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Besides EGFR other tyrosine kinase
2020-11-13

Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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br APC C Uses a
2020-11-13

APC/C Uses a Dynamic Cullin–RING Mechanism to Elongate Polyubiquitin Chains Human APC/C generates Lys11-linked poly-Ub chains through an entirely different mechanism, via the distinctive E2 enzyme, UBE2S 30, 31, 32. Although APC2 and APC11 are necessary and sufficient to activate UBE2S, the mecha
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The interface between the E
2020-11-13

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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br Conclusion As far as we know this work constituted
2020-11-13

Conclusion As far as we know, this work constituted the first use of silver nitrate staining and sequential FISH in V. vinifera. This technique allowed the unequivocal identification of Ag-NORs and corresponding rDNA loci. Besides, silver nitrate staining and sequential FISH may bring new insight
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While the mechanism of DHODH inhibition
2020-11-13

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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Studies of Jelski and Szmitkowski show
2020-11-13

Studies of Jelski and Szmitkowski show that differences of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) activity between ghrelin receptor of many cancers and healthy tissue may be one of the factors intensifying carcinogenesis [7]. Moreover, changes of ADH and ALDH activity in canc
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br Application of the screening system
2020-11-13

Application of the screening system for ITP-binding proteins Inosine is a nucleoside with hypoxanthine as a base. Inosine nucleotides are relatively abundant in human reductase enzyme because inosine monophosphate (IMP) is a general precursor molecule for the de novo synthesis of AMP and GMP or
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The all NTP pyrophosphatase and NUDIX families
2020-11-13

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 i
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br P Y receptor structure br
2020-11-13

P2Y receptor structure Pharmacology Several subtype selective compounds have been developed in recent years (Jacobson and Müller, 2016; Rafehi and Müller, 2018). These compounds are helpful tools for analyzing the roles of P2Y receptor subtypes in physiology and pathophysiology. The present ar
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br Use of CDK inhibitors
2020-11-13

Use of CDK inhibitors in CLL today There has been explosive development of novel therapeutics for CLL in the last decade and a massive transformation of practice is underway [75]. Most of this development and excitement revolves around B-cell receptor (BCR) signaling inhibitors: the Bruton tyrosi
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br Materials and methods br Results br
2020-11-13

Materials and methods Results Discussion We confirmed the published cDNA and protein sequence of feline CSF-1R and stably cloned the cat receptor into the Ba/F3 cell line. Activation of feline CSF-1R by recombinant human CSF-1 was previously tested by Woolford et al. [14]. Expression of onc
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Currently multiple clinical trials of CSF
2020-11-13

Currently, multiple clinical trials of CSF-1/CSF-1R-targeting agents in combination with standard treatment modalities and immunotherapies are underway (Table 1). In particular, results for combinations with checkpoint blockade inhibitors and other immunotherapeutic approaches are eagerly awaited.
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br Chemistry Scheme shows the
2020-11-13

Chemistry Scheme 1 shows the synthesis of compounds 15-1–15-33 from commercially available 2-(4-aminophenyl)acetonitrile (8a). Protection of the starting material 8a with di-t-butyl dicarbonate afforded 9. The reaction of 9 with methyl 1-chloroisoquinoline-4-carboxylate in the presence of sodium
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We further examined our hypothesis that the activation of
2020-11-13

We further examined our hypothesis that the activation of CRF and CCK systems is responsible for the enhanced anxiety-like behavior induced by immobilization stress using two antagonists to block the expression of CRF1 and CCK2 receptors. It was found that CCK2 receptor antagonist CR2945 or CRF1 ant
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RQ-00203078 In the preclinical evaluation of CRF receptor
2020-11-12

In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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