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From the general synthetic route we first
2019-07-26
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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bms-536924 br Materials and methods br Acknowledgements We t
2019-07-26
Materials and methods Acknowledgements We thank Drs. Nathan Sherer (University of Wisconsin-Madison) and Bryan Cullen (Duke University) for generous reagent gifts. The following reagent was obtained through the NIH AIDS Reagent Program, Division of AIDS, NIAID, NIH: HIV-2ROD phage from Dr. Ron
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It was reported that IVM modulates various
2019-07-26
It was reported that IVM modulates various ion channels, such as type-A GABACls, α7 acetylcholine-gated cation channels, P2X4 ATP-gated cation channels, and glycine-gated chloride CEP-37440 in vertebrates (Adelsberger et al., 2000, Khakh et al., 1999, Krause et al., 1998, Krůšek and Zemková, 1994,
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br Introduction Phosphorus P is an important nutrient for
2019-07-26
Introduction Phosphorus (P) is an important nutrient for plant growth; however, in many regions of the world soils are low in plant-available P (Holford, 1997). Therefore, P fertilisers play an important role in agriculture. Most P fertilisers in current use are derived from phosphate rock; howev
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Evidence for interactions between the endothelin and
2019-07-26
Evidence for interactions between the endothelin and the angiotensin system has also become plentiful. It has become clear that the two systems, in addition to acting independently, can act synergistically (Emori et al., 1989, Imai et al., 1992) as well as promote the peptide mRNA expression in endo
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br Molecular characterization of LEI
2019-07-26
Molecular characterization of LEI/L-DNase II LEI, like most serpins, is a metastable protein and its anti-protease activity is related to its “stressed to relaxed transition”. So that, the inhibition of elastase by the well described suicide mechanism generates the cleaved form of LEI (see Padron
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The role of activation of
2019-07-26
The role of activation of xenosensor nuclear receptors such as PPARα, CAR, and PXR in producing hepatomegaly and liver tumors in rodents has been well-established (Klaunig et al., 2003, Lake, 2009). In the case of PPARα, the increase in liver weight results from increased peroxisomal mass and expans
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The two most important biological machineries controlling pr
2019-07-25
The two most important biological machineries controlling proteostasis, PQC, and degradation are autophagy and the ubiquitin-proteasome system (UPS) (). Autophagy is a lysosome-dependent, tightly regulated catabolic process that degrades unwanted cell organelles and cytoplasmic constituents in lysos
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br Experimental Procedures br Author Contributions br
2019-07-25
Experimental Procedures Author Contributions Acknowledgments Research in the Davis laboratory was supported by grants 4R37NS019904, 5R01NS052351, and 1R35NS097224 from NINDS. Research in the Martemyanov laboratory was supported by grants DA036596 and DA026405 from NIDA, and MH105482 from NI
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DNA PK Jackson is activated by DNA double stranded
2019-07-25
DNA-PK (Jackson, 1997) is activated by DNA double-stranded breaks (DSBs). It is a trimeric complex composed of the catalytic subunit, DNA-PKcs, and the Ku70/80 heterodimer. DNA-PK mediates non-homologous end joining (NHEJ), which joins programmed DSBs created during V(D)J recombination and class swi
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Previous synthetic lethal screening efforts Cox et al have
2019-07-25
Previous synthetic lethal screening efforts (Cox et al., 2014) have mainly used RNAi as a means of identifying potential targets (Barbie et al., 2009, Kim et al., 2016, Luo et al., 2009, Scholl et al., 2009), although a few screens (Shaw et al., 2011, Steckel et al., 2012) have been performed with s
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For a physiologically relevant interaction ligand
2019-07-25
For a physiologically relevant interaction, ligand and receptor have to be expressed in the same place. Collagen II is found primarily in cartilage. DDR2 is expressed in proliferating chondrocytes in vivo, and its staining pattern in tibial growth plates is similar to that of collagen II. In additio
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br Materials and methods br Results br Discussion In the
2019-07-25
Materials and methods Results Discussion In the past decade, GWAS have attempted to identify genetic variants that confer risk for many human diseases, whose inherited components remain unexplained (Manolio et al., 2009). In a few cases risk variants identified by GWAS have paved the way fo
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Models and theories The CPA equation of state is
2019-07-25
Models and theories The CPA equation of state is composed predominantly of two parts: physical item and the association item based on the thermodynamic perturbation theory [21], [22], [26], [27]. The physical item is used to represent intermolecular physical interaction, usually representing the SR
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WRTs AI AI and AI showed the same ST as
2019-07-25
WRTs AI-82/1, AI-9-1 and AI-60 showed the same ST as was published by Dingle et al. in RTS 103, 013 and 097 (Dingle et al., 2011). WRTs 015 and 002 were assigned as WRTs 015-like and 002-like due to slight changes in their CE-ribotyping profiles; however, the ST of WRT 002-like (ST8) was identical t
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