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Kinetic isotope effects KIEs inform on
2021-04-28

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 Canrenone mg of labeled substra
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Intriguingly one E residue may serve as a
2021-04-28

Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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br Materials and methods br Results br Discussion UPP compon
2021-04-28

Materials and methods Results Discussion UPP components including the proteasome, E1s, E2s, E3s and DUBs may become one the most important AGI-5198 of therapeutic targets for the pharmaceutical industry in the near future and supersede those which are involved in the phosphorylation system
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In light of the overall loss of
2021-04-28

In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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Previous studies have indicated that hSSB may
2021-04-28

Previous studies have indicated that hSSB1 may be phosphorylated at threonine residue 117 (T117) [13] and acetylated at lysine residue 94 (K94) [15], both of which promote hSSB1 function in response to ionising radiation exposure. Mass spectrometry screens of proteins immunoprecipitated with phospho
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Instead of receptor interaction or GT activity
2021-04-27

Instead of receptor interaction or GT activity, we focused on the CPD and autoprocessing. The CPDs from the 2 toxins are highly homologous: each cysteine protease targets an intramolecular substrate and mediates InsP6-induced autoprocessing to release the GTD into host cytosol.40, 41 However, TcdB i
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Accumulated evidence indicates that apelin plays
2021-04-27

Accumulated evidence indicates that apelin plays a protective role in ischemic stroke, contributing to post-stroke recovery (Yang et al., 2014; Chen et al., 2015; Xin et al., 2015; Yan et al., 2015). Apelin gene (APLN) encodes prepro-apelin with 77 amino acids, while the C-terminal 23 SB743921 are
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As the primary model we selected LDL receptor knockout mice
2021-04-27

As the primary model we selected LDL-receptor knockout mice because these resemble the human plasma lipoprotein profile more closely. Currently, genetic models with reduced milk cholesterol content, which mimic cholesterol-free formula feeding, are unavailable. Thus, instead of modifying milk choles
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Recently pharmacological studies have revealed that natural
2021-04-27

Recently, pharmacological studies have revealed that natural compounds achieve increasing attention due to its high therapeutic effectiveness and low adverse effect, compared with the chemically synthesized compounds. Emodin is a kind of natural anthraquinone derivative enriched in traditional Chin
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The nucleus accumbens is a critical locus
2021-04-27

The nucleus accumbens is a critical locus for ER/mGluR signaling in the context of addiction ER/mGluR signaling is regulated by caveolin proteins and palmitoylation Because of the vast implications of ER/mGluR association, it is important to understand what regulates their interaction. Such regu
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Previous studies demonstrated that cPLA translocates to the
2021-04-27

Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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br Roles of DDR in epithelial cell
2021-04-27

Roles of DDR1 in epithelial cell differentiation Roles of DDR1 in cell migration, and invasion Dichotomous functions of DDR1 in disease progression Conclusions and perspectives The switch in SBI-0206965 from DDR1 to DDR2 during EMT is another important issue. The DDRs may exert distinct
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The potent estrogen EE induced a
2021-04-27

The potent osmi EE2 induced a decrease in CYP2C11 activity (reduction in 2α-OH and 16α-OH testosterone) and protein at the 200 ppb dose and in this respect was similar to nonylphenol and genistein. This result agrees qualitatively with the results of Hallstrom et al. (1996) who exposed male rats to
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Increasing evidence supports that the B cell lymphoid malign
2021-04-27

Increasing evidence supports that the B-cell lymphoid malignancies develop from various stages of B-cells, hijacking the mechanisms that drive B-cell differentiation and activation [27]. For instance, mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL) originate from the pre-germinal c
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br Results br Discussion Taking
2021-04-27

Results Discussion Taking advantage of the highly specific protein–protein interactions among cognate ibotenic acid that mediate SUMO conjugation to substrates, we have developed a novel strategy for achieving inhibition of SUMO conjugation in vivo based on disruption of SUMO E1–E2 interactio
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