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TNKS 22 Analysis of Table shows that
2021-08-11
Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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Acknowledgments br Prostaglandin D PGD plays a key
2021-08-10
Acknowledgments Prostaglandin D (PGD) plays a key role in mediating allergic reactions such as those seen in asthma, allergic rhinitis, atopic dermatitis and allergic conjunctivitis. PGD is the major cyclooxygenase product formed and secreted by activated mast cells and its levels in bronchoalveo
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To assess which export pathway is used by the
2021-08-10
To assess which export pathway is used by the iNOS mRNA, we inhibited CRM1 activity by incubation of DLD-1 3mb australia with LMB. Since LMB covalently and exclusively binds to CRM1, it represents a potent and specific inhibitor of the CRM1 transport activity [38]. Inhibition of CRM1 activity as we
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To determine the time course of ZD P CPG DNA
2021-08-10
To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour cftr channel were exposed to the drug for 10, 30 or 60 min. The levels of DNA interstrand cross-links in HT29 or LS174T cells did not increase with exposure time, suggesting that
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We have previously reported the characterization of A a nove
2021-08-10
We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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URB597 We have previously shown that sustained pCPT treatme
2021-08-10
We have previously shown that sustained 8-pCPT treatment favored Ca2+-dependent arrhythmogenic activity in rat ventricular cardiomyocytes [8]. Fig. 2 shows line-scan Ca2+ images of myocyte incubated without (Fig. 2A left) and with 8-pCPT (Fig. 2A right) subjected to a train of electrical stimulation
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br Conclusions Enzyme prodrug therapy mediated by implantabl
2021-08-10
Conclusions Enzyme prodrug therapy mediated by implantable biomaterials combines the benefits offered by the site specific drug delivery techniques and the systemic administration of drugs. From the former, SMEPT inherits the localized mode of drug delivery with lower systemic distribution of the
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While a number of studies
2021-08-09
While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub FRAX486 sale specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-RING interface in governing su
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AMPHs facilitate dopamine release which further triggers
2021-08-09
AMPHs facilitate dopamine release, which further triggers dopamine depletion [72]. Indeed, we observed that repeated treatment of MPA significantly inhibited TH-, DAT-, and VMAT-2 levels. Since DAT and VMAT-2 are important for dopaminergic terminal markers [10], their decreases suggest that MPA-indu
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br Materials and methods br Results br Discussion
2021-08-09
Materials and methods Results Discussion Although autophagy is known to be implicated in the therapeutic effect of DNA alkylating agents such as MNNG [28], [29], [30], the molecular mechanisms underlying autophagy induced by MNNG remain largely elusive. In this study, we present evidence sh
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Several authors have been pursuing the
2021-08-09
Several authors have been pursuing the aim of finding good performing organic solvent compatible adsorbers useful in the context of API purification [[10], [11], [12], [13], 22, 23]. For sulfonate GTIs, scavenging nucleophilic resins [22, 23] or molecular imprinted polymers (MIPs) [10] have been exp
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An AmDH is engineered by mutating
2021-08-09
An AmDH is engineered by mutating two conserved amino Genistein synthesis residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions, respectivel
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As temperatures increase rates of spontaneous deamination al
2021-08-09
As temperatures increase, rates of spontaneous deamination also increase such that hyperthermophilic organisms must have efficient mechanisms for dealing with this potential hazard.8., 9. The hyperthermophile Methanococcus jannaschii has both a dCTP deaminase (encoded by the gene at locus MJ0430) an
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br Acknowledgements These studies were supported by
2021-08-09
Acknowledgements These studies were supported by a research grant from the NIH (R01 AR065594) to C. Putterman. Introduction Macrophages integrate and adapt to their locally encountered cytokine and chemokine milieu. In tumors characterized by an unresolving inflammation, the tumor cell-killin
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br Experimental br Results and discussion br
2021-08-06
Experimental Results and discussion Conclusions The fungus Mucor circinelloides MUT44, previously shown to have ene-reductase activity [11], possesses ten genes coding for putative ene-reductases belonging to the Old Yellow Enzymes family. Since the reduction of CC double bonds is one of th
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