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To investigate an involvement of GPR
2021-10-25
To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) Adenine HCl were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-63 cells, while n
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Combination inhibitors of FAAH TRPV and or COX may have
2021-10-25
Combination inhibitors of FAAH, TRPV1, and/or COX2 may have the advantage of effective pain relief with a high therapeutic index. For example, arachidonoyl serotonin (AA-5-HT) inhibits both FAAH (IC=1–12μM) and TRPV1 (IC=37–270nM against 100nM capsaicin in HEK-293 cells)., In mice, AA-5-HT had great
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br Introduction Currently HIV infection treatment guidelines
2021-10-25
Introduction Currently, HIV-1 infection treatment guidelines adopted in USA and EU provide for the simultaneous administration of three antiretroviral drugs (HAART “Highly Active Anti-Retroviral Therapy”) in severely compromised patients [[1], [2], [3]]. Coupling at least two different mechanisms
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Several plant derived molecules such as resveratrol curcumin
2021-10-25
Several plant-derived molecules such as resveratrol, curcumin, zerumbone, and physalin B have been reported as modulators of Hh/Gli signaling pathway (Hosoya et al., 2008, Mohapatra et al., 2015). Our previous studies have demonstrated that a sesquiterpene lactone and diarylheptanoids from Siegesbec
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na ca exchanger Several layers of regulation for this canoni
2021-10-25
Several layers of regulation for this canonical activation of the HH pathway exist. First, the protein kinase A (PKA), the casein kinase 1α (CK1α) and GSK3β can phosphorylate and mark for proteosomal degradation the GLI transcription factors. [36] Second, Suppressor of Fused (SUFU) binds to GLI and
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br Materials and methods br Results We
2021-10-25
Materials and methods Results We studied 16 patients infected with HCV genotypes 1a and 1b, naïve for protease inhibitor-based therapy. All patients, chronically infected, were selected by the Hepatology Department for triple therapy. Most of them had severe liver fibrosis at the beginning of
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Under increased drug pressure more protease variants
2021-10-25
Under increased drug pressure, more protease variants with more than one substitution will likely become clinically relevant. The accumulation of additional substitutions can allow RAS variants to emerge that alone are not viable, but in combination can rescue the viral fitness. We previously demons
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Mice lacking S nitrosoglutathione reductase GSNOR a denitros
2021-10-25
Mice lacking S-nitrosoglutathione reductase (GSNOR), a denitrosylase that regulates S-nitrosylation, have increased levels of S-nitrosoglutathione (GSNO) and exhibit nitrosative stress. GSNO is in equilibrium with protein S-nitrosylation in cells, and GSNOR controls the cellular concentration of pro
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The GPR receptor is also
2021-10-25
The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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A subsequent modeling study by a
2021-10-25
A subsequent modeling study by a different group was based on the bovine rhodopsin homology model using the 1L9H construct [38]. However, the site-directed mutagenesis data and docking suggested that the niacin-binding pocket is different to that described in the aforementioned report, but similar t
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Previous studies have shown that zinc interacts with
2021-10-25
Previous studies have shown that zinc interacts with other allosteric modulators at the glycine receptor (Kirson et al., 2013, McCracken et al., 2010, McCracken et al., 2013). Of note, the chelation of zinc via tricine decreases the effects of alcohol at α1-, α2-, and α3-containing glycine receptors
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Which is the preferred dimer configuration the
2021-10-25
Which is the preferred dimer configuration, the one corresponding to the active state or the one corresponding to the desensitized state? Umbrella sampling simulations of a pair of GluA2 LBDs, using distances at the top (proximal to the ATD) and the bottom (proximal to the TMD), indicate that the de
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In the present study five Glu substituted analogues of GIP
2021-10-25
In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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Recently unimolecular multi functional peptides that combine
2021-10-25
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with GSK2126458 synthesis and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control
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br Role of ghrelin in reward and addiction In
2021-10-25
Role of ghrelin in reward and addiction In addition to its well-known effects on AS 101 australia homeostasis regulation at the hypothalamic level [reviews in (Al Massadi et al., 2017, Muller et al., 2015)], ghrelin also has the ability to increase food motivation acting on hypothalamic and extr
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