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MMV s distinct mode of
2022-09-30
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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This study appears to provide an additional example
2022-09-29
This study appears to provide an additional example, albeit an unanticipated one, of the importance of renal ETB receptor function in the normal control of blood pressure and salt and water homeostasis. ETB receptor-deficient rats, collecting duct-specific ETB receptor knockout mice, and rats chroni
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Compounds and were evaluated for their pharmacokinetic prope
2022-09-29
Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure wa
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In this paper we demonstrate
2022-09-29
In this paper, we demonstrate a ganciclovir based TLC-SERS sensing technique combined with machine learning analysis to quantitatively detect seafood allergen in real spoiled tuna samples. We fabricate a diatomaceous earth TLC plate as a separable SERS-active substrate to detect histamine in artifi
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NMS-873 While the binding of HK to VDAC
2022-09-29
While the binding of HK1 to VDAC1 is strong and continuous, the binding of HK2 to VDAC1 is much weaker, and alternates between a cytoplasmic and a mitochondrial-bound states (John et al., 2011). This dynamic process is regulated by the metabolic and energetic requirements of the NMS-873 and provide
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NHS-LC-Biotin The compounds f and a e
2022-09-29
The compounds 8f and 9a–e were found to be potent inhibitors of both isoforms of GSK-3 as characterized by IC50 values in the low nanomolar range. In addition, all of them showed good selectivities against other kinases. Substituents in the ortho- and para-positions of structure 8 and 9 lead to pote
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Flavonoids are able to modulate proinflammatory signaling pa
2022-09-28
Flavonoids are able to modulate proinflammatory signaling pathways to prevent OS and apoptosis [139]. Paraoxygenase-2 (PNO2) is an enzyme involved in neuroprotection by preventing OS mediated damage in mitochondria. Flavonoids can modulate the JNK/AP-1 pathway to increase expression of PNO2 [111]. F
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Previously localization studies have been conducted using an
2022-09-28
Previously, localization studies have been conducted using antibody-based detection of Pgp protein in tissues of Clade V nematodes. In transgenic C. elegans, Cel-Pgp-3 and Cel-Pgp-1 proteins localized to the apical membranes of the excretory and intestinal cells and the anterior pharynx (Broeks et a
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The standard model of stress postulates the activation
2022-09-28
The standard model of stress postulates the activation of both the sympathoadrenomedullary axis and the hypothalamo-pituitary-adrenocortical axis. Long-term activation of either neuroendocrine axes has been shown to be harmful [12]. Short-term activation of the sympathoadrenomedullary axis is used t
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br NMDA receptor LBDs The study
2022-09-28
NMDA receptor LBDs The study of GluA2 was later expanded to include NMDA receptors [22]. NMDA receptors are obligate heterotetramers that are composed of two glutamate-binding subunits and two glycine-, or d-serine-, binding subunits. In this study, crystal structures of the NMDA receptor glycine
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This data is in accordance with our
2022-09-28
This data is in accordance with our recent results on the influence of cholesterol-depleting agent methyl-β-cyclodextrin on platelets (Borisova et al., 2011a). Dissipation of the proton electrochemical gradient of secretory granules by methyl-β-cyclodextrin did not evoke the release of endogenous gl
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br Regulation of Glu transporters The pivotal role of Glu
2022-09-28
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino Kobe0065 calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcriptio
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br Acknowledgements This work was supported by the
2022-09-28
Acknowledgements This work was supported by the grants from National key Basic Research Program of China (2012CB124702), 948 Program (2015-Z33), National Natural Science Foundation of China (31172093, 31301947), the National Science Foundation for Fostering Talents in Basic Research (J1103510), S
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Introduction Since the development of the
2022-09-27
Introduction Since the development of the first radioimmunoassay (RIA) to measure hormone levels in the late 1950s, for which Rosalyn Sussman Yalow was awarded the Nobel Prize for Medicine in 1977 (the second woman ever receiving it), the use of biotin-LC-LC-tyramide in molecular research has incr
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Similarly spectrophotometric titrations were carried out
2022-09-27
Similarly, spectrophotometric titrations were carried out under conditions identical to those used for the fluorescence titrations. exhibited a predominant LDC000067 band at around 493 nm. The titrations with all G-quadruplex DNAs resulted in a hypochromic effect along with a bathochromic shift of
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