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We further examined our hypothesis
2021-03-05

We further examined our hypothesis that the activation of CRF and CCK systems is responsible for the enhanced anxiety-like behavior induced by immobilization stress using two antagonists to block the expression of CRF1 and CCK2 receptors. It was found that CCK2 receptor antagonist CR2945 or CRF1 ant
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Furthermore positioning the naphthalene nucleus in
2021-03-05

Furthermore, positioning the naphthalene nucleus in 3d within the main active site and forming one hydrogen bond with Tyr385 in addition to many hydrophobic interactions with Val349, Leu352, Gly526, Ala527 and Leu531 residues, correlates well with the position and hydrophobic interactions of the tri
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br Roles for intracellular chloride channels br
2021-03-05

Roles for intracellular chloride channels Specific chloride channel proteins in intracellular membranes Concluding remarks Introduction The sulfonylurea derivative glybenclamide (GLYB) is used as oral hypoglycemic agent to treat non-insulin dependent diabetes mellitus [1], [2]. The antid
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Nrf and HO are key factors in the
2021-03-05

Nrf2 and HO-1 are key factors in the regulation of oxidative stress in the body. Research has shown that KLF2 can activate Nrf2 and HO-1 [14]. To investigate the mechanisms by which KLF2 regulates eNOS uncoupling and oxidative stress, Nrf2 was inhibited or HO-1 was knocked down in KLF2 overexpressin
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As proof of principle the effect of selective blockade was
2021-03-05

As proof of principle, the effect of selective blockade was measured using TAK-044, a peptide antagonist with approximately 250-fold selectivity for the ETA subtype over ETB as measured by ligand binding in the human heart. A 30-mg infusion over 15 minutes of TAK-044 (providing a serum concentration
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The expression of cytokine inducible genes is mediated
2021-03-05

The expression of cytokine-inducible genes is mediated by a number of components within the cell. It has been shown that Jak2 and the Ras/Raf/MAP kinase signaling cascades are required for the expression of DUB-1[9], [29]. However, the enhancer domain of DUB-1 lacks a consensus sequence for Stat bin
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The Lysine mutant is located in the tail region
2021-03-05

The Lysine429 mutant is located in the tail region of 5-HT2A, which is predicted to be unstructured. This region has been shown to interact, in vitro, with PSD95 and leads to differences in signaling (Xia et al., 2003). The ASK motif, a component of the tail region, is also important for regulation
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During the past three decades platinum based DNA
2021-03-05

During the past three decades, platinum-based DNA-alkylating agents have been employed in the treatment of various cancers [14]. Oxaliplatin is currently used as a first-line treatment for colorectal cancer (CRC) [15]. Unfortunately, a large portion of CRC patients receiving oxaliplatin-based chemot
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The homologous DDRs are composed of an N terminal discoidin
2021-03-04

The homologous DDRs are composed of an N-terminal discoidin homology domain, followed by a sequence of ∼220 amino acids unique to the DDRs, a transmembrane domain, a large juxtamembrane domain, and a conserved cytoplasmic tyrosine kinase domain. In a previous study, we demonstrated that DDR activati
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Studies of LRRK tagged with green fluorescent protein reveal
2021-03-04

Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the 5-EdU of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defines its function
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van Linden et al developed a comprehensive guide
2021-03-04

van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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The structures of the set
2021-03-04

The structures of the set of pyrazoles of are contained in the supplied with this manuscript. Acknowledgments Prostaglandin D (PGD) is known to bind with high affinity to two G protein-coupled seven-transmembrane receptors DP1 and DP2. The latter receptor, also known as CRTH2 (chemoattractant
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Beside the previously reported Topo I inhibition
2021-03-04

Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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Introduction Progesterone also known as P is a steroid hormo
2021-03-04

Introduction Progesterone, also known as P4, is a steroid hormone acting as a key component in the complex regulation of female reproductive function. P4 plays major physiological roles in the uterus and ovary by releasing mature oocytes helping in implantation and maintenance of pregnancy, as well
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Meanwhile high levels of extraversion have been
2021-03-04

Meanwhile, high levels of extraversion have been associated with weaker conditioning and faster L 006235 learning (Eysenck, 1970). Similar to neuroticism/anxiety, the role of extraversion for fear conditioning and extinction has found only limited empirical support (Rauch et al., 2005) with several
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