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Not only has the cortical actin network been found
2022-05-09
Not only has the cortical Escitalopram Oxalate receptor network been found to influence plasma membrane properties but also to interact with exo- and endocytic vesicles (Gormal et al., 2015, Tomatis et al., 2013). The interplay between actin and membranes is integrally regulated by the phosphoinosi
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Syt itself does not catalyze lipid mixing
2022-05-09
Syt1 itself does not catalyze lipid mixing and membrane fusion. Rather, the pairing of vesicular and target membrane SNAREs into complexes serves to pull bilayers together to drive fusion; Ca•syt1 accelerates these fusion reactions so that they occur on rapid timescales in a manner that is precisely
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Classical drugs target the viral enzymes reverse transcripta
2022-05-09
Classical drugs target the viral glucocorticoid receptors reverse transcriptase (RT), protease and integrase (IN) [[4], [5], [6]]. Raltegravir (ISENTRESS/MK-0518) is the prototypical integrase strand transfer inhibitor (INSTI) leading to an extremely strong reduction in viral load [7] and it has bee
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Simeprevir br Conflict of interest statement br References
2022-05-09
Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We thank Urann Chan for assistance with the figures. This work was supported in part by National Institutes of
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It was then found that
2022-05-09
It was then found that TAZ, a YAP holomog, binds heteromeric SMAD2/3–4 complexes in a TGF-ß-dependent fashion, and is recruited to TGFβ response elements (Varelas et al., 2008). Knockdown experiments identified TAZ as critical for nuclear accumulation of SMAD2/3/4 complexes in response to TGF-ß, and
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br Materials and methods br Results Estimations of
2022-05-09
Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of Phusion high-fidelity DNA polymerase concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact si
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Under increased drug pressure more protease
2022-05-09
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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br Introduction Hepatitis B virus HBV infects about billion
2022-05-09
Introduction Hepatitis B virus (HBV) infects about 2 billion people worldwide and is a leading cause of liver disease including liver fibrosis, cirrhosis and hepatocellular carcinoma (Trepo et al., 2014). Most current HBV therapies are based on nucleos(t)ide analogs and pegylated interferon alpha
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br Materials and methods br Results br Discussion
2022-05-09
Materials and methods Results Discussion D. abbreviatus larvae are voracious feeders, and the nutrients consumed as part of their diet are broken by gut proteases and utilized for growth and development. Since proteases play an important role in larval and adult food digestion, it is import
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To assess the roles of GPR and GPR in malignant
2022-05-07
To assess the roles of GPR120 and GPR40 in malignant properties of pancreatic cancer cells, we generated GPR120 and GPR40 knockdown (PANC-sh120 and PANC-sh40, respectively) nibr synthesis from PANC-1 (Fig. 2A). While no difference of cell growth rate between control PANC-RFP cells and PANC-sh120 cel
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To gain insights for further improvement
2022-05-07
To gain insights for further improvement of the agonistic activity, we compared the structural features of the -carbamate piperidine moiety in with that of the spirocyclic moiety in –. Obviously, the substituent corresponding to an isopropyl group on the -carbamate in was lacking in the spirocyclic
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Recently a G protein coupled receptor GPR
2022-05-07
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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No compounds in this series showed any appreciable
2022-05-07
No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in mal
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In the present study both experimental
2022-05-07
In the present study, both experimental and theoretical studies were performed to explore the inhibitory mechanisms of indomethacin and its analogues towards GLOI. A remarkable correlation (=0.974) was derived for the four structurally similar NSAIDs and two curcumins between the experimental bindin
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In this study we also profiled
2022-05-07
In this study, we also profiled the expression of the transporters in wild-type RBL-2H3 cells, RBL-2H3 Sc98 cells, and rat peritoneal mast cells. OCT1 and PMAT were expressed at high levels in both RBL-2H3 Sc98 and RBL-2H3 cells. However, OCT2 and OCT3 were weakly or least detected in RBL-2H3 Sc98 c
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