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The present study sought to determine if chlorodifluoroaceto
2021-03-02
The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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In the present study promoting bile acid synthesis by
2021-03-02
In the present study, promoting bile Neurotensin synthesis synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for live
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Obviously there are some limitations in our study
2021-03-02
Obviously, there are some limitations in our study; due to sample constraints, we had to focus our efforts on one specific T cell epitope from one candidate autoantigen. Optimally, we could have studied several different peptides in parallel. Additionally, all RA patients included in the study have
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Imatinib STI is a first line tyrosine kinase
2021-03-02
Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (D
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The best characterized APC C substrates are recruited via
2021-03-01
The best-characterized APC/C substrates are recruited via various linear motifs (e.g., D boxes, KEN boxes, and ABBA motifs) that serve as degrons, binding to distinct regions of the β-propeller domain of a coactivator (Figure 1, Figure 3B) (reviewed in [44]). In addition, D boxes also simultaneously
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Inflammatory action of certain cytokines can influence cell
2021-03-01
Inflammatory action of certain cytokines can influence cell proliferative routes (Deshmane et al., 2009). When mTOR is inhibited, for instance by the action of Rapa, TGF-β1, which has an anti-inflammatory action, is increased. The relationship between high levels of TGF-β1 and anatoxin a synthesis
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br Patients and Methods Patients who had been initiated
2021-03-01
Patients and Methods Patients who had been initiated on a DPP-4 inhibitor (see in the online version at doi:10.1016/j.clinthera.2018.06.002) between April 2012 and June 2017, when the common threshold for dose adjustment for all non-linagliptin DPP-4 inhibitors was a creatinine clearance (CrCl) l
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The inhibition of NPY cleavage may also contribute
2021-03-01
The inhibition of NPY cleavage may also contribute to the effect of gliptins on blood pressure [123]: NPY is an agonist of Y1 receptor mediating peripheral vasoconstriction. Interestingly, blood pressure in adult SHRs was not affected by single dose administration of a specific DPP-4i whereas blood
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In addition to G coupling it is
2021-03-01
In addition to Gα coupling, it is important to consider that the transition from goal-directed to habitual drug taking also relies on striatal D2R-A2AR heterodimers. Following cocaine self-administration, D2R-A2AR density is increased in the NAc, leading to greater antagonism of the inhibitory (anti
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While apparent that His Artemis fractionated
2021-03-01
While apparent that [His]6-Artemis fractionated over a HAP column is devoid of 5′–3′ exonuclease activity but still retains DNA-PK dependent hairpin-opening activity, we sought to further assess DNA-PK dependent Artemis overhang cleavage activity to ensure all the in vivo, intrinsic enzymatic activ
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UNC0638 br Materials and methods br Acknowledgments
2021-03-01
Materials and methods Acknowledgments Introduction Proton pumps convert the energy of high-energy compounds into the UNC0638 of protons across biomembranes. They play two physiological roles: pH regulation and the formation of proton-motive forces in their membranes. The simplest of these
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br Materials and methods br Results
2021-03-01
Materials and methods Results and discussion Conclusions Clitocypin is another member of the mycocypin family of cysteine protease inhibitors that is unique to PI103 shown to exhibit strong insecticidal activity against Colorado potato beetle larvae. This effect is concentration dependent
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The ability of TKIs in inducing CRTH expression could be
2021-03-01
The ability of TKIs in inducing CRTH2 expression could be related to the c-terminal of CRTH2 receptor that is important molecular determinant in the down-stream signaling cascade activation [20]. This requires further studies to prove it or disprove it. Additionally, further studies are needed to ex
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Kim et al reported for
2021-03-01
Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b
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The highest concentrations from several
2021-03-01
The highest concentrations (from several tens to often hundreds or thousands ng/L) are reported in animal farm flush water, and associated runoffs and lagoons in China and in the U.S. Lower concentrations are reported in WWTP influents and effluents. In WWTP influent waters DRO, LNG, NET and PRG hav
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