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CaneCPI showed strong inhibitory activity against recombinan
2020-11-17

CaneCPI-4 showed strong inhibitory activity against recombinant falcipain-2 and falcipain-3, with IC values of 11.9±0.4nM and 42.3±0.8nM, respectively (Table 1, Supplementary material). Falcipains are involved in hemoglobin cleavage, with generation of two fractions: the heme and the globin. The hem
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Recent pharmaceutical research in the field
2020-11-17

Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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Ultimately we decided to investigate the role of
2020-11-17

Ultimately, we decided to investigate the role of Cyp3a in obesity because Hepatic P450 Reductase-null (HRN) mice with no P450 activity show hepatic steatosis with increased Cyp2b10 and Cyp3a11 expression, perturbations in liver size, lipid homeostasis, and increased liver polyunsaturated fatty acid
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In a previous study we reported that the systemic administra
2020-11-17

In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in Nilvadipine australia reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present experiments w
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Two major mechanisms including apoptosis and oxidative stres
2020-11-17

Two major mechanisms including apoptosis and oxidative stress have been suggested for MTX-induced cytotoxicity (Hafez et al., 2015; Neuman et al., 1999; El-Sheikh et al., 2015). It has been reported that MTX promotes cell death via apoptosis in both cancerous and non-transformed cells (Mazur et al.,
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The major concern of PDE I use in liver
2020-11-17

The major concern of PDE-5-I use in liver cirrhosis is the potentially harmful effect on systemic blood pressure. Data of clinical studies are conflicting [27], [30], [31], [32], but available patient details suggest that in advanced liver cirrhosis, PDE-5-Is lower systemic blood pressure to a great
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Besides having a remarkable progestogenic effect an
2020-11-17

Besides having a remarkable progestogenic effect, an additional characteristic of DRSP is its strong antimineralocorticoid effect and antiandrogenic action [11]. DRSP is characterized by an antimineralocorticoid effect that is stronger when compared to progesterone. The decreasing synthesis of proge
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br Introduction Detection of driver mutations in patients wi
2020-11-16

Introduction Detection of driver mutations in patients with advanced non-small cell lung cancer (NSCLC) is critical because they receive great benefit from kinase inhibitors [[1], [2], [3], [4]]. However, it is often difficult to obtain tumor tissue in advanced NSCLC patients. Cell-free DNA (cfDN
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Another example of negative regulation is the
2020-11-16

Another example of negative regulation is the inhibition of the yeast endosome-associated DUB Doa4 by Rfu1 (free ubiquitin chains 1). In a yeast genetics screen, deletion of Rfu1 was serendipitously found to alter global ubiquitin levels [69]. DUBs can regulate these levels by liberating conjugated
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br Acknowledgement br Introduction Human dihydroorotate dehy
2020-11-16

Acknowledgement Introduction Human dihydroorotate dehydrogenase (hDHODH), a flavin-dependent mitochondrial enzyme involved in de novo Nevirapine biosynthesis, is a validated therapeutic target for the treatment of autoimmune diseases such as rheumatoid arthritis and cancer [1], [2], [3]. Lefl
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biotin 100 mg Saururus chinensis Lour Baill Saururaceae a
2020-11-16

Saururus chinensis (Lour.) Baill. (Saururaceae), a perennial herb, is widely cultivated in China and southern Korea. It has been traditionally used as folk medicine for the treatment of inflammation, jaundice and gonorrhea [8]. Previous chemical studies of S. chinensis have revealed the presence of
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br Four active site residues of KSTD are fully conserved
2020-11-16

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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Our recent discovery M P H R
2020-11-16

Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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Eukaryotic cell cycle machinery is thought to appropriately
2020-11-16

Eukaryotic cell cycle machinery is thought to appropriately modulate cell proliferation and cell expansion in various developmental stages and environmental conditions. The core feature of cell-cycle control is the fluctuation of CDK activity, which is regulated by three interactive and conserved me
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br Conclusions Taken together a distinct contrast is observe
2020-11-16

Conclusions Taken together, a distinct contrast is observed between ERK1/2 phosphorylation in hypothalamic and extra-hypothalamic Bleomycin A5 hydrochloride regions. The hypothalamus is the only brain region where ERK1/2 phosphorylation was increased 15minutes after the OF stressor. In SD rats C
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