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Historically covalent drugs have had great
2019-09-25
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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One possible explanation for differences in
2019-09-25
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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Consistent with prior reports this study also found the
2019-09-25
Consistent with prior reports, this study also found the level of 11 cytokines (MIF, IL-1Ra, CTACK, M-CSF, Basic FGF, VCAM-1, SDF-1α, IL-8, IL-16, PDGF-β, and GRO-α) significantly decreased in the sera of adult HFMD patients in comparison with controls. MIF is a pro-inflammaory cytokine that is asso
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During host cell interactions G intestinalis trophozoites up
2019-09-25
During host-cell interactions, G. intestinalis trophozoites up-regulate several cell-associated proteins, including high-cysteine membrane proteins (HCMPs) and variant surface proteins (VSPs) [8]. The parasite also releases around 200 proteins upon host-cell contact, including many proteases [9,10].
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The cysteinyl leukotrienes cysLTs LTC
2019-09-25
The cysteinyl leukotrienes (cysLTs) LTC, LTD, and LTE are increased in the airways of asthmatic subjects, with the ability to induce bronchoconstriction, vascular permeability, and mucus secretion., , , , CysLTs are well established as mediators of allergic rhinitis and asthma on the basis of the e
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HC-030031 The use of inhibitors clearly
2019-09-25
The use of inhibitors clearly has its caveats and the field should come to a consensus on etomoxir concentration to maximally block LC-FAO while minimalizing off-target effects. The current papers convincingly show that 200 μM is too high, but it should be noted that 3 μM does not fully suppress LC-
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The aim of this study was to use molecular methods
2019-09-25
The aim of this study was to use molecular methods to characterise C. difficile isolates circulating in the Czech Republic from 2013 to 2015. Material and methods Discussion During a three-year period (2013–2015) a total of 32 hospitals voluntarily participated in this project, but only 11 ho
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As shown in Figs a and b with the SO
2019-09-25
As shown in Figs. 3(a) and (b), with the SO effect, the absolute values of the VDEs change by at most 0.19eV. Table 1 also shows that the observed peak splitting energies in the Sm-Ho complexes were reproduced even without the SO effect. Considering its significant importance in the electronic struc
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Antioxidants such as SFN have been proposed
2019-09-25
Antioxidants such as SFN have been proposed to be chemopreventive agents to inhibit, delay or reverse the development of cancer (Bayat Mokhtari et al., 2018). SFN was shown in breast epithelial cell culture to suppress oxidative metabolism of E2/E1 and thus protect against estrogen-mediated DNA dama
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Due to its several industrial applications the
2019-09-25
Due to its several industrial applications, the recombinant production of collagen and all its derivatives as gelatins has been pursued for many years in different biological systems as mammalian signaling (Toman et al., 1999), tobacco plants (Ruggiero et al., 2000), silkworms (Tomita et al., 2003)
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We continued to investigate the contribution of the EP recep
2019-09-25
We continued to investigate the contribution of the EP1 GSK621 clinical to nociceptive sensitization by utilizing its natural ligand PGE and tested the effect of local subcutaneous injection of PGE (5nmol in 5μl) into one hindpaw on mechanical and heat pain thresholds. Wild-type mice displayed maxi
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Our finding that activating DDR variants are
2019-09-25
Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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At present there have been relatively few studies
2019-09-25
At present, there have been relatively few studies that evaluated potential correlations between pulmonary and pleura metastases, hilar and mediastinal apoptosis inducer nodes, and organs associated with distant metastasis and EGFR mutations [33,34,37]. Further research on these relationships is nee
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One of the most fundamental distinctions between
2019-09-25
One of the most fundamental distinctions between Ub signals is substrate monoubiquitination versus polyubiquitination. With the exception of the E2, UBE2W, which represents a special case because it orbifloxacin only ubiquitinates the flexible N-termini of substrates [5], [6], [20], most examples o
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br Material and methods br Results and
2019-09-25
Material and methods Results and discussion Conclusions Acknowledgements S. De thanks DST, New Delhi for generous grant of the SERC Fast Track Scheme No. SR/FT/CS-057/2008. R. Kundu thanks the University of Kalyani for financial assistance. We are grateful to Prof. K. Bhattacharyya of IA
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