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We recently reported the first cyclopropene analog of the
2021-10-21
We recently reported the first cyclopropene-analog of the amino EW-7197 neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworkers) [28]. We o
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It must be noted that
2021-10-21
It must be noted that while the accumulated evidence on molecular mechanisms has resulted in well-established experimental methods to externally act on single-cell characteristics and networks, safe and efficient external methods to modify multicellular states are still a matter of basic research. C
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Neovascularization upon IMQ treatment was
2021-10-21
Neovascularization upon IMQ treatment was observed to different degrees in WT and GAL3-KO mice, whereas the increase in vascular endothelial growth factor mRNA levels was genotype independent. Because we observed lower levels of the cytokines IL-17A, IL-22, IL-23, and TNF-α in IMQ-treated skin of GA
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Through the analysis of various synthetic
2021-10-21
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Potassium Canrenoate motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of dis
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Sonidegib is currently under investigation for the treatment
2021-10-21
Sonidegib is currently under investigation for the treatment of relapsed/refractory acute leukemia (NCT01826214) [76]. All patients experienced at least 1 AE, including anemia, diarrhea, fatigue, nausea, muscle spasms, decreased appetite, and blood creatine phosphokinase increased. The ongoing phas
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br Competing interests br Funding br
2021-10-21
Competing interests Funding Ethical approval Acknowledgement Introduction Hepatitis C is a disease that infects the liver through transmission of the hepatitis C virus (HCV). Because the symptoms of this infection are not pronounced, the infected individuals may not even be aware of t
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br Materials and methods br Results br Discussion
2021-10-20
Materials and methods Results Discussion Recently, we characterized the interaction of the PH domains of various Lbc family RhoGEFs with the activated small GTPase, RhoA, and demonstrated that this could serve as a positive feedback mechanism for robust activation of RhoA (Medina et al., 20
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Two different genes encode GSK isoforms and that
2021-10-20
Two different genes encode GSK-3 isoforms α and β that have very similar catalytic domains but significantly differ in their N- and C-termini. The α and β isoforms split from a common precursor approximately at the emergence of vertebrates, suggesting that at least one of the isoforms took on a new
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The fact that GSK recognition of its substrate involves
2021-10-20
The fact that GSK-3 recognition of its substrate involves pre-phosphorylation supports the rational for using synthetic phosphorylated peptides as substrate competitive inhibitors [57]. Phosphorylated peptides derived from the N-terminal pseudosubstrate sequence of GSK-3β were very weak inhibitors o
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The pharmacokinetics of was obtained in mouse rat and
2021-10-20
The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indi
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In a recent study Neelaveni et
2021-10-20
In a recent study, Neelaveni et al. [47] revealed that new thiazolidinedione derivatives (Fig. 6 a and 6 b) produced dual PPARγ and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from the pancreas. These derivatives were reported
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Cyclosporine sale br Formation of secretory vesicles and tra
2021-10-20
Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for Cyclosporine sale off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013).
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With the increasing use of INSTIs in clinical practice drug
2021-10-20
With the increasing use of INSTIs in clinical practice, drug resistance to this class in different HIV-1 subtypes should be carefully monitored and investigated. Studies on HIV-1 diversity and drug resistance would greatly help our understanding of viral transmission, pathogenesis and ART resistance
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CONUT score is an effective detector of predicting
2021-10-20
CONUT score is an effective detector of predicting OS and RFS in HCC patients. We found that patients with a damaged immune-nutrition status had significantly poor OS and RFS. Our initial literature review also retrieved other studies evaluating the survival of HCC patients using CONUT score [36,48,
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As GSH cellular redox status is
2021-10-20
As GSH cellular redox status is critical for various biological phenomena including apoptosis and inflammation [34], [35] we hypothesized that inflammation could modulate GSTP1-1 gene expression. Indeed, reactive oxygen species (ROS) are released at inflammation sites and can be eliminated from Angi
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