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Among the compounds prepared at this
2022-07-08

Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with modera
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cantharidin synthesis br Materials and methods br
2022-07-08

Materials and methods Results Discussion The GO system is an important mechanism for maintaining the integrity of genetic material in many eukaryotic organisms. This is demonstrated by the high conservation, across different evolutionary lineages, of the sequences of the proteins that compo
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antimalaria medication The calculations for the R substrate
2022-07-08

The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn antimalaria medication is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but with exc
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The advent of next generation
2022-07-08

The advent of next-generation sequencing (NGS) has shown that considerable variation in human genome is still undiscovered and therefore a considerable number of rare variations that are related to disease susceptibility may still be unknown. NGS has allowed to strengthen the association between los
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Hippo signaling is an emerging tumor suppressor pathway that
2022-07-08

Hippo signaling is an emerging tumor suppressor pathway that plays key roles in normal physiology and tumorigenesis through the regulation of cellular proliferation and survival [4]. In humans, YAP is over-expressed as a result of genomic amplification of the 11q22 locus in a wide spectrum of human
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br Acknowledgements This work was supported by the grants fr
2022-07-08

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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Extending time action is another strategy
2022-07-07

Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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D appears to be important for receptor
2022-07-07

D83 appears to be important for receptor function as a mutation to an alanine produced a non-functional channel. Interestingly, maintaining the charge as in D83E produced only a small reduction in GABA sensitivity. Other mutations at this position which included residues capable of hydrogen bonding
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Another TKI used in cancer
2022-07-07

Another TKI used in cancer therapy is the Abl inhibitor imatinib mesilate which has also a beneficial effect on glucose homeostasis in diabetic humans [39], [40], [41]. Imatinib has a clear impact on NFκB activation and anti-apoptotic preconditioning of β-cells [39], attenuating islet inflammation [
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br Introduction The term autophagy
2022-07-07

Introduction The term “autophagy” was coined by Christian de Duve in 1963 to describe the process of removing and degrading intracellular components such as unused proteins and damaged organelles through lysosomes [1,2]. Autophagy has been divided into three main types, namely, macroautophagy, mi
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Arsenic is generally found in the form of iAs in
2022-07-07

Arsenic is generally found in the form of iAs in arsenic plants. Arsenic is primarily metabolized in the liver through methylation processes. Human metabolism of arsenic results in the formation of the methylarsenic metabolites, MMA and DMA, which are more water soluble (Khaleghian et al., 2014; Wei
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Adipocytes play diverse roles in
2022-07-06

Adipocytes play diverse roles in energy homeostasis by controlling energy consumption [8] and function as a source of proteins and cytokines, which mediate numerous physiological functions [9]. Excessive accumulation of adipocytes, as well as an increase in either their size or number, causes obesit
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Histone acetylation is regulated by
2022-07-06

Histone acetylation is regulated by two groups of enzymes, histone acetyltransferases (HATs) and deacetylases (HDACs), with antagonizing functions (Wang et al., 2009b). Among members of HATs, p300 and CBP are homologous. Both are global transcriptional co-activators (Ogryzko et al., 1996), and play
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Nazar and colleagues reported a normal HER gene
2022-07-06

Nazar and colleagues reported a normal HER2 gene number in 13 primary and 2 recurrent ethmoid sinus adenocarcinomas, without any histological and immunohistochemical characterization, so a comparison with the present findings is impossible [14]. More recently, 552 head and neck carcinomas have been
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Platycodon grandiflorum is a member of the genus
2022-07-06

Platycodon grandiflorum is a member of the genus Platycodon and is commonly known as balloon flower. In East Asia, P. grandiflorum is used for the treatment of asthma, coughs, inflammatory diseases, pulmonary tuberculosis, and diabetes (Takagi and Lee, 1972). Furthermore, recent studies have reporte
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