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Studies carried out with LTRAs before the
2020-02-06
Studies carried out with LTRAs before the identification of the CysLT2R, showed a controversial picture, as results that suggest a role for cysteinyl-LTs in the expansion of ischemic damage and in cardiac dysfunction during reperfusion [5], [68], [69] were evenly balanced by others suggesting that t
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br The amygdala complex The amygdala complex is
2020-02-06
The amygdala complex The amygdala complex is composed of distinct nuclei and subdivisions including the lateral (LA), basolateral (BL), and basomedial (BM) amygdala; the medial (Imp), lateral paracapsular (lpc), and main intercalated cell cluster (IN); and the lateral and medialcentral amygdala (
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Many studies reporting on discoveries of DUBs
2020-02-05
Many studies reporting on discoveries of DUBs in the TGFβ and BMP pathways have relied on RNAi strategies to investigate loss-of-function impact. While RNAi strategies are useful tools, there are limitations ranging from limited knockdowns of targets to potential off-target effects. New and better t
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br Four active site residues of KSTD are fully
2020-02-05
Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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br General Characteristics of the Type II Dehydrogenases Alt
2020-02-05
General Characteristics of the Type II Dehydrogenases Alternative NAD(P)H dehydrogenases conduct the reaction of the rotenone-insensitive oxidation of cytosolic and mitochondrial matrix NADH and/or NADPH (Fig. 1) (Melo et al., 2004, Rasmusson et al., 2004, Rasmusson et al., 2008). They catalyze t
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Kim et al reported for bioactive compounds originating
2020-02-05
Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b
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P H is a nonheme iron II dioxygenase that uses
2020-02-05
P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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In addition to PGC transcriptional
2020-02-05
In addition to PGC1α, transcriptional co-repressors such as NCOR and RIP140 participate in oxidative muscle remodeling induced by exercise, whereby reductions in their expression and the resulting de-repression of downstream TFs activates oxidative gene expression (Seth et al., 2007, Yamamoto et al.
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Herein the interactions of etamicastat nepicastat and zamica
2020-02-05
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the Semaxanib exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remains
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Because EBI is expressed on the
2020-02-04
Because EBI2 is expressed on the major subsets of immune cells, and small molecule antagonists for EBI2 were recently described (Benned-Jensen et al., 2013, Gessier et al., 2014), EBI2 constitutes a tempting drug target reminiscent of the sphingosine-1-phosphate receptor superagonist fingolimod/Gile
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Fusaric Acid Programmed cellular death or apoptosis is
2020-02-04
Programmed cellular death or apoptosis is a process genetically controlled that plays an important role in cellular homeostasis, being an important defense mechanism to remove cells that have been infected, damaged or mutated (Smith and Smith, 2012, Wlodkowic et al., 2011). Nevertheless, apoptosis s
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Introduction Amphetamine AMPH methamphetamine MA
2020-02-04
Introduction Amphetamine (AMPH), methamphetamine (MA), and 3,4-ethylenedioxymethamphetamine (MDMA) are widely abused psychoactive substances, with the basic chemical structure of phenylethylamine [1]. The abuse of these drugs is associated with psychostimulant, anorectic and hallucinogenic properti
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As mentioned above there are two major pathways
2020-02-04
As mentioned above, there are two major pathways for the DSB repair in mammalian cells, NHEJ and HR/HDR (homology-directed repair) [13], [51]. NHEJ is active throughout the cell cycle, predominately during the G0 and G1 phases and is considered the major pathway for the DSB repair in human cells [52
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br Conclusions Enzyme can be delivered to the
2020-02-04
Conclusions Enzyme can be delivered to the tumour by using humanised or fully human Fructose Colorimetric/Fluorometric Assay Kit receptor or even loaded into synthetic nanospheres produced from silica [64] or liposomally entrapped [65]. For any future ADEPT developments, a number of basic points
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Therefore HNE is an attractive therapeutic
2020-02-04
Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo
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