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MMV s distinct mode of inhibition
2021-09-13
MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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Introduction Vesicular exocytosis an intracellular membrane
2021-09-13
Introduction Vesicular exocytosis, an intracellular membrane trafficking pathway, is a ubiquitous process for intercellular communication. It occurs when an intracellular vesicle fuses with the cell membrane and subsequently releases an infinitely minute number of chemical or biochemical messengers
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We confirmed a decrease in extracellular glutamate uptake
2021-09-11
We confirmed a decrease in extracellular glutamate uptake and the presence of efflux in an endothelial cell model of oxygen-glucose deprivation (OGD), which effectively simulates the inefficient energy supply after brain injury [15], and analysed the function of endothelial EAATs and explored the ro
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To validate the effects of the G a HMT
2021-09-11
To validate the effects of the G9a HMT inhibitors on HMEC-1 harmine and transcriptional responses we generated knockdown cells for G9a using an shRNA approach. Upon transduction of HMEC-1 and doxycycline activation of the shRNA, both G9a HMT mRNA and protein expression were effectively decreased (F
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Corollary and Lemma Finally Corollary and Lemma
2021-09-11
(Corollary 3 and Lemma 9). Finally, Corollary 5 and Lemma 10 show that if then the support of is wide enough and so must contain the points of maximum of the attached. However, the support of is too narrow and so does not contain the points of maximum of the remote. Hence, the remote has at most two
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We are pursuing a hit to lead medicinal chemistry campaign
2021-09-11
We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Resul
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Here we used Drosophila and
2021-09-11
Here, we used Drosophila and mouse models to address the biological function of RALs in the adult intestine. Our results demonstrate a conserved in vivo role for RALs in ISC function during tissue homeostasis and regeneration. ISCs lacking RALs were at a disadvantage compared to wild-type neighbors.
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br Consequence physiological function of ROS dependent inhib
2021-09-11
Consequence/physiological function of ROS-dependent inhibition of GSNOR Plants response to environmental changes induced by abiotic and biotic factors by enhanced accumulation of ROS resulting in temporary imbalance of the cellular redox homeostasis. This as oxidative stress/burst termed event tr
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Several studies have proposed that high
2021-09-11
Several studies have proposed that high levels of KYNA in the ABT-888 contribute to cognitive dysfunctions presented by patients who suffer from schizophrenia [30], [31], [32], [33]. Considering that: (i) KYNA is a known GPR35 agonist [2], (ii) cognitive impairments in patients with schizophrenia a
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Atglistatin br Conclusion The wild study reports seasonal va
2021-09-11
Conclusion The wild study reports seasonal variations in reproductive physiology, behavior and Atglistatin plasticity at different age stages in wild-caught Mongolian gerbils. The gerbils in breeding seasons have more mature sexual development, higher exploratory behavior, higher novelty prefere
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In this study for the first time
2021-09-11
In this study, for the first time: 1) the electrochemical glutamate oxidase-based biosensor was optimized for the determination of low micromolar glutamate concentrations; 2) the algorithm of the analysis of exocytotic and transporter–mediated glutamate release was developed; 3) the comparative anal
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Pyrogallol is an organic gallic acid converting compound
2021-09-11
Pyrogallol is an organic gallic acid-converting compound that has three hydroxyl groups and belongs to the phenol family. Gallic ibuprofen solubility is obtainable from the galls and barks of various trees, and a simple heating procedure can induce the decarboxylation of gallic acid to produce pyro
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Importance of glucokinase in glucose homeostasis and a possi
2021-09-11
Importance of glucokinase in glucose homeostasis and a possibility to change its activity using the activators define the scientific interest in the development of new allosteric activators of GK (Liu et al., 2012, Pfefferkorn et al., 2011, Waring et al., 2013, Behera et al., 2015). Activation of gl
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br Materials and methods br Results br Discussion
2021-09-11
Materials and methods Results Discussion Common to catfish fry production, high stocking densities as well as intensive handling during transport can result in low dissolved oxygen levels (Abdalla and Romaire, 1996; Torrans et al., 2003), which can result in fish stress. It is not known at
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br Conflict of interest br Introduction Since its discovery
2021-09-11
Conflict of interest Introduction Since its discovery in 1958 [1]the Ca2+-dependent K+ efflux in human red blood Fmoc-Asp(OtBu)-OH (RBC) (further referred to as the Gárdos effect) has been extensively studied (see 2, 3for review) and has been helpful in understanding the role of the Ca2+-acti
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