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Our study provides proof of principle for
2019-10-09
Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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Modulating protein stability specifically inhibiting ubiquit
2019-10-09
Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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Despite the important agronomic traits regulated by
2019-10-09
Despite the important agronomic traits regulated by SUMO, most research studies on SUMOylation have been mainly limited to model plants, such as Arabidopsis and rice (Wang et al., 2011), due to the lack of molecular tools specific to other economically relevant plants. On the other hand, plants harb
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To study the role of DNA PK in
2019-10-09
To study the role of DNA–PK in the response to replication arrest, we used the DNA replication inhibitor aphidicolin (APH). APH, a mycotoxin isolated from Cephalosporium aphidicola, inhibits DNA replication by interacting with the replicating DNA polymerase α (pol α). APH specifically inhibits the a
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The aniline R group was extensively
2019-10-09
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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Finally we assessed the utility of
2019-10-08
Finally, we assessed the utility of monitoring cfDNA in terms of predicting disease progression earlier than radiological progression. These patients may have a chance to receive subsequent chemotherapy before worsening symptoms. Although the number of the patients who experienced progression was re
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The strand domain swap in the UbV
2019-10-08
The β strand domain swap in the UbV.XR dimer appears to be a unique arrangement for a Ub-based dimer. In solution, free Ub has a KD of ∼5 mM for the monomer-dimer equilibrium, and the two subunits in the dimer adopt a range of relative orientations involving residues from Ub’s β sheet (Liu et al., 2
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p as a cyclin dependent
2019-10-08
p21, as a cyclin-dependent kinase inhibitor, exert significant negative regulator of proliferation, and it could be transcriptional upregulated by p53 in order to impel transient Bardoxolone methyl arrest (Romanov et al., 2010). Using western blotting, we found that the protein expression of p21 up
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Several authors have been pursuing
2019-10-08
Several authors have been pursuing the aim of finding good performing organic solvent compatible adsorbers useful in the context of API purification [[10], [11], [12], [13], 22, 23]. For sulfonate GTIs, scavenging nucleophilic resins [22, 23] or molecular imprinted polymers (MIPs) [10] have been exp
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br Conformational properties of DGK br Interaction of DGK wi
2019-10-08
Conformational properties of DGKϵ Interaction of DGKϵ with its lipid substrate A major component of the interaction between DGKϵ and lipid bilayers is the insertion of the hydrophobic segment comprising residues 20–42 into the membrane, as discussed above. However, this is not the only interac
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GANT 58 pathway Targeting both PARP and DHODH for anti cance
2019-10-08
Targeting both PARP-1 and DHODH for anti-cancer therapy would certainly be beneficial as these enzymes share a common role in the DNA replication and repair mechanisms which are involved in the hyper-proliferation of cancer cells. Since benzimidazole-containing compounds have been reported to show g
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Collagen compaction and alignment are generated by cell
2019-10-08
Collagen compaction and alignment are generated by cell-mediated contractile forces (Stopak and Harris, 1982). The transmission of actomyosin forces to collagen has been mainly attributed to integrins and the activation of the Rho-ROCK pathway (Clark et al., 2007, Kural and Billiar, 2013, Provenzano
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EPI-001 However recent studies revealed that the
2019-10-08
However, recent studies revealed that the function of Crm1 might not only limit to nucleocytoplasmic transport, but also be involved in regulation of centrosome duplication. As the major microtubule organizing centers in animal cells, centrosomes play a significant role in cell cycle, spindle format
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The final test that was performed was to determine whether
2019-10-08
The final test that was performed was to determine whether the trigger points of the current limiters are stable across a wide temperature range. This test was performed within a thermal-vacuum chamber on each current limiter individually. All the current limiter trip currents were set to approximat
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From the results of previous experiments with
2019-10-08
From the results of previous experiments with the purvalanol B affinity matrix, it is not clear whether the selective capture of parasite CK1 enzymes is a reflection of their high abundance or rather their affinity for the ligand compared with other kinases present in the lysates. Based on compariso
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