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br Introduction The Ras superfamily
2021-10-07

Introduction The Ras superfamily of small GTPases is composed of more than 150 protein members involved in a wide variety of biological processes, such as proliferation, differentiation, cytoskeletal organization, and protein trafficking [1]. The Ras superfamily proteins act as molecular switches
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Lean mass is representative of the muscle tissue mass
2021-10-07

Lean mass is representative of the muscle tissue mass equivalent of all the body parts containing water, excluding fat, bone minerals, and such substances which do not contribute to the NMR signal, such as hair, claws, etc. (ECHO-MRI (Houston, TX) user's manual). It was interesting that in the Bob-C
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GW was also the starting point for a
2021-10-07

GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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The effects of opioids such as morphine are
2021-10-07

The effects of opioids such as morphine are mediated through the opioid receptors. Opioid receptors are widely expressed both peripherally and in the CNS (Chen et al., 1993, Evans et al., 1992). The opioid agonist morphine has been shown to amplify the effect of the tubular cell-gp120 interaction on
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br Results br Discussion The twin cysteine motif is
2021-10-07

Results Discussion The twin-cysteine motif is an evolutionary conserved motif in all primate lentiviruses except HIV-1 and some strains of SIVcpz according to sequence analysis (Bohl et al., 2013). It is assumed that only those SIVcpz which have lost the twin-cysteines successfully evolved to
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The two competitive bivalent GlxI inhibitors polyBHG nM and
2021-10-06

The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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Tetrazole is one of the most commonly used
2021-10-06

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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Photoincorporation of pTFDBzox AP occurred predominantly in
2021-10-06

Photoincorporation of 21-pTFDBzox-AP occurred predominantly in the β3 subunit, very modestly in the α1 subunit and not at all in the γ2 subunit. These observations taken together with the sensitivity of 21-pTFDBzox-AP enhancement of GABA currents to the α1 M1 mutation Q242 W4 suggest that the 21-pTF
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We reviewed the results of comprehensive genomic
2021-10-04

We reviewed the results of comprehensive genomic profiling (CGP) in 26,054 cases of NSCLC and examined the frequency and clinical characteristics of patients whose tumors harbor FGFR fusions. To our knowledge, this is the most in-depth evaluation of FGFR fusions exclusively in NSCLC. Here we will de
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Integrase inhibitors have been licensed for use in
2021-10-03

Integrase inhibitors have been licensed for use in the UK since 2008. BHIVA now recommend starting all treatment naïve patients on a regimen containing two NRTIs, plus one of the following: a ritonavir boosted PI, an NNRTI, or an integrase inhibitor. They make further recommendations for patients wi
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Evidence indicates that astrocytes play a role in the
2021-10-03

Evidence indicates that astrocytes play a role in the modulation of NMDAR activity in the CA1 (Henneberger et al., 2010; Papouin et al., 2017a, Papouin et al., 2017b; Robin et al., 2018). Therefore, we sought to examine whether astrocytes are involved in the H1 receptor antagonist/inverse agonist-in
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R 59-022 There have been a few studies investigating
2021-10-03

There have been a few studies investigating the effects of histamine on mast cells but the majority of these has been on rodent and cultured mast cells (Hofstra et al., 2003, Lippert et al., 2004, Jemima et al., 2014). How representative these systems are of primary human cells is a moot point since
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br Introduction Histamine was generally accepted
2021-10-03

Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activi
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The inhibition of HDAC increases
2021-10-03

The inhibition of HDAC increases the level of histone acetylation and consequently turns the chromatin to be loose and active, allowing multiple transcription factors to access to promoters of diverse genes including tumor suppressor genes []. As compound possessed potent HDAC inhibitory activity a
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Immunohistochemical analysis of sheep skin sections showed t
2021-10-03

Immunohistochemical analysis of sheep skin sections showed that sGC prtotein is expressed in the hair follicles with different location and abundance between white and black sheep skin (Fig. 6). In white sheep skin, Strong sGC positive signal was detected in the upper hair dermal papilla but no posi
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