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The strand domain swap in the UbV XR dimer appears
2021-08-12

The β strand domain swap in the UbV.XR dimer appears to be a unique arrangement for a Ub-based dimer. In solution, free Ub has a KD of ∼5 mM for the monomer-dimer equilibrium, and the two subunits in the dimer adopt a range of relative orientations involving residues from Ub’s β sheet (Liu et al., 2
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Autoradiography studies have shown cerebellum to be devoid o
2021-08-12

Autoradiography studies have shown RG7388 to be devoid of D1-R [40], confirming that this region may serve as reference for estimation of free and non-specifically bound radioligand concentration in tissue (= non-displaceable uptake). In initial human studies using [11C]SCH 23390 and [11C]NNC 112, q
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DNA methylation assay To test the biological activity of pur
2021-08-12

DNA methylation assay. To test the biological activity of purified A1S_0222, a methylation assay was performed using the Int1 DNA. As an alternative DNA substrate, Seq3 (located in gene A1S_0965 of A. baumannii ATCC 17978) was amplified from Acinetobacter baumannii 29D2 using the oligonucleotides Se
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br Materials and methods br
2021-08-12

Materials and methods Results Discussion In this paper, we have demonstrated application of the glmS ribozyme reverse genetic tool for chemogenomic profiling in Plasmodium spp. This tool can provide robust attenuation of expression for different target genes, across different strains varyin
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We have previously reported DAPK
2021-08-12

We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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Cholera Toxin Cytochrome P CYP enzymes plays an
2021-08-12

Cytochrome P450 (CYP-450) enzymes plays an essential role in pharmacology of drugs and toxicology of xenobiotics. Inhibition of these enzymes may lead to increase plasma levels of a concomitantly administered drug (Lee et al., 2013). It may prolong or reduce the pharmacological effects and increase
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Compounds were screened for their activity against the
2021-08-11

Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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Kumar et al studied Umbelliferone
2021-08-11

Kumar et al. studied Umbelliferone β-D-galactopyranoside (UFG) (benzopyrone), found in many plants exhibiting numerous pharmacological actions. The results of the study showed that UFG in a dose of 10, 20 or 40mgkg-1 per day, helps to prevent paw edema and arthritic score development for arthritis i
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Second when considering the Poisson point process the high d
2021-08-11

Second, when considering the Poisson point process, the high-density or large-radius limit of the percolation probability tends to 1 exponentially fast and is governed by the isolation probability. In the random environment, the picture is more subtle since the regime of a large radius is no longer
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br Agonist binding ETA activation
2021-08-11

Agonist binding ETA activation is promoted by binding of the endogenous peptidergic agonists to their orthosteric binding site on the receptor. ET1 and ET2 (Trp6-Leu7-ET1) bind with equal high affinity to ETA, whereas the third endogenous isopeptide ET3 (Thr2-Phe4-Thr5-Tyr6-Lys7-Tyr14-ET1) binds
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br Funding This work was supported by the National Natural
2021-08-11

Funding This work was supported by the National Natural Science Foundation of China (grant number 81671411); Beijing Natural Science Foundation (grant number 7162062); Beijing Nova Program Interdisciplinary Cooperation Projects (grant number Z161100004916045); Beijing Municipality Health Technolo
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br Materials and methods br Results
2021-08-11

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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Other studies have investigated the role
2021-08-11

Other studies have investigated the role of HDAC inhibitors in particular signaling pathways mediated by EWS–FLI1 (Matsumoto et al., 2001). A recent investigation, showed a physical association of EWS–FLI1 and HDAC1 that helps mediate a disruption in the p53 activation of downstream targets (Li et a
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The majority of serpins inhibit
2021-08-11

The majority of serpins inhibit serine proteases, but serpins that inhibit caspases or papain-like cysteine proteases have also been identified [4], [5]. Inhibitory serpins are ‘suicide’ or ‘single use’ inhibitors that use a unique conformational change to inhibit proteases. This conformational tran
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br Effects of culture conditions on drug
2021-08-11

Effects of culture conditions on drug-induced gene Tazobactam sodium salt in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment that ar
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