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Two recently developed highly specific EZH enzymatic inhibit
2022-07-21
Two recently developed, highly specific EZH2 enzymatic inhibitors, GSK126 and EPZ-6438, are currently in clinical trials for treating lymphomas (Kim and Roberts, 2016). Although these EZH2 inhibitors have shown antitumor effects in lymphoma cells with enzyme-activating mutations of EZH2 (Knutson et
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Compounds that induce exocytosis in cultured cells include
2022-07-21
Compounds that induce exocytosis in cultured Splitomicin receptor include Ca2+-dependent [14] or Ca2+-independent [15] mechanisms. Ca2+-dependent exocytosis releases soluble enzyme content from lysosomes [16] operating by increasing the cytosolic concentration of Ca2+[13] by recruiting extracellula
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Before discovery of their histone demethylase
2022-07-20
Before discovery of their histone demethylase function, the JARID1 isoforms were identified across diverse fields including stem cell biology and congenital disease, as detailed in Box 2. Their observed roles in cancer progression and therapy resistance have led to ongoing pursuit of inhibitors tail
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Dual H H receptor antagonists developed by
2022-07-20
Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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To search for potential variants of SLA
2022-07-19
To search for potential variants of SLA-DOB and CD4 associated with different (percentage) levels of the five (T-lymphocyte subsets, total antibody IgG, interferon alpha (IFN-α), Toll like receptor 3 (TLR3), interleukin 6 (IL-6) in serum and porcine reproductive and respiratory syndrome virus (PRRSV
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The life cycle of T cruzi requires both vertebrate
2022-07-19
The life cycle of T. cruzi requires both vertebrate and invertebrate hosts. In the insect (invertebrate) vector, the protozoan undergoes extracellular replication, whereas in the mammalian (vertebrate) host it replicates by obligate intracellular multiplication (Rodrigues et al., 2014). Hence, the p
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Resolving the molecular details of glyco proteome variation
2022-07-19
Resolving the molecular details of (glyco)proteome variation in different tissues and organs of the human body is critical for the understanding of human biology and disease [59]. Glycoproteomic analysis of disease-related tissues and cells has provided valuable information to identify promising tar
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Several reports have shown that
2022-07-19
Several reports have shown that the ICD of CLRs is involved in the desensitization process of this superfamily. The analysis of our chimeric constructs between GlyRα1 and GLIC revealed differences in desensitization properties. In contrast, other ion channel properties such as channel block and ion
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PTMs have been shown to influence transporter
2022-07-19
PTMs have been shown to influence transporter kinetics, both directly and indirectly (Xu & You, 2017). They do not just regulate the innate structure-function relationship driven by a transporter's global architecture, but rather are also able to regulate this relationship down to the resolution of
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CCT007093 australia GKRP binds to the inactive super open co
2022-07-19
GKRP binds to the inactive, super-open conformation of GCK, acting as a competitive inhibitor of glucose association with the enzyme (Fig. 3) [45]. Upon formation of the inhibitory complex with GKRP, GCK is sequestered into the hepatocyte nucleus [48]. The detailed mechanism by which GKRP mediates t
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Some other neuroinflammatory neuroendocrine and
2022-07-19
Some other neuroinflammatory, neuroendocrine, and neurotrophic pathway but not the ghrelin/GHSR pathway may mediate the CUMS-induced depression- and anxiety-like behaivors. The endogeous ghrelin/GHSR pathway activated by chronic mild stress may plays a role in homeostasis. With respect to the mechan
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br Materials and methods br Results
2022-07-18
Materials and methods Results Discussion Induction of neuronal cell death is the main neurotoxic mechanism of arsenite (Vahidnia et al., 2007). Previous studies have demonstrated that arsenite may trigger neuronal cell death via apoptosis, autophagy as well as necrosis (Yen et al., 2012; La
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br Acknowledgements We thank Dr Bhushan Nagar and Dr
2022-07-18
Acknowledgements We thank Dr. Bhushan Nagar and Dr. Albert Berghuis for access to the X-ray diffraction machine at McGill University. We also thank Dr. Manon Couture and Dr. Steve Charette at Université Laval for access to scientific equipment. Funding for this research was provided by Discovery
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To date the crystal structures of HIV IN complexed with
2022-07-18
To date, the crystal structures of HIV-1 IN complexed with ligands and related proteins could help us in studying the interactions between the inhibitors and IN. Until now, 114 co-crystal structures of HIV-1 IN with small molecular ligands 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34,
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br Results br Discussion br STAR Methods
2022-07-18
Results Discussion STAR★Methods Acknowledgments The authors thank Drs. Michael Wegner, Ron Waclaw, and Ed Hurlock for critical comments. We thank Drs. Lihui Tsai and Jiang Wu for CHD8 and ASH2L-expressing vectors, respectively, Dr. Yueh-Chiang Hu for generating transgenic lines, and Jing
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