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Besides by substrate and product KSTDs may also be inhibited
2020-07-02
Besides by substrate and product, Δ1-KSTDs may also be inhibited by other steroids. N. simplex ATCC 6946 Δ1-KSTD was strongly inhibited non-competitively by dicortinone (60), a steroidal dimer, and by bis-1-dehydrodicortinone, with values of 0.7 and 0.75 μM, respectively. This enzyme was also inhibi
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br Cysteine proteases as molecular targets for trypanosomati
2020-07-02
Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these str
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LED209 sale br Authors contributions br Acknowledgements br
2020-07-01
Authors’ contributions Acknowledgements Introduction Retinoic LED209 sale is a key signalling molecule in healthy development and in differentiation of stem cells, albeit uncontrolled levels of retinoic acid can lead to mutagenesis [1]. In eukaryotes retinoic acid is made by oxidation of a
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br Results br Discussion Thus the biochemical and structural
2020-07-01
Results Discussion Thus, the biochemical and structural studies of six Maf proteins from different organisms have revealed two subfamilies of new enzymes with the metal-dependent nucleoside triphosphate pyrophosphatase activity against both canonical and noncanonical pyrimidine nucleotides (Yh
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Among prostaglandins PG PGD remained the most elusive specie
2020-07-01
Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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Injurious effects of cigarette smoke CS
2020-07-01
Injurious effects of cigarette smoke (CS) on human health are progressively being acknowledged both in animal and human studies. CS is a highly complex mixture that contains substantive amounts of toxic oxidants, nitric oxide, organic compounds, free radicals and microbial cell components including
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It should be noted that the
2020-07-01
It should be noted that the long-lifetime binding-responsive luminescence of ARC-1528 and ARC-1530 becomes evident only upon illumination with radiation at near-UV range where the excitation of ATB or ASB moiety is possible. At higher wavelength range (visible light), the fluorophore (5-TAMRA) can b
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br Discussion The present study found
2020-07-01
Discussion The present study found cholinesterase activity in Saccostrea sp. to vary significantly among three tissue types (digestive gland, gills, adductor muscle) and to respond differentially to four toxicants, three of which were non-organophosphates. Furthermore, a comparison of enzyme acti
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br Materials and methods br Results br Discussion Approximat
2020-07-01
Materials and methods Results Discussion Approximately 90% of pulmonary emphysema causes are related to smoking and its progression in patients and are characterized by severity levels [5]. Experimental models using CS to induce emphysema are widely used because they resemble the emphysema
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br Rationale and hypothesis To discover an allosteric inhibi
2020-07-01
Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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One architecture termed closed has been visualized at near
2020-07-01
One architecture, termed closed, has been visualized at near-atomic resolution in cryo-EM maps of recombinant complexes that superimpose with earlier lower-resolution EM data obtained for APC/CCDC20–MCC purified from HeLa CGP 55845 hydrochloride arrested during the mitotic checkpoint (Figure 4E) 38
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br STAR Methods br Acknowledgments We are grateful to
2020-07-01
STAR★Methods Acknowledgments We are grateful to Matthias Mayer at ZMBH in Heidelberg for access to his CD-spectrometer and his help in data interpretation. Technical support by Wolfgang Weinig is gratefully acknowledged. This project was financially supported by the European Union as part of t
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br Electron transfer pathway Intramolecular or inter
2020-07-01
Electron transfer pathway Intramolecular (or inter-domain) electron transfer (IET) in CDH has been studied in much depth [], and similar IET occurs in CcPDH, from the PQQ cofactor in the AA12 domain to the heme b in the AA8 domain. When two kinds of electron acceptors are used for measuring enzym
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Atg cleaves Atg at the peptide bond
2020-07-01
Atg4 cleaves Atg8 at the peptide bond on the glycine residue at the C-terminus, thus allowing the conjugation of Atg8 to phosphatidylethanolamine (PE) with the participation of other autophagy molecules. Atg4 can also serve as a deconjugating enzyme, which cleaves the amide bond of the conjugated At
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In order to validate the ATP
2020-06-30
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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