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Increased levels of PCNA monoubiquitination by
2021-07-29

Increased levels of PCNA monoubiquitination by UbL73P expression in a damage-independent manner mimics the phenotype observed for USP1 knockdown (Huang et al., 2006, Jones et al., 2012). USP1 is the only DUB to date shown to remove ubiquitin from PCNA in vivo. This finding reveals the highly dynamic
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Dipeptidyl peptidase inhibitors DPP is
2021-07-29

Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit Escitalopram Oxalate secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good ef
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We have reported previously that aminoacrylate
2021-07-29

We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD
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In our current work we have
2021-07-29

In our current work, we have undertaken liquid phase combinatorial synthesis methods for the synthesis of 1,2,5-trisubstituted benzimidazole derivatives as hDHODH inhibitors. Synthesised Y-27632 were also screened by molecular docking studies over the reported hDHODH structure. The synthesised molec
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As for antiviral activity eight out of
2021-07-29

As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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Cystatins are potent inhibitors of cysteine proteases from t
2021-07-29

Cystatins are potent inhibitors of cysteine proteases from the C1A family. These inhibitors primarily reduce the activities of cathepsin L-like proteases, although high concentration of barley cystatin hampers the degradation of storage proteins caused by cathepsin F-like protein (HvPap-1) (Cambra e
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Proteins that associate to PCNA are characterized by having
2021-07-29

Proteins that associate to PCNA are characterized by having conserved motifs as the PCNA-interacting protein (PIP) motif [29,30], its variant PIP-like motif [31,32] or the APIM motif (Alk B homologue 2 PCNA interacting motif [33,34]); for instance, p21 contains a PIP motif [30], and DNA polymerases
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br Thermodynamic modeling br Selection
2021-07-29

Thermodynamic modeling Selection of data The solutes were selected based on the set of data needed to evaluate the CPA-EoS for prediction of their solubility in CO2 + cosolvent, as shown in Fig. 1. Critical temperatures, melting temperatures and enthalpies of fusion of the solutes are required
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A neurotoxic syndrome called Intermediate
2021-07-28

A neurotoxic syndrome called “Intermediate syndrome” has been described after acute cholinergic crisis, which has been interpreted as the result of pre- and postsynaptic disruptions of neuromuscular transmission (Senanayake and Karalliedde, 1987). Other toxic effects with unknown molecular targets h
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Hepatocyte proliferation is accompanied by changing gene exp
2021-07-28

Hepatocyte proliferation is accompanied by changing gene expression [1,2]. as two of the three estrogen receptors are transcription factors: Estrogen Receptor alpha (ERα) and ERβ [[3], [4], [5]]. The most potent ligand estradiol, binds to ERα/ERβ and exerts changing cognate gene transcription [5]. O
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Introduction Penetrator with Enhanced Lateral Effect PELE is
2021-07-28

Introduction Penetrator with Enhanced Lateral Effect (PELE) is a kind of ammunition which consists of a low-density material as the filling and a high-density material as the jacket [1,2]. When PELE impact target, the jacket is radially accelerated, expanded and fractured because of distinctive lat
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DDR although normally expressed in
2021-07-28

DDR2, although normally expressed in molar concentration calculator 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 m
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The differences between ground and transition state properti
2021-07-28

The differences between ground and transition state properties are exemplified by a comparison of our human–yeast results with those of a structural study of possible differences in ubiquitin-Uba-1 binding in yeast (known structure) with human (simulated in [12]). Their discussion focuses on Ubiquit
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br Experimental All starting materials and reagents were
2021-07-28

Experimental All starting materials and reagents were purchased from Sigma-Aldrich, Merck and Loba Chemie. Thin layer chromatography (TLC) was performed on silica gel G60 F254 (Merck) plates and eluted with the mobile phase n-hexane: ethyl acetate (70:30%v/v). Melting points were recorded on auto
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A-803467 br General Characteristics of the
2021-07-28

General Characteristics of the Type II Dehydrogenases Alternative NAD(P)H dehydrogenases conduct the reaction of the rotenone-insensitive oxidation of cytosolic and mitochondrial matrix NADH and/or NADPH (Fig. 1) (Melo et al., 2004, Rasmusson et al., 2004, Rasmusson et al., 2008). They catalyze t
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