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br Introduction Protein modification by
2020-10-27
Introduction Protein modification by ubiquitin and ubiquitin-like proteins is one of the most common and important regulatory mechanisms in biology (Finley et al., 2004, Pickart, 2004). Ubiquitination is carried out by an enzymatic cascade consisting of three steps. In the first step, ubiquitin
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Since the initial identification of DNA ligase inhibitors
2020-10-27
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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br Conclusion br Competing interests br Authors contribution
2020-10-27
Conclusion Competing interests Authors\' contributions Acknowledgements The work was supported by Aurigene Discovery Technologies (M) Sdn. Bhd., Industrial Doctoral Program sponsorship by Ministry of Higher Education, Malaysia and research grants by the University of Malaya, grant number
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br Four active site residues of KSTD are
2020-10-27
Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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br Discussion The differences in
2020-10-27
Discussion The differences in the kinetic properties of L-AmDH and LeuDH presented herein reflect a different kinetic mechanism. When compared to its parent enzyme, L-AmDH displayed a different substrate binding order, lower affinity for the keto substrate, and stronger product inhibition. The tw
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Moreover the imbalance between pro and anti inflammatory
2020-10-27
Moreover, the imbalance between pro and anti-inflammatory cytokine production is present in various types of diseases. The use of substances able to induce anti-inflammatory cytokines could represent an important advance in the therapeutic treatment of a range of diseases. In this context, medicinal
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SB-715992 Experiments on the rat model
2020-10-27
Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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As previously reported azole class antifungal drugs inhibit
2020-10-27
As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le
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D609 mg Published results have revealed relationships betwee
2020-10-27
Published results have revealed relationships between serine 81 in AR and some CDKs, especially CDKs 1, 5 and 9 [12], [13], [14], [15], [16]. These results are often supported by pharmacological inhibition of a certain CDK. An effect of CDK1 inhibition on suppression of S81-phosphorylation was previ
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Two additional hydrogen bonds are formed by the substituted
2020-10-26
Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th
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In the present study we examined
2020-10-26
In the present study we examined whether the gene for estrogen receptor alpha, Esr1, plays a role in the expression of maternal memory in female rats. The approach utilized a newly developed rat Esr1 knockout (KO) rat model (Rumi et al., 2014) to evaluate whether deletion of the Esr1 CTX0294885 affe
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DDR although normally expressed in cells with mesenchymal fe
2020-10-26
DDR2, although normally expressed in UCB 35625 with mesenchymal features, has also been reported to enhance EMT. In A549 lung cancer cells, TGFβ1 increases the expression of type I collagen and DDR2. Knocking-down COL1A1 or DDR2 with siRNA is sufficient to inhibit EMT and cell migration induced by
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Kinetic isotope effects KIEs inform on
2020-10-26
Kinetic isotope effects (KIEs) inform on bond vibrational changes between the ground state (GS) and TS of a chemical reaction and remain one of the most powerful experimental techniques for interrogating TS structure. KIEs on enzyme reactions measured by the internal glycogen phosphorylase of label
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Egr together with catecholamine biosynthetic enzymes such
2020-10-26
Egr1, together with catecholamine biosynthetic enzymes, such as tyrosine hydroxylase (TH), dopamine β-hydroxylase (DBH), and phenylethanolamine N-methyltransferase (PNMT), is induced in adrenal medulla by different types of stress (Liu et al., 2005, Morita et al., 1996, Nankova et al., 1993, Papanik
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In this paper we describe a facile and
2020-10-26
In this paper, we describe a facile and universal method for in situ crosslinking of DNA micelles, using spherically directed reduction of metal ions. As shown in Scheme 1A, a single-stranded DNA (ssDNA) consisting of a ligand domain, a template domain, and a lipid domain was designed as a monomer t
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