drug screening in P berghei Fig
2021-07-07
The data from drug screening in P. berghei (Fig. 3D) provide proof of concept that chemogenomic profiling can be accomplished in P. berghei in the same manner as P. falciparum, in that significant increases in the EC50 ratio were found only for antifolate drugs in the parasite with attenuated TgDHFR
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Epoxomicin Introduction DHFR is an important enzyme
2021-07-07
Introduction DHFR is an important enzyme in both mammals and microorganism including Mycobacterium tuberculosis (Mtb). It catalyzes folic Epoxomicin conversion to dihydro and tetrahydro folic acid which is a crucial step in folate pathway [1]. Inhibition of folate pathway leads to interruption of t
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DAPK is a kD Ca calmodulin CaM regulated Ser Thr
2021-07-07
DAPK is a 160-kD Ca2+/calmodulin (CaM)-regulated Ser/Thr kinase that mediates cell death. The activated forms of DAPK and DRP-1 are capable of inducing two distinct cytoplasmic events characteristic of programmed cell death, including membrane blebbing and the formation of autophagic vesicles (Inbal
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Recent studies investigating the effects of mesenchymal stem
2021-07-07
Recent studies investigating the effects of mesenchymal stem cell (MSC) therapy in rodent models including chronic renal failure and glomerulonephritis have demonstrated that MSC therapy can result in beneficial effects [57], [58]. In cats, autologous intra-renal injections of either adipose tissue-
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In rats exposed to day of nicotine
2021-07-07
In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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The effect of the simple dopaminergic tonic
2021-07-07
The effect of the simple dopaminergic tonic/phasic model on cognitive processing has been investigated by a few studies (Nolan et al., 2004; Rosa et al., 2010). Rosa et al. (2010), using a Stroop task that requires different levels of cognitive flexibility and stability, observed an association betw
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In summary we demonstrated the high potency
2021-07-07
In summary, we demonstrated the high potency of fluxametamide against M. domestica, L. striatellus, and T. urticae GABACls, which leads to high acaricidal/insecticidal effects on these arthropod pests. In contrast to its high potencies against the GABACls of arthropod pests, fluxametamide exhibited
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The most significant finding was the
2021-07-07
The most significant finding was the inhibition of EROD and BFCOD activity by CLO. Inhibition of EROD and BFCOD were reversible, as pre-incubation did not enhance CLO inhibitory potency, and no reductions in IC50 values were observed. We further characterized the kinetic pattern of inhibition using
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toll like receptors In anticipation of an approach based on
2021-07-06
In anticipation of an approach based on modification of the cyclohexylacetic toll like receptors subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1,
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br Electron transfer pathway Intramolecular
2021-07-06
Electron transfer pathway Intramolecular (or inter-domain) electron transfer (IET) in CDH has been studied in much depth [], and similar IET occurs in CcPDH, from the PQQ cofactor in the AA12 domain to the heme b in the AA8 domain. When two kinds of electron acceptors are used for measuring enzym
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RDH belongs to C family of the short chain
2021-07-06
RDH10 belongs to 16C family of the short-chain dehydrogenase/reductase (SDRs) superfamily of proteins [12], [13]. Notably, in human genome adjacent to the gene encoding RDH10 on chromosome 8 are located two other genes encoding members of the SDR16C family: retinol dehydrogenase epidermal 2 (RDHE2,
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Haggar et al reported the synthesis of
2021-07-06
Haggar et al. reported the synthesis of two new series of 8-(2-imino/oxo/thioxo pyrimidin-4-yl)-4-methyl-6-nitro-2-oxo-2H-chromen-7-yl benzoates 56 (X=O, S, NH) and 8-(pyrazol-3-yl)-4-methyl-6-nitro-2-oxo-2H-chromen-7-yl benzoates 57 [Y=C(O)CH3, 2,4-(NO2)2C6H3]. The 8-acetyl-4-methyl-6-nitro-2-oxo-2
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In addition to PDCA we also
2021-07-06
In addition to 2,4-PDCA, we also tested other broad-spectrum 2OG oxygenase inhibitors as vCPH inhibitors. N-Oxalyl glycine (NOG, IC50 = 21.2 ± 2.1 µM), a close 2OG isostere, and IOX1 (IC50 = 47.2 ± 2.7 µM), which is a relatively broad-spectrum JmjC demethylase inhibitor, were not as potent in inhibi
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In summary we show that PE significantly ameliorate HCD
2021-07-06
In summary, we show that PE significantly ameliorate HCD-induced atherosclerosis in apoE−/− mice. Dietary fiber may influence the intestinal microbiota and thus the circulating levels of SCFAs. SCFAs, such as butyrate, inhibit cholesterol uptake and promote cholesterol excretion from enterocytes. Ou
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Further proof is required as to whether ER
2021-07-06
Further proof is required as to whether ER membrane receptors play a role in the maintenance of bone mass. It is also possible that other non-genomic pathways may be involved. Nevertheless, whatever the precise mechanism of action of estrogens may be, the imbalance between bone formation and resorpt
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