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A high throughput screening campaign
2024-02-20
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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Autocrine regulations of several adipokines e g leptin
2024-02-20
Autocrine regulations of several adipokines (e.g., leptin and resistin) on adipocytes have been reported (Karastergiou and Mohamed-Ali, 2010, Ye et al., 2010). Several lines of evidence have shown that apelin influences adipocyte functions, such as, lipolysis and glucose uptake (Dray et al., 2008, Y
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The physiologic conditions and signaling mechanisms that reg
2024-02-20
The physiologic conditions and signaling mechanisms that regulate apelin secretion and APLNR expression in malignant tissues appear to be multifactorial. Previous studies have shown that hyperplastic and neoplastic cholangiocytes secrete a variety of hormones, peptides, and growth factors that help
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Oxipurinol br Antibiotic drug discovery approaches Tradition
2024-02-20
Antibiotic drug discovery approaches Traditionally, novel Oxipurinol were largely discovered by phenotypic screening approaches of various sources of compounds, such as natural products isolated from extracts of soil microbes and semi-synthetic or fully synthetic compound libraries derived from k
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Based on structure activity relationship of
2024-02-19
Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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br Author Contributions br Acknowledgments br Introduction C
2024-02-19
Author Contributions Acknowledgments Introduction Cerebral ischemia-reperfusion (I/R) injury is a pathological phenomenon that occurs after restoration of blood supply to Vandetanib hydrochloride tissues subsequent to ischemia or hypoxia (Carden and Granger, 2000). It typically occurs afte
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NPE-caged-proton However relatively little information is av
2024-02-19
However, relatively little information is available concerning the biochemical properties and other features of such enzymes in Taeniid species. In the current report, a M17 leucine aminopeptidase gene of T. pisiformis (TpLAP) was cloned and expressed, and its enzymatic activity, biochemical propert
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br Does TIPARP contribute to the diverse species sensitivity
2024-02-19
Does TIPARP contribute to the diverse species sensitivity to TCDD toxicity? In chick embryo hepatocytes TIPARP was reported to mediate the TCDD-dependent suppression of hepatic gluconeogenesis, by reducing cellular NAD+ levels and reducing PCK1 expression, suggesting that ADP-ribosylation enhance
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Daun02 Another interesting interaction concerns NMDA precond
2024-02-19
Another interesting interaction concerns NMDA preconditioning to protect against glutamate neurotoxicity. It has been shown that an A1R antagonist prevented neuroprotection evoked by NMDA preconditioning against glutamate-induced cellular damage in cerebellar granule cells. In this study, the functi
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Firms are subject to corporate taxation and
2024-02-19
Firms are subject to corporate taxation, and face either an ACE or a CBIT tax scheme. The two tax regimes achieve financing neutrality by treating debt and equity equally, but differ according to whether deduction of capital costs from the corporate tax 49 9 is allowed or not. While ACE allows for
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br Conclusion br Acknowledgments This research has been supp
2024-02-19
Conclusion Acknowledgments This research has been supported by the Ratchadaphiseksomphot Endowment Fund 2013 of Chulalongkorn University (CU-56-341-AS) and the Ratchadapiseksompotch Fund (RA55/22), Faculty of Medicine, Chulalongkorn University. The authors commemorate the 100th Anniversary of
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With regard to the first question subcellular fractionation
2024-02-19
With regard to the first question, subcellular fractionation studies revealed that BDK and PPM1K are clearly detectable in both the mitochondrial and cytosolic subcellular fractions, thus making it possible for these enzymes to interact with both the BCKDH and ACL substrates. The preferential presen
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br Discussion Herein we demonstrate that mice deficient
2024-02-19
Discussion Herein, we demonstrate that mice deficient in L-12/15 LO are more sensitive to 3-NP-induced toxicity although a substantial individual variability in striatal lesion size in response to 3-NP in both genotypes was observed. This variability is not atypical; several studies demonstrate s
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Over the years measures of total antioxidant status
2024-02-19
Over the years, measures of total antioxidant status (TAS) have been developed to capture the collective effect of antioxidant defense capacity, including enzymatic and nonenzymatic systems (Fraga et al., 2014, Franco et al., 2007). Multiple antioxidant enzymes, as well as antioxidant vitamins and m
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Once apoptosis has been initiated the HMGA proteins themselv
2024-02-19
Once apoptosis has been initiated the HMGA proteins themselves undergo marked changes in both the types and extent of their post-translational modifications (PTMs; review in [149,175]), some of which are likely correlated with alterations in chromatin structure. For example, the early stages of apop
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