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muscarinic receptor antagonists Free fatty acid receptor FFA
2021-12-06
Free fatty muscarinic receptor antagonists receptor 1 (FFAR1, also known as GPR40) belongs to the family of G protein-coupled receptors (GPCRs) and was de-orphanized in 2003 as a receptor for medium-to long-chain free fatty acids (FFAs) [9,10]. Mainly expressed in beta cells of pancreatic islets, G
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Up to now the research about
2021-12-06
Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett
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In order to test whether the
2021-12-06
In order to test whether the enhanced hyperpolarization in the presence of increasing amounts of extracellular Ca2+ could be due to an ionophore effect of NS309, red cell uptake of 45Ca and partition of 45Ca into a water/n-octanol phase +/−100 μM NS309 were determined. However, no indication of iono
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GSK 650394 Hypocotyl development is a crucial phase of early
2021-12-04
Hypocotyl development is a crucial phase of early vegetative growth that influences seedling vigor contributing to fitness and productivity of a plant system (Stinchcombe and Schmitt, 2006; Luo et al., 2017). The development of a hypocotyl is characterized by an initial slow growth phase followed by
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The Ala to Leu substitution would reduce the
2021-12-04
The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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br Acknowledgement This research was supported by Basic Scie
2021-12-04
Acknowledgement This research was supported by Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2016R1A2B4012818). Oral ionophore is the most popular administration route due to good patients’ com
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A biochemical characterisation of this functionally crucial
2021-12-04
A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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The mast cell has long been recognized as central to
2021-12-04
The mast cell has long been recognized as central to the mediation of allergic responses not least because it is the principal repository of histamine in the body. Following activation by allergens, the mast cell can release histamine as well as generate a host of additional mediators such as cystei
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In summary P P macrocyclization proved
2021-12-04
In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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Here we investigate the structural and biochemical propertie
2021-12-04
Here we investigate the structural and biochemical properties of the N-GTPase domain of p190RhoGAP-A. We determine the crystal structure and find that N-GTPase adopts an extended GTPase-like fold with six unique inserts that seem to preclude its ability to bind typical GAP, GEF, or Pyocyanin molecu
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GSK is a critical component
2021-12-04
GSK-3 is a critical component of the Wnt signaling pathway. The Wnt/beta-catenin signal transduction pathway is important in normal growth and development and is also frequently dysregulated in cancer and other diseases. The Wnt/beta-catenin pathway is finely tuned by both positive and negative inte
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In this study we further expanded the antitumor bioactivity
2021-12-04
In this study, we further expanded the antitumor bioactivity, with the BALB/c S-180 tumor model, which is long-established due to its highly aggressive in all strains of laboratory mice and rats (Cui et al., 2003). We investigated the tumor-regressing ability of β-glucan by different modes of admini
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br Acknowledgements This research was
2021-12-03
Acknowledgements This research was funded by Ministry of Education Malaysia (MOE), and supported by the Department of Nutrition, Exercise & Sports, Department of Drug Design, University of Copenhagen, Denmark and Universiti Malaysia Pahang (UMP), Malaysia. HPLC equipment used for high-resolution
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The active site of PS is located at
2021-12-03
The active site of PS1 is located at the interior of its TM horseshoe-like fold (29) (Fig. 1). TM2 and TM6 serve as “doors” for substrate entry (30), as also observed in recent molecular dynamics (MD) simulations of the PS1 subunit (31). Recent coarse-grained (CG) and atomic simulations also showed
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br Promotion of GLS expression Glutamine metabolism
2021-12-03
Promotion of GLS2 expression Glutamine metabolism is another target for alteration in ferroptosis. Glutamine is required for the induction of ferroptosis during serum-induced injury after amino 4-ethylphenyl sulfate starvation [72]. The first step of glutamine catabolism is its conversion to glu
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