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Recent work has detailed the impact of genetic deletion of
2024-05-15
Recent work has detailed the impact of genetic Pridinol Methanesulfonate of AMPK in the liver, revealing only minor phenotypes upon removal in mice (Boudaba et al., 2018). However, these studies very elegantly showed the potential for small molecule-mediated activation of AMPK to elicit large chang
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br Conclusion We have identified three non competitive
2024-05-15
Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina
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Despite extensive studies on the expression of T pallidum
2024-05-14
Despite extensive studies on the expression of T. pallidum-induced pro-inflammatory cytokines, very little is known about T. pallidum-mediated intracellular signaling pathway activation, that leads to cytokine expression in macrophages. A network of signaling molecules, transcription factors, epigen
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An important observation in our
2024-05-14
An important observation in our study is the lack of effect of paroxetine pretreatment alone on β2AR membrane expression, which suggests that paroxetine, and pharmacologic inhibition of GRK2 in general, does not directly induce changes in receptor dynamics. Rather, the decreased ligand-induced β-arr
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The AChR is composed of
2024-05-14
The AChR is composed of five homologous, membrane-spanning subunits. AChRs containing two α, one β, one δ and one γ subunit (AChRγ) predominate during embryonic development and mice lacking AChRγ die at birth (Takahashi et al., 2002). After birth, the AChRγs are replaced during the first 2 postnatal
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Osteoblasts have been thought to be the
2024-05-14
Osteoblasts have been thought to be the major cell type that expresses RANKL (Suda et al., 1999) which is a ligand for osteoprotegerin (OPG) and which functions as a key factor for osteoclast differentiation and activation. Recently, Nakashima and his colleagues (Nakashima et al., 2011) demonstrated
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br Conflict of interest br Acknowledgements We
2024-05-14
Conflict of interest Acknowledgements We thank Ann Jackman, Mike Ormerod and members of Julian Downward's and Alan Ashworth's groups for helpful discussions. This work was supported by grant number PEM/GME/D391/40 from the Kidani Trust (S. Kaye) and by Keele University. Introduction Autota
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NOXA a BH only protein
2024-05-14
NOXA, a BH3-only protein, is best known as a selective inhibitor of MCL-1, which is a highly expressed pro-survival protein in many human malignancies [30]. In addition, NOXA was recently proven to act as a direct activator via directly binding to BAX to induce apoptosis [31]. Given that its levels
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The known crystal structures of class
2024-05-14
The known crystal structures of class C GPCR VFTs do not include attached TM domains, therefore current conformational data may not accurately reflect the dynamics of extracellular domains in full-length receptors. Nevertheless, compelling mechanisms of signal transduction can still be postulated. S
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PTC209 HBr The most likely explanation for the
2024-05-14
The most likely explanation for the species differences in aromatase distribution and the unique PTC209 HBr distribution in humans is the unique location, size and highly elaborate organization of the human aromatase gene (e.g. Bulun et al., 2003). The human Cyp19 is a large gene located on chromoso
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br Materials and methods br Results br Discussion
2024-05-14
Materials and methods Results Discussion In this study, we administrated BDE-153 to newborn rat pups at PND 10 and cultured primary neurons, measured neuronal apoptosis and LDH activity in vivo and in vitro, then explored the possible predominant pathway underlying the neuronal apoptosis by
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Plasma apelin levels predict the major cardiovascular event
2024-05-14
Plasma apelin levels predict the major cardiovascular event after percutaneous coronary intervention in patients with ST elevation myocardial infarction (STEMI), and adverse events are higher in patients with lower plasma apelin levels [75]. Apelin and its receptor are markedly upregulated in the he
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Several strategies have been employed to
2024-05-14
Several strategies have been employed to design and engineer peptide biosensors of kinase activity, which are quite different from the strategies developed to generate genetically encoded KARs. In all cases, HhAntag induces changes in the spectral properties of the fluorophore(s) incorporated into
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Neural activity resulting from sensory experience is require
2024-05-13
Neural activity resulting from sensory experience is required for the refinement and maturation of neural circuits during cortical critical periods. This refinement is thought to be important for functional optimization of primary sensory cortices, enabling critical functions such as feature detecti
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These results validate the docked pose
2024-05-13
These results validate the docked pose of the ALR2-3e complex in comparison to the docked complex of the ALR2-4c complex of which the compound docked completely out of the binding pocket of ALR2 (). This concludes to that the removal of the acetic 17 alpha hydroxylase moiety leads to inactive or w
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