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The interface between the E
2020-03-26
The interface between the E3 ligase and the E2 enzyme can vary, and ZNF451 and SP-RING ligases stabilize this interaction via noncovalent binding to a scaffold SUMO (SUMOB) on the backside of the E2 (Cappadocia et al., 2015; Eisenhardt et al., 2015; Streich & Lima, 2016). By contrast, RanBP2 does no
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Substituents at the C position
2020-03-25
Substituents at the C11 position — An oxygen-containing substituent at the C11 position also affects the catalytic activity of Δ1-KSTDs. The Δ1-KSTDs from the Gram-positive bacteria R. equi [29], N. simplex ATCC 6946 and IFO 12069 [48,49,52], and R. rhodochrous IFO 3338 [27] were able to 1(2)-dehydr
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To determine direct DDR binding partners and to further
2020-03-25
To determine direct DDR1-binding partners and to further connect to Akt and mTOR signaling, we performed mass spectrometry on DDR1 immunoprecipitates and found various candidates of the Akt and mTOR pathway such as LARP1 (La-related protein 1) and RPS6 (40S ribosomal protein S6/ S6). Most intriguing
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br Cytokines and NK cells br Combined effects
2020-03-25
Cytokines and NK cells Combined effects of cytokines and other stimuli on NK cell function Cytokine-stimulated NK FAK Inhibitor 14 have enhanced capacity to kill tumor cells. However, usually, individual cytokines do not seem to be sufficient for full activation, proliferation, survival and e
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br Fragment based drug discovery
2020-03-25
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical JNJ-7706621 space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It
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The pyrrolo benzodiazepines PBDs are a family
2020-03-25
The pyrrolo[2,1-][1,4]benzodiazepines (PBDs) are a family of antitumour antibiotics that includes the natural products anthramycin and DC-81. They exert their cytotoxicity by covalently bonding to the exocyclic C2–NH group of guanine residues in the minor groove of DNA through their N10–C11 imine fu
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Cell swelling stimulates the release of certain amino acids
2020-03-25
Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino vorapaxar taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that volume-activated t
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Bioinformatics analysis for genes encoding proteins ESR
2020-03-25
Bioinformatics analysis for genes encoding proteins (ESR1, IL6, TERT, DNMT3B) showed that NF-kB is one of the transcription factors that might be regulating their expression, especially for IL6, TERT and DNMT3B genes. Previous studies have demonstrated that PA induces NF-kB activation, thus increasi
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br Roles of ERR in Physiology
2020-03-25
Roles of ERRγ in Physiology and Disease Concluding Remarks and Future Perspectives Over the last decade, the generation of tissue-specific ERRγ transgenic or knockout mice and the use of synthetic ligands have rapidly advanced our understanding of the roles of ERRγ in cellular functions, altho
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Considering these reports and with the aim of further
2020-03-25
Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on b
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Although CK phosphorylated Msn as well as Msn Fig A
2020-03-24
Although CK2 phosphorylated Msn4 as well as Msn2 (Fig. 1A), the two CK2-dependent phosphorylation sites in Msn2 are not conserved in Msn4. Thus, Msn2 and Msn4 might be differently regulated by CK2-dependent phosphorylation. Msn2 and Msn4, which have 41% identity and similarity in size and amino arn
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ER redox imbalance leads to the accumulation of
2020-03-24
ER redox imbalance leads to the accumulation of misfolded proteins, which might trigger the unfolded protein response (UPR) [17]. In the initiation of UPR, GRP78 preferentially binds to unfolded proteins, shifting the binding equilibrium away from IRE-1, PERK, and ATF-6, the initiators of UPR [18].
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The all NTP pyrophosphatase and NUDIX families maintain the
2020-03-24
The all-α NTP pyrophosphatase and NUDIX families maintain the deoxynucleotide triphosphate (dNTP) pool balance, limit the incorporation of harmful nucleotides, and represent a promising therapeutic approach to develop anticancer and immunosuppressive agents., , , , Among these housekeeping enzymes
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The different diagnostic outcomes of the two assays are
2020-03-24
The different diagnostic outcomes of the two assays are also dependent on the used stimuli. The QuantiFERON-CMV assay targets CD8 + T biotin-LC-LC-tyramide by using peptides whereas the T-Track-CMV targets CD4+ and CD8 + T cells by stimulation with two viral proteins [18]. In our study, a specifici
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br Substoichiometric substrate modification E ligases cataly
2020-03-23
Substoichiometric substrate modification E3 ligases catalyze the rapid transfer of the SUMOD from the E2 enzyme to the substrate. By definition, enzymes are recycled in the reaction, allowing multiple rounds of substrate modification by a single enzyme. Thus, enzymes function at substoichiometric
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