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Zhang et al screened three thousand compounds library and
2023-01-04
Zhang et al. screened three thousand compounds library and found two active 3,5,6-substituted indolin-2-one molecules. Further, they designed various derivatives of this scaffold and among them compound 23 from the series was found active with 1.8 μM on Aurora-B kinase luminescent assay [53]. Jeffe
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In this study we showed
2023-01-04
In this study, we showed that TRIM48 promotes ASK1 activation through ubiquitination-dependent degradation of a negative regulator of ASK1 activation, protein arginine methyltransferase 1 (PRMT1). Knocking down TRIM48 suppressed oxidative-stress-induced cell death mediated by ASK1, and the additiona
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Chlorogenic acid an abundant polyphenol found in coffee and
2023-01-04
Chlorogenic BIBR 1532 (7), an abundant polyphenol found in coffee and the human diet, has various biological activities including antioxidant and anticancer effects [54]. Jiang et al. reported that compound 7 had a selective cytotoxic activity on human oral tumor cells (HSG, HSC-2) as compared with
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The first and the best characterized mechanism of receptor d
2023-01-04
The first and the best-characterized mechanism of receptor-dependent internalization of Aβ is mediated via the α7-nicotinic MMP-2 Inhibitor I synthesis receptor [82]. Lipoprotein receptor protein represents the second best-studied route that facilitates the uptake of Aβ by neurons, involving additi
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Interestingly metabolic dysfunction is also observed
2023-01-04
Interestingly, metabolic dysfunction is also observed in amyotrophic lateral sclerosis (ALS). Patients and mouse models of familial ALS exhibit higher levels of resting RO 4929097 expenditure and lower fat-free mass, indicating a hypermetabolic phenotype. Lim et al. (2012) found that reducing AMPK a
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br A and tau in Alzheimer
2023-01-04
Aβ and tau in Alzheimer's disease The two classical histopathological hallmarks of AD are extracellular insoluble Aβ deposits, known as Aβ plaques, and intracellular accumulations of insoluble microtubule-associated tau protein, known as neurofibrillary tangles [14]. Aβ peptides are produced as a
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br Experimental Procedures br Acknowledgments We thank
2023-01-04
Experimental Procedures Acknowledgments We thank the members of the Qing laboratory for helpful suggestions and Biotree Biotech Co., Ltd. (Shanghai, China) for metabolomics analysis and data interpretation. This study was supported by the National Key Research and Development Program of China
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MD was the recipient of the Intergroupe Francophone de Canc
2023-01-04
MD was the recipient of the Intergroupe Francophone de Cancérologie Thoracique (IFCT) Alain Depierre Grant in 2014. JP was the recipient of the ARISTOT (Association de Recherche, d’Information Scientifique et Thérapeutique en Oncologie Thoracique) grant in 2016. Conflicts of interest statement
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br Downstream signalling of AKT A
2023-01-04
Downstream signalling of AKT A consensus phosphorylation motif has been described for AKT substrates: R-X-R-X-X-S/T-B where X represents any amino cx 5461 and B represents bulky hydrophobic residues (Alessi, Caudwell, Andjelkovic, Hemmings, & Cohen, 1996). Numerous AKT substrates have been publis
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br ABCA modulates intracellular sphingolipid metabolism in
2023-01-04
ABCA2 modulates intracellular sphingolipid metabolism in the LE/LY Recycling of plasma membrane lipids that occurs by constitutive endocytosis and vesicularization of complex glycolipids, complex sphingolipids and cholesterol as well as free cholesterol liberated from LDL after receptor-mediated
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br Perspectives and challenges Previously the main
2023-01-04
Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular
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GSK180 br Introduction Myasthenia gravis MG is an
2023-01-04
Introduction Myasthenia gravis (MG) is an autoimmune disease characterised by failure of transmission at the neuromuscular junction (NMJ). In 80–85% of myasthenia gravis patients, the disease is mediated by antibodies to the nicotinic GSK180 receptor (AChR; (Lindstrom et al., 1976). Many investig
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In vitro studies with soman inhibited non
2023-01-04
In vitro studies with soman-inhibited, non-aged AChE revealed a species dependent reactivating potency of HI-6 and MMB-4. With guinea pig AChE second order reactivation rate constants of 0.051 and 0.038mM−1min−1 were determined for HI-6 and MMB-4, respectively (Luo et al., 2007). Corresponding value
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In this study we make the first simultaneous recordings
2023-01-04
In this study, we make the first simultaneous recordings of SB 216763 release in multiple brain regions at a temporal resolution less than 1 s. One of the most striking findings is that acetylcholine release has a remarkably similar temporal profile in the mPFC and dHPC, suggesting a coordinated act
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From our in vivo studies and previously reported
2023-01-02
From our in vivo studies and previously reported findings [25], we have found that orteronel possesses excellent oral BA. Indeed, single oral dosing of orteronel at doses of 0.3–10.0mg/kg decreased serum DHEA levels in a dose-dependent manner. Of interest, DHEA levels did not return to levels compar
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