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In anticipation of an approach based on
2020-12-10
In anticipation of an approach based on modification of the cyclohexylacetic Estradiol valerate subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1,
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br Four active site residues of KSTD
2020-12-10
Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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Indeed a significant difference was observed for
2020-12-10
Indeed, a significant difference was observed for the binding of glycated α-synuclein. Thus, g-α-synuclein bound to other part of GAPDH in 4 of 10 simulations (Fig. 2F, brown, yellow and dark-green chains, and Fig. 2G, brown chain). This additional binding site is located on the interface between O
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Another notable finding in this study is that Cbl b
2020-12-10
Another notable finding in this study is that Cbl-b-mediated ubiquitination accelerates the degradation of phosphorylated DDR2. Cbl family has been documented to facilitate RTK degradation either in proteasome through K48-linked poly-ubiquitination or in lysosome through mono-, multiple mono- and K6
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br Materials and methods br Author contributions br Acknowle
2020-12-10
Materials and methods Author contributions Acknowledgements Supported by grants from the Zhejiang Provincial Natural Science Foundation (LY16H030016, LY17H030012), and the Zhejiang Science and Technology Public Welfare Project (2015C33279), Anesthesiology Center in North of Zhejiang Provinc
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We have previously disclosed the discovery of
2020-12-10
We have previously disclosed the discovery of a 7-azaindole-3-acetic Thiomyristoyl CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that wor
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CTX0294885 Two major mechanisms including apoptosis and oxid
2020-12-10
Two major mechanisms including apoptosis and oxidative stress have been suggested for MTX-induced cytotoxicity (Hafez et al., 2015; Neuman et al., 1999; El-Sheikh et al., 2015). It has been reported that MTX promotes cell death via apoptosis in both cancerous and non-transformed cells (Mazur et al.,
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Population genetic summary statistics for five super
2020-12-09
Population genetic summary statistics for five super- and 26 sub-populations, including haplotype and diplotype frequencies (analogous to allele and genotype frequencies), observed (Ho) and expected (He) heterozygosities, pairwise genetic distances, and tests for detection of departures from Hardy W
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The present study was the first to examine how
2020-12-09
The present study was the first to examine how COMT genotype and estradiol are associated with Pseudo-UTP functioning in healthy postmenopausal women. We hypothesized that with decreased circulating estradiol after menopause, the COMT genotype relationship to cognition would remain and perhaps beco
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The phenolic hydroxyl group of ezetimibe tolerated various s
2020-12-09
The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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An additional difference in ACC between H
2020-12-09
An additional difference in ACC-1 between H. contortus and C. elegans is the results from the oocyte expression experiments. Here we found that unlike Cel-ACC-1 that was reported to form a functional homomeric channel (Putrenko et al., 2005), Hco-ACC-1 does not. However, we have observed that in gen
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Ketoprofen Resistance to avermectins has been associated wit
2020-12-09
Resistance to avermectins has been associated with point mutations of GluCls in C. elegans, D. melanogaster, T. urticae and P. xylostella (Dent et al., 2000; Dermauw et al., 2012; Kane et al., 2000; Kwon et al., 2010; Wang et al., 2016a, 2017). Our electrophysiological study found a 8.2-fold reducti
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br Particle swarm optimization for NLBP br Computational tes
2020-12-09
Particle swarm optimization for NLBP Computational tests Conclusions Acknowledgements This work was supported by the State Key Development Program for Basic Research of China (No. 2009CB421104) and the National Natural Science Foundation of China (Nos. 50809004 & 41071323). Main Text
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So what can we glean from this illuminative foray into
2020-12-09
So what can we glean from this illuminative foray into how Chk1 and MK2 participate in checkpoint control? First and foremost, this work reveals that U 18666A deficient in the tumor suppressor p53 contain two spatially distinct G2/M phase checkpoint control kinase networks. This provides compelling
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br Materials and methods br
2020-12-09
Materials and methods Results and discussion Conclusions The current research work deals with preparation of CES from RHA and comparative study of Ni (II) ion adsorption on CES and RHA. It was observed that carbon embedded silica shows more porous structure and more surface area as compared
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