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In summary we discovered azaindole substituted hydroxypyrido
2021-11-08
In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that
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Molecular dynamics studies have proved an effective means
2021-11-08
Molecular dynamics studies have proved an effective means of characterising transition state pathways between the inward- and outward-facing states, and providing the relative propensity for each state. For example, long-timescale simulations of the membrane-embedded LeuT dimer, totalling ∼21 μs, ha
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The ester moiety is a promising structural
2021-11-08
The ester moiety is a promising structural motif at the C-3 position for the development of drug-like molecules. However, the labile C-3 ester bond impels these derivate to be susceptible to plasmatic degradation by esterases and this is natural steroidal metabolic process [39,40]. Hence, the isoste
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In the absence of HH ligand HH signaling is actively
2021-11-08
In the absence of HH ligand, HH signaling is actively maintained in a repressed state by the activity of the HH receptor Patched (PTCH). PTCH is a 12-transmembrane domain protein whose intracellular localization is concentrated at the cmv virus of the primary cilium, a single antenna-like structure
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Many studies support that Gli transcription
2021-11-08
Many studies support that Gli transcription factors are not solely regulated by Hh/smo signaling but are also influenced by crosstalk with other pathways, such as RAS, PI3K/AKT, transforming growth factor-b/SMAD, PKC, or extracellular signal-regulated kinase pathways which are downstream and indepen
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The findings in mice were echoed in the human
2021-11-08
The findings in mice were echoed in the human studies, in which the effects of higher doses of LY3298178 caused greater weight loss than the selective GLP-1RA dulaglutide. In patients with T2DM, LY3298176 demonstrated meaningful weight loss after only four weeks of treatment. This was consistent wit
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Among sensitizers tested in the previous study six test
2021-11-08
Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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In a follow up study the same research group
2021-11-08
In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c
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Recent evidence indicates that prolonged vasoconstriction of
2021-11-08
Recent evidence indicates that prolonged vasoconstriction of conductance and resistance arteries involves VSMCs PLX3397 polymerization, through activation of small GTPases [4] and a subsequently transition to a more solid rheology [5]. Actin polymerization occurs in two steps, nucleation and elongat
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SBI-0206965 synthesis Introduction RNA splicing occurs in th
2021-11-08
Introduction RNA splicing occurs in the nucleus when noncoding sequences (introns) are removed from the pre-mRNA transcript and coding sequences (exons) are joined to form a mature mRNA [1,2]. This reaction is catalyzed by a multiprotein complex called spliceosome. The spliceosome consists of five
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br Methods and materials br Results br Discussion In
2021-11-08
Methods and materials Results Discussion In this study we demonstrate that CF epithelial 6 his exhibit features of apoptosis in their basal, unstimulated state including increased caspase (-3 and -8) activation compared to non-CF epithelial cells. Analysis of factors responsible for this b
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br STAR Methods br Acknowledgments We
2021-11-08
STAR★Methods Acknowledgments We thank the Shanghai Synchrotron Radiation Facility (SSRF) BL18U for help with X-ray data collection. We thank Dr. Thomas F.J. Martin for providing the pcDNA3.1-CAPS-1 plasmid and Dr. Xiaofei Yang for providing the pFHUUIG_shortU6 (l309) plasmid. We thank Dr. Shun
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br Discussion The LISA analysis indicated
2021-11-08
Discussion The LISA analysis indicated that HIV was geographically clustered in the north-west districts of Amhara Region. A high rate of HIV infection was found in Metema and Mirab Armacho districts, which share borders with Eretria and Sudan. Various studies have linked risk of infectious disea
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br Introduction Glycolysis plays a
2021-11-08
Introduction Glycolysis plays a key role in no sodium salt synthesis energy metabolism [[1], [2], [3]]. It is initiated mainly by hexokinase I (HKI), the major hexokinase isoform of the brain ([3,4] and references therein). Up to 90% of brain HKI is bound to the mitochondrial outer membrane (MOM
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br Materials and methods br Author contributions br
2021-11-08
Materials and methods Author contributions Acknowledgments We thank members of the Skaar laboratory for critical evaluation of the manuscript. This work was supported by grants from the National Institutes of Health, R01AI069233 (EPS), and T32GM008554-21 (LJL). Introduction Pseudomonas
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