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The amyloid precursor protein APP is a membrane protein thou
2022-05-04

The amyloid precursor protein (APP) is a membrane protein thought to be involved in plasticity, synapse formation and repair, and export of metal ions [68]. The APP present in the brain can be cleaved by three different secretases [73], [74]. Cleavage of APP first by alpha secretase and then gamma-s
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Our overall goal is to develop selective compounds for
2022-05-04

Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and
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To get a broader view of
2022-05-04

To get a broader view of the interplay between glycolysis and Hippo signaling, we tested the involvement of YAP1 in the regulation of C-MYC and GLUT1 expression. We were able to detect a YAP1-TEAD1 interaction in the nuclear fraction of Jurkat parp inhibitor and confirm the inhibition of this inter
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br Xenobiotics and the Glucocorticoid Receptor br Conclusion
2022-05-04

Xenobiotics and the Glucocorticoid Receptor Conclusion Transparency document Acknowledgements The author wishes to thank Professor Wilhelm Engström from the Swedish University of Agricultural Sciences (Department of Biomedical Sciences and Veterinary Public Health) for his proof reading
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Ulimorelin also known as TPZ is
2022-05-04

Ulimorelin, also known as TPZ101, is a macrocyclic molecule that is a potent agonist of the ghrelin receptor (Hoveyda et al., 2011). Due to its ability to stimulate gastrointestinal motility, ulimorelin has been evaluated as a possible treatment in gastroparesis (Ejskjaer et al., 2010), ileus (Frase
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The release of FBPase and aldolase from
2022-04-29

The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle TAME mg was about 6–7 times higher in the presenc
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Although oxidative stress induces a decrease in intracellula
2022-04-29

Although oxidative stress induces a decrease in intracellular ATP level, the underlying mechanism is obscured. We hypothesized that oxidative stress induced by H2O2 could decrease astrocytes ATP level through lysosome exocytosis in Ca2+-dependent pattern. In present study, using H2O2 stimulation to
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Since stroke and cerebrovascular diseases were
2022-04-29

Since stroke and cerebrovascular diseases were considered serious AEs following vaccination, we performed manual chart review to confirm the diagnosis and symptom onset date for all stroke and cerebrovascular disease cases identified by ICD-9 codes. Chart review of 131 presumptive cases confirmed 82
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Though studied less extensively than in
2022-04-29

Though studied less extensively than in cholangiopathies and fatty liver diseases, the Hh pathway is active in other forms of human liver disease, such as Schistosomiasis[58], [101] and chronic viral hepatitis,[100], [125] as well as in several animal models of liver disease, including drug-induced
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br An approach for the key challenges facing forensic
2022-04-29

An approach for the key challenges facing forensic science One of the key challenges for forensic science is to avoid being side-tracked by one of the louder narratives in the media that the big problem forensic science faces is ‘junk science’ and ‘rogue scientists’. These are clearly important i
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br STAR Methods br Acknowledgments We thank Prof
2022-04-29

STAR★Methods Acknowledgments We thank Prof. Y. Tomari at the University of Tokyo for experimental advice and K. Hanada for technical assistance. This research was supported by Grants-in-Aid for Scientific Research on Innovative Areas “Nascent Chain Biology” (JP15H01548 and JP17H05677 to T.I. a
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Of xenobiotic quinones thymoquinone methyl
2022-04-29

Of xenobiotic quinones, thymoquinone (2-methyl-5-isopropyl-1,4-benzoquinone; Fig. 1) is one of the most thoroughly studied for its pharmacological properties. It is the most active component of Nigella sativa, commonly called black cumin2, 3, the essential oil of the seeds of which are used for trea
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A repertoire of cytotoxic payloads is increasing
2022-04-29

A repertoire of cytotoxic payloads is increasing; among those, MMAE has been utilized for the highly effective ADC brentuximab vedotin. However, the ADCs which utilized MMAE to target GCC in solid tumors have shown a poor efficacy suggesting that various tumor types respond differently to a given to
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With able to modulate inflammation and effect obesity
2022-04-26

With ω3 able to modulate inflammation and effect obesity-related outcomes, it is of interested that two G-protein coupled receptors (GPCR), GPR120 and GPR40, were recently deorphanized and shown to recognize ω3 acids (docosahexaenoic, C22:6; eicosapentaenoic, C20:4; and α-linolenic, C18:3), as well
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G protein coupled receptor GPCR ligands can
2022-04-26

G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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