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Several main strategies for targeting E s described
2021-04-25

Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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Several functions of FAT have been suggested It has been
2021-04-25

Several functions of FAT10 have been suggested. It has been shown that FAT10 binds noncovalently to the mitotic spindle checkpoint protein MAD2 and that this binding might cause chromosome instability in the cancer pyk2 inhibitor overexpressing FAT10 (Liu et al., 1999, Ren et al., 2006). In other s
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Haj Yahya et al applied native chemical ligation for
2021-04-25

Haj-Yahya et al. [52] applied native chemical ligation for the construction of diubiquitin probes. They attached a cysteine residue to the lysine side chain of the proximal ubiquitin and ligated the distal module using the C-terminal thioester of ubiquitin. Elimination of the sulfur umbelliferone r
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br Concluding remark br Acknowledgements br Detection
2021-04-25

Concluding remark Acknowledgements Detection and repair of the numerous, and potentially lethal, DNA lesions arising in human Gemcitabine HCl daily is largely mediated by an efficient system collectively termed the DNA-damage response (DDR). Paradoxically, DNA-repair processes within cancer
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While the mechanism of DHODH inhibition induced differentiat
2021-04-25

While the mechanism of DHODH inhibition-induced differentiation is not fully understood, this phenomenon may be caused by pyrimidine depletion. Pyrazofurin, an inhibitor of OMP decarboxylase, was able to induce differentiation and suggests pyrimidine depletion as a potential mechanism (Sykes et al.,
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Alternatively procedural factors may have contributed to the
2021-04-25

Alternatively, procedural factors may have contributed to the conflicting results. For instance, in order to have a more circumscribed area of drug diffusion, a volume of 0.05μl was injected in experiment 1b, which is four times lower than the one used in the mentioned plus-maze investigation. Besid
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Zinc protoporphyrin IX australia This work is inspired by th
2021-04-25

This work is inspired by the systematic work of Coutinho and co-workers, who obtained several very useful experimental data, which will be also used in our work, and applied the CPA equation of state for the modeling of systems relevant to the production of biodiesel [8], [9], [10], [11], [12], [13]
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In some pancreatic and non pancreatic tissues
2021-04-25

In some pancreatic and non-pancreatic tissues, the chloride and calcium channels are heavily regulated by phosphorylation by protein kinases, such as PKC, cyclic AMP-dependent protein kinase (PKA), PKCaMKII, PI3K and protein tyrosine kinases [7,36,37]. Since the interaction of triterpenes with recep
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Interestingly increased level of both
2021-04-25

Interestingly, increased level of both circulating ET-1 and urinary excretion of ET-1 have been observed in patients treated with nephrotoxic immunosuppressive agents as cyclosporine A and tacrolimus (Slowinski et al., 2002). Other nephrotoxic agents, such as cisplatin, also increase urinary excreti
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Not all of the biological activities exhibited by progestoge
2021-04-25

Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the parp apoptosis pathway is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of the cell
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Finally we demonstrated for the
2021-04-25

Finally, we demonstrated for the first time that the physiological combinations of estradiol and progesterone levels of premenopausal and postmenopausal women efficiently stimulated the growth of T47D spheroids while clinically relevant concentrations of TPA and UPA suppressed the growth of T47D sph
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In addition to the ESIs identified that
2021-04-25

In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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For most enolases fluoride acts as
2021-04-25

For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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In the phase I AURA trial patients with EGFR
2021-04-25

In the phase I AURA trial, patients with EGFR activating mutations and centrally confirmed tumor and/or plasma genotyping (BEAMing) T790M result were enrolled. Among 216 patients with both plasma and tissue genotyping results, the concordance rate was 82% for YM 155 19 deletions, 86% for L858R and
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br Genes involved in oxysterol metabolism The
2021-04-25

Genes involved in oxysterol metabolism The main enzymes that participate in the metabolism of oxysterols generally belong into one of two groups: transferases or oxidoreductases [22]. The following chapter describes those genes of oxysterol metabolism whose polymorphisms have been associated with
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