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In previous work we showed
2021-10-11

In previous work we showed that benzophenanthridines do not affect the surface expression of GlyT1 (Jursky and Baliova, 2011). The results from the surface biotinylation studies reported in Fig. 3 show that the surface expression of the Y370F mutant is not significanly affected by the alkaloids in t
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Extensive pharmacological and structural analysis shows GCGR
2021-10-11

Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in 25 sta receptor 14, 17, 20. Functionally identical to REMD-477, REM
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Another key component of proper DA cell physiology is
2021-10-11

Another key component of proper DA cell physiology is the basal firing activity of SN DA neurons, which maintains extracellular levels of dopamine in the dorsal striatum that are essential for voluntary movement [106]. Changes in SN DA neuron activity directly impacts the amount of dopamine released
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In the last years a plethora of studies overstepped the
2021-10-11

In the last years, a plethora of studies overstepped the classic concept of the ENS as purely modulator of GI secretion and motility, focusing on its potential as source of substances acting on immune cells and consequently involved in the control of local inflammatory events, as in the Inflammatory
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Ionotropic aminobutyric acid GABA receptors GABARs belong to
2021-10-11

Ionotropic γ-aminobutyric cycloheximide solubility (GABA) receptors (GABARs) belong to the Cys-loop ligand-gated ion channel (LGIC) superfamily and play an important role in the rapid inhibitory synaptic transmission in nervous systems of both vertebrate and invertebrate (Buckingham et al., 2005). I
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With the identification of small nonpolar substituents at R
2021-10-09

With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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br Materials and methods br
2021-10-09

Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta ML385 [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract, adipocytes an
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In principle an ideal Fenton
2021-10-09

In principle, an ideal Fenton reaction element should have multiple oxidation states to form a redox cycle in the process of H2O2 decomposition to HO•. Although iron is very effective in catalyzing Fenton reaction, it requires a low pH value (pH 2-4) to reach the optimal catalytic efficiency, which
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We also intended to determine the possible mechanism
2021-10-09

We also intended to determine the possible mechanism underlying EZH2 upregulation in the PC. Although no recurrent mutations of EZH2 have been described in CLL [27, 28, 29], we aimed to rule out the possibility of activating mutations in the background of EZH2 overexpression. We detected no mutation
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The PAS and CC domains of sGC have
2021-10-09

The PAS and CC domains of sGC have been studied less by comparison, though their function in sGC signal transduction is likely important. PAS domains are versatile as they can play varied roles in different proteins, such as quaternary structure organization, cofactor binding, and signal transductio
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Our study has strengths and limitations We believe
2021-10-09

Our study has strengths and limitations. We believe we are the 1st to report a novel model of secondary hypogonadism. Several animal models for hypogonadotropic hypogonadism (kisspeptin and the kisspeptin receptor knockout) exist but we are unaware of animal models of secondary hypogonadism with dif
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br Synthetic Antagonists for FFA
2021-10-09

Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this
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It may seem counterintuitive that a lymphocyte which is
2021-10-09

It may seem counterintuitive that a lymphocyte which is unable to proliferate could have neoplastic potential since the very definition of neoplasia is one of autonomous clonal expansion of a cell. The lack of co-stimulatory molecules CD27 and CD28 can potentially be overcome by activating NK cell r
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br AUTHOR CONTRIBUTIONS br ACKNOWLEDGMENTS br
2021-10-09

AUTHOR CONTRIBUTIONS ACKNOWLEDGMENTS Introduction Chronic neuropathic pain is a common symptom in patients with human immunodeficiency virus (HIV)-1 infection. Glycoprotein 120 (gp120) is an HIV-1 protein that can cause pain behaviors in animal models (Hao, 2013, Nasirinezhad et al., 2015,
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Mapping and separation of the anti GlyT
2021-10-09

Mapping and separation of the anti-GlyT1C epitopes allowed us to verify the existence of calpain cleavage sites in isolated mouse synaptosomes. In order to allow calcium to enter the intrasynaptosomal compartment and activate endogenous calpain, we incubated synaptosomes in hypoosmotic high (200μM)
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