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br Results br Discussion Our UbV library was originally desi
2020-11-18
Results Discussion Our UbV library was originally designed to develop inhibitors of deubiquitinases (Ernst et al., 2013). Recently, we showed that UbVs could exhibit multiple binding modes and mechanisms to modulate HECT E3 activity (Zhang et al., 2016)—one set occupied the HECT domain E2-bind
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These studies suggested that PV PVH might
2020-11-18
These studies suggested that PV/PVH might promote bone formation activities and/or inhibit bone resorption activities probably due to its anti-inflammation activity; however, the underlying mechanism remained unknown. Furthermore, it is unclear if PVH shows better activity than that of PV; this is i
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br Acknowledgment This work was supported by the Estonian
2020-11-18
Acknowledgment This work was supported by the Estonian Science Foundation (Grant ETF8862). Introduction In higher eukaryotes ionizing-radiation (IR) induced DNA double-strand breaks (DSB) are primarily repaired by the non-homologous end joining (NHEJ) pathway [1]. Ku, a heterodimeric protein
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br Synthesis and mechanism of fluorescent DNA
2020-11-18
Synthesis and mechanism of fluorescent DNA-CuNMs Application of fluorescent DNA-CuNMs Summary and conclusions In summary, we introduce recent research progress in the synthesis and various applications of DNA-CuNMs. DNA-CuNMs with novel catalytic, electrical and optical properties can be ob
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Even though Et modification of DNA delayed
2020-11-18
Even though Et743 modification of DNA delayed the progress of the translocating enzyme significantly, it did not trap RecBCD on DNA, nor did it alter the activity of the enzyme significantly. Under catalytic conditions, no loss of enzyme activity was observed (Table 2), nor were stable unwinding int
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Given the excellent in vitro pharmacology profiles of methyl
2020-11-17
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic good intentions functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT
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For the SAR optimization of the right hand
2020-11-17
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic 58 5 mg moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by condensatio
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br Contributors br Acknowledgements br Introduction Pemphigu
2020-11-17
Contributors Acknowledgements Introduction Pemphigus disorders are characterized by autoantibodies binding to desmosomes between epidermal cells, resulting in the loss of cell to cell adhesion and blister formation. In pemphigus foliaceus, autoantibodies predominantly bind to desmoglein 1,
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In a study on the
2020-11-17
In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve
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Nevertheless of the different types of scoring systems so fa
2020-11-17
Nevertheless, of the different types of scoring systems so far proposed, each of these [14], [29], [30] considered some aspects that could describe the fibrotic evolution, though none provided a quantitative assessment. Calvaruso et al. [8] showed that CPA had a better histological correlation with
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It is generally thought that the nature of a
2020-11-17
It is generally thought that the nature of a memorial and the meaning attributed to it HKI-272 by a tourist determines, at least in part, the behaviour that is socially appropriate (Mayo, 1988). Duncan (1995) argues however, that certain places are structured in such a way that they facilitate ritu
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Meanwhile high levels of extraversion have been associated w
2020-11-17
Meanwhile, high levels of extraversion have been associated with weaker conditioning and faster Bcl Family Set I learning (Eysenck, 1970). Similar to neuroticism/anxiety, the role of extraversion for fear conditioning and extinction has found only limited empirical support (Rauch et al., 2005) with
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Which other approaches can complement signaling optogenetics
2020-11-17
Which other approaches can complement signaling optogenetics to paint a more complete picture of developmental Erk signaling? For now, the authors have dynamically manipulated Erk signaling but measured the Erk output at steady-state using classic immunofluorescence techniques (Johnson and Toettcher
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Further modifications on the position of
2020-11-17
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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In this report we describe studies of
2020-11-16
In this report we describe studies of the effects of peroxisome proliferator-activated receptor γ (PPARγ) and acyl-CoA synthetase (ACSL1) on palmitate-induced ER stress in the human cardiomyocyte-like cell line AC16 [22], which was derived from adult ventricular heart tissue. PPARγ is a nuclear rece
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