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The biology of the A BR
2023-09-27
The biology of the A2BR is complex and needs to be considered contextually as the expression and effect of receptor engagement varies according to time post hypoxic injury, cell type and downstream signaling pathway. For example, A2BR expression is dynamic - low under basal and increasing under isch
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A high throughput small molecule
2023-09-27
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found OSMI-1 to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was perfo
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br Materials and methods br Results and discussions
2023-09-26
Materials and methods Results and discussions Conclusion Fermented camel milk with NS4 exhibited remarkable ACE-inhibitory activity, which revealed its potential application for the preparation of fermented camel milk beverage or fermented camel milk derived peptides in different foods or i
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Valrocemide The hippocampus is the primary brain
2023-09-26
The hippocampus is the primary brain structure involved in learning and memory. The role of hippocampal synaptic plasticity in neurological processes in cognition and depression has been extensively demonstrated. Synaptophysin is a critical substance in synaptogenesis, which is necessary for learnin
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br The future of cancer therapeutics with Aurora kinase
2023-09-26
The future of cancer therapeutics with Aurora kinase inhibitors Involvement of Aurora kinases in deregulating multiple tumor suppressor and oncogenic pathways together with the preclinical findings on the efficacy of Aurora kinase inhibitors in attenuating growth of tumor Actinomycin D suggests
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Our outcrossing data confirmed that ACL
2023-09-26
Our outcrossing data confirmed that ACL1 and ACL2 have important temporal and spatial functions in ascospore delimitation in G. zeae. When each ACL deletion mutant was used as male for outcrossing, nuclear division and spore delimitation were not properly progressed in most asci. Ascospores that con
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br Metabolic effects of apelin in obesity
2023-09-26
Metabolic effects of apelin in obesity and type 2 diabetes Mice fed a high fat diet (HFD) for several weeks become obese, hyperglycemic, hyperinsulinemic and insulin resistant. Acute apelin treatment by intravenous injection or by infusion during a hyperinsulinemic–euglycemic clamp in obese and i
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br Funding This study was supported
2023-09-26
Funding This study was supported by a grant from the Science and Technology Program of Guangzhou (No. 2014Y2-00181) and the personnel training program of Southern Medical University (No. PY2015N023). Conflict of interest statement Authors’contributions Introduction Chronic cerebral hypo
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Interestingly intermittent high doses of AKT
2023-09-26
Interestingly, intermittent high doses of AKT inhibitors have been shown to be a more effective strategy both clinically and pre-clinically. High doses appear to be required for induction of apoptosis and intermittent schedules overcome the low therapeutic index of these compounds. This is particula
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The identification of novel kinase inhibitor scaffolds is
2023-09-25
The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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Telomerase action at the telomere is highly regulated it
2023-09-25
Telomerase action at the telomere is highly regulated; it preferentially elongates the shortest telomeres, and recruitment of the enzyme complex to the telomere occurs in mid-S phase of the cell cycle (Bianchi and Shore, 2007, Britt-Compton et al., 2009, Teixeira et al., 2004, Hemann et al., 2001, T
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br Concluding remarks and future
2023-09-25
Concluding remarks and future perspectives While the rational engineering of protein-based switches has yet to be fully developed, emerging empirical rules facilitate the construction of tailor-engineered c-Myc Peptide with custom input and output parameters. Both in the context of molecular diag
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br Angiotensin receptor neprilysin inhibitors Sacubitril val
2023-09-25
Angiotensin receptor-neprilysin inhibitors Sacubitril/valsartan is the first-in-class ARNI, comprising of molecular moieties of valsartan (ARB) and a neprilysin inhibitor prodrug, sacubitril (AHU377) [51]. Upon ingestion, sacubitril is rapidly metabolised into an active neprilysin inhibitor, sacu
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Perforation of the surface membrane however is not
2023-09-25
Perforation of the surface membrane, however, is not the only mechanism of calcium dysregulation by Aβ at the presynaptic terminals. When in excess, both monomers and oligomers modulate biophysical properties of voltage-activated calcium GSK 0660 australia as well as calcium release from the endopla
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Calcium entry through postsynaptic NMDARs activates intracel
2023-09-25
Calcium entry through postsynaptic NMDARs activates intracellular signaling cascades including Ca2+/calmodulin (CaM)-dependent protein kinase II (CaMKII) and calcineurin. The spatiotemporal abundance of this Ca2+/CaM complex determines the direction of synaptic plasticity, resulting in LTP (Malinow
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