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br Results br Discussion br
2020-03-12
Results Discussion Experimental Procedures Acknowledgments In the preceding paper, we reported 3-amido-4-anilinoquinolines as highly selective inhibitors of CSF-1R kinase, along with our initial efforts to optimize the series. Examples from the 6,7-dimethoxyquinoline series were very p
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Epigenetic silencing of genes that
2020-03-12
Epigenetic silencing of genes that determine tumor invasiveness, growth patterns of tumors, and tumor-cell apoptosis12, 29 may also affect the expression of drug-metabolizing enzymes, thereby providing an additional genetic mechanism in pharmacogenomics. Trisomy 8 that contains wild-type GGH could b
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Introduction The inflammation process involves sequential
2020-03-12
Introduction The inflammation process involves sequential activation of signaling molecules, pro-inflammatory mediators, such as prostaglandins, leukotrienes, and oxygen free radicals [1]. Two cyclooxygenases met inhibitor were responsible for activation of the production of prostaglandins (PG1s)
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br Results and discussion br Conclusion In this investigatio
2020-03-12
Results and discussion Conclusion In this investigation, pharmacophore models of CK1 inhibitors were developed using a pharmacophore modeling protocol proposed by us. The optimal pharmacophore hypothesis, Hypo2, was adopted to retrieve potential CK1 inhibitors from the commercial chemical data
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While we previously demonstrated that TraG is inhibited by s
2020-03-12
While we previously demonstrated that TraG is inhibited by specific transglycosylase inhibitors and that enzymatic activity is strongly reduced upon mutation of the potential catalytic core (Arends et al., 2013), the enzymatic mechanism of both domains was not assigned. Here, by mass spectrometry an
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Introduction CYP is a superfamily of
2020-03-12
Introduction CYP450 is a superfamily of heme-containing monooxygenases, many of which are expressed in the liver, and they are significant phase-I C-type natriuretic peptide (1-22) (human, rat, swine) in drug metabolism and detoxification. There are three subfamilies (CYP1, CYP2 and CYP3) that are
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With respect to bone metabolism and
2020-03-12
With respect to ‘bone metabolism and ossification’-related genes, treatment of SaOS-2 osteoblast-like Quinidine with MS-10 up-regulated IGFBP-4, TG2, and SOST. Up-regulation of IGFBP-4 in SaOS-2 cells inhibits DNA and protein synthesis induced by IGF-1 (Kudo et al., 1995, Kudo et al., 1996). In add
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A key inciting event in
2020-03-12
A key inciting event in atherosclerosis is the deposition of circulating low-density lipoprotein (LDL) in the subendothelial space of major arteries. In the subendothelium, native LDL is no longer protected by circulating antioxidants and is oxidatively modified to oxidized LDL (OxLDL) [5]. OxLDL is
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The two most important biological
2020-03-12
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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In the current study cocaine did not
2020-03-12
In the current study, cocaine did not significantly increase negative subjective effects and nepicastat did not increase these responses. This outcome is somewhat surprising given that the most commonly reported effect to date has been to increase the aversive properties of cocaine such as anxiety,
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To ascertain separation of the
2020-03-11
To ascertain separation of the distinct enzymatic activities found in this protein preparation following separation on the HAP column, a rigorous quantitative analysis was conducted on the nickel–agarose elution and HAP FT pools of protein. For these analyses, each pool of protein was dialyzed in th
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In this report we evaluate if
2020-03-11
In this report, we evaluate if this molecular mechanism is used universally by high-fidelity DNA polymerases during the replication of DNA lesions that are structurally distinct from abasic sites. This was approached by quantifying the kinetic parameters for the incorporation of modified and non-nat
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Despite its significance in tumor suppression the
2020-03-11
Despite its significance in tumor suppression, the molecular mechanism by which DAPK is regulated and its interplay with other tumor suppressors and oncoproteins have not been completely unraveled. Although primarily regulated by CaM binding (Cohen et al., 1997), DAPK activity can also be modulated
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HEK cells stably transfected with CysLT were
2020-03-11
HEK-293 Dehydroepiandrosterone stably transfected with CysLT1 were stimulated with LTD and internalization was studied by confocal microscopy, FACS or cell-surface ELISA. Cells were co-transfected with wildtype and dominant negative (DN) mutants of arrestin and dynamin. Clathrin-mediated endocytos
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tcid br Conclusion br Conflict of interest br
2020-03-11
Conclusion Conflict of interest Acknowledgments The authors extend their appreciation to the Deanship of Scientific Research at King Saud University for funding the work through the research group project No. RGP-120. Introduction Methods Results Conclusions Introduction Pat
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