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We have reported previously that aminoacrylate derivatives
2021-02-09
We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD
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In this study using REMD with the
2021-02-09
In this study, using REMD with the crystal environment, we investigate the effect of cryo-cooling on the crystal structure of Escherichia coli DHFR. DHFR is an important model enzyme (for review, see, e.g., (30)), and has been studied for decades (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43).
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Transduction of cellular signals by G protein coupled recept
2021-02-09
Transduction of cellular signals by G protein-coupled receptors (GPCRs) is stringently regulated to prevent the deleterious effects of unrestrained GPCR signaling. The rapid termination of signaling mediated by agonist-occupied GPCRs is referred to as homologous desensitization and involves the foll
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Compounds and were outliers for this
2021-02-09
Compounds and were outliers for this equation being the two most reactive compounds. The presence of outliers implies that other factors or specific mechanisms are involved in their chemical hydrolysis. Generally urea derivatives prove to be highly stable in aqueous solutions in vitro. Additional
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Chrysin A further quandary concerning rediscoveries arises i
2021-02-09
A further quandary concerning rediscoveries arises in habitats modified and frequented by humans, where rediscovered species may occur through accidental or deliberate introductions (Metcalf et al., 2007) rather than having persisted despite adverse conditions. Confusion regarding origin could evoke
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br Particle swarm optimization for NLBP
2021-02-09
Particle swarm optimization for NLBP Computational tests Conclusions Acknowledgements This work was supported by the State Key Development Program for Basic Research of China (No. 2009CB421104) and the National Natural Science Foundation of China (Nos. 50809004 & 41071323). Main Text
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One possible pitfall of using
2021-02-09
One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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simvastin In our former work our interest was in
2021-02-09
In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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As CP is a crucial player in
2021-02-09
As CP110 is a crucial player in centriole duplication, it is intriguing to ask whether centriole duplication would also be affected in the absence of the CP110-stabilizing effects of USP33. Li et al.[4] found that USP33 depletion did not inhibit normal centriole duplication through loss of centriole
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br Conclusion As far as we
2021-02-09
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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In agreement with the study on
2021-02-08
In agreement with the study on porcine microsomes (Ekstrand et al., 2015), our results indicated a somewhat higher degree of inhibition of CYP2E1 activity in the male pools compared to females. Nevertheless, the degree of this Tempol inhibition did not reach 50%, indicating that quercetin is unlike
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CYP A is involved in the
2021-02-08
CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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77 8 While a growing body of knowledge demonstrates the impo
2021-02-08
While a growing body of knowledge demonstrates the importance of COX-1 and COX-2 accompanied with neuroinflammation in altitude related conditions. In fact, PGE2 has been widely thought to promote the neuronal inflammation and degeneration in many neurological maladies (Griffin et al., 2013, Jiang a
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br Discussion Personality develops throughout a human s
2021-02-08
Discussion Personality develops throughout a human's life and is related to his or her innate temperament. While personality features are shaped by various experiences of daily life and moderate a wide range of specific behaviours related to particular situational contexts, temperament reveals it
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Although the presence of at least one triple helix domain
2021-02-08
Although the presence of at least one triple helix domain is typically the collagen signature, collagens are modular proteins composed of a succession of collagenous (COL) and non-collagenous domains (NC) that are both involved in collagen functions and in receptor binding. COL domains are linked by
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