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br Summary and perspectives In recent decades enormous advan
2020-03-16
Summary and perspectives In recent decades, enormous advances have been achieved in the development of enzyme-activatable imaging probes, enabling the accurate detection of enzyme activity in vivo to better understand the biological function of enzymes in disease processes. Activatable probes are
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Enzyme mimics belong to a type
2020-03-16
Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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br Transparency document br Acknowledgments This study
2020-03-16
Transparency document Acknowledgments This study was funded by ICMR, Govt. of India. Alisha Dhiman acknowledges UGC-DSKPDF, India for post-doctoral fellowship and Monisha Gopalani acknowledges CSIR, India for Senior Research Fellowship. AIRF, JNU is acknowledged for TEM, confocal microscopy an
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Modulating protein stability specifically inhibiting ubiquit
2020-03-13
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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Given the fact that most criticism on genetic association st
2020-03-13
Given the fact that most criticism on genetic association studies is the lack of replicability (Hirschhorn, Lohmueller, Byrne, & Hirschhorn, 2002), the aim of the present study is to investigate the influence of the DBH polymorphism rs1611115 (C-970T) on RD in two independent samples of healthy part
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C PHNO has been described as a full agonist at
2020-03-13
[11C]-(+)-PHNO has been described as a full agonist at both D2 and D3 receptors [54,55]. [11C]-(+)-PHNO was initially developed as a PET radiotracer for imaging the high affinity state of the D2 receptor (i.e., highD2) as a means of measuring synaptic dopamine changes in response to pharmacologic ch
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Consistent with the known tolerance of
2020-03-13
Consistent with the known tolerance of the Suzuki–Miyaura reaction to a wide range of aryl substituents, we subsequently found that the commercially available 3-hydroxyphenylboronic Combretastatin A4 sale pinacol ester () could be coupled to , to give directly and in comparable yield. Smooth conve
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In Hevea brasiliensis both the soluble PPase and
2020-03-13
In Hevea brasiliensis, both the soluble PPase and the membrane-bound V-PPase are present in the latex; the soluble PPase is in the C-serum (cytosol) of the latex [6] and the V-PPase is on the tonoplast of the lutoid, a special vacuole in the laticifers of rubber trees [7]. The V-PPase on the lutoid
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Given the importance of cysteine cathepsin inhibitors as put
2020-03-13
Given the importance of cysteine cathepsin inhibitors as putative therapeutic molecules and microbial virulence factors, we chose to investigate whether Yersinia enterocolitica may be a potent producer of such inhibitors. Y. enterocolitica is the most heterogeneous species within the genus Yersinia.
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Within their range of applicability
2020-03-13
Within their range of applicability, both approaches matched the phase boundaries and yields generally to within the measurement error. The approaches matched the phase compositions generally to within 11 wt% or less with the average absolute deviations listed below: One advantage of the proposed a
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br Allosteric inhibitors In general candidate drugs that bin
2020-03-13
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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Although in vitro and in
2020-03-13
Although, in vitro and in vivo immunosuppressive effects of female steroids have been described in fish (Yamaguchi et al., 2001, Law et al., 2001), their mode of action was not evaluated in detail. Consequently, it is of considerable interest to investigate the intracellular pathways that regulate t
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Introduction Psoriasis is a chronic
2020-03-13
Introduction Psoriasis is a chronic, recurrent and inflammatory skin disease, and it is characterized by erythema, skin hyperplasia, scales, and hyperproliferation of keratinocyte [1]. It is reported that the psoriasis occurrences are about 3% worldwide [2], but the number varies depending on ethni
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Because of the lack of sequence current knowledge on the
2020-03-13
Because of the lack of sequence, current knowledge on the cellular regulation of CoA-IT is scarce. However, recent work has suggested an interesting new role for CoA-IT in regulating the extent of the AA mobilization response in primed macrophages. Bacterial lipopolysaccharide (LPS) is a poor trigge
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br Results br Discussion br Materials
2020-03-13
Results Discussion Materials and Methods Acknowledgment This work was funded by the Collaborative Research Centre (SFB) 807 of the German Research Foundation (DFG) and supported by the state of Hessen (Center for Biomolecular Magnetic Resonance) and the German Research Foundation (DO545/
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