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br Author contribution br Acknowledgements We want to
2021-07-23

Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General
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Due to the high attractiveness of E and E ligases
2021-07-23

Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), LY2584702 (Davydov et al., 2004, Huang et al., 2005, Kenten et al., 2005, Ma
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The modification of proteins with the
2021-07-23

The modification of proteins with the small 76-amino Scrambled 10Panx receptor protein ubiquitin (Ub) plays a central role in many key cellular processes. Ubiquitylation of a target protein requires the concerted action of a cascade of three enzymes (Figure 1). The ubiquitin-activating enzyme (E1)
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Electron transport via DHODH activity will allow the generat
2021-07-23

Electron transport via DHODH activity will allow the generation of mitochondrial ROS without the consumption of α-ketoglutarate or NADH. Glutamine-dependent flux through the TCA cycle and oxidative phosphorylation can also enable generation of mitochondrial ROS (Weinberg et al., 2010). The latter pr
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In rats exposed to day of
2021-07-22

In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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To determine the time course of ZD P CPG DNA
2021-07-22

To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour Spiperone hydrochloride 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, sugg
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Emi protein consists of an N terminal
2021-07-22

Emi2 protein consists of an N-terminal regulatory region and a C-terminal functional region. The C-terminal region contains a destruction box (D-box), which likely competes with APC/C substrates (including cyclin B) for APC/C binding, and a zinc-binding region (ZBR), which somehow inhibits APC/C ubi
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Soon after the discovery of ET
2021-07-22

Soon after the discovery of ET1 and the cloning of its ETA and ETB receptors, low-molecular-weight compounds were identified that can prevent the binding and effects of radioactively labeled ET1 3, 5, 6, 8. Initially, these ERAs resulted from screening efforts (e.g. BQ123 39, 49 and bosentan [50]).
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Table summarizes the literature data available on
2021-07-22

Table 4 summarizes the literature data available on the occurrence of these two dopamine hydrochloride synthesis of steroidal compounds in sludge and sediments. In activated and digested sewage sludge, the concentrations of ethynyl estradiol (17 ng/g), estrone (37 ng/g ), and estradiol (49 ng/g) f
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In mammals ribonucleotide reductase RNR is a unique
2021-07-22

In mammals, ribonucleotide reductase (RNR) is a unique enzyme that catalyzes the rate-limiting step of de novo synthesis of deoxyribonucleoside triphosphates (dNTPs).7, 8 Mammalian RNR consists of two homodimer subunits: the large catalytic dimer RRM1 and the small regulatory dimer RRM2 or RRM2B. An
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Recent studies have reported that
2021-07-22

Recent studies have reported that miR-454 plays an important role in various cellular processes and diseases, such as inflammation, infection, osteogenic differentiation, and cancers [25,27,29,30]. Multiple evidence has documented that miR-454 promotes the proliferation, migration and invasion, and
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The majority of serpins inhibit serine proteases but
2021-07-22

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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The potential off target activity of against other
2021-07-22

The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these d
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br Type II NAD P H Dehydrogenases in Fungi Fermentative
2021-07-21

Type II NAD(P)H Dehydrogenases in Fungi Fermentative YeastSaccharomyces cerevisiaeBecause S. cerevisiae is a facultative sc9 mg yeast capable of meeting its energy requirements with ATP generated by fermentation, only relatively few mitochondrial proteins are essential for cell viability. The mi
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Cdk1/2 Inhibitor III Introduction Formate dehydrogenase enzy
2021-07-21

Introduction Formate dehydrogenase enzymes (FDHs) are a group of heterogeneous proteins that catalyse the reversible formate () oxidation to carbon dioxide () (Eq. (1)). These enzymes are classified in two families, one gathering the enzymes that hold no redox-active centres and another that includ
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