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Almost of drugs in the market undergo deactivation
2020-02-21
Almost 75% of drugs in the market undergo deactivation though oxidation, reduction or hydrolysis by cytochrome P450 (CYP) enzymes, and then, either directly or by facilitated excretion from the body (Guengerich, 2008). The CYP3A subfamily is of particular interest because of its broad substrate spec
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Kim et al reported for bioactive compounds originating from
2020-02-21
Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b
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Ultrasound is an acoustic wave with a frequency kHz that
2020-02-20
Ultrasound is an acoustic wave with a frequency >20 kHz that needs a medium to propagate [20]. Accompanied by the spread of an ultrasonic wave, a series of alternating cycles of compression and rarefaction emerge in the liquid medium. During the rarefaction cycle, microbubbles are formed because of
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The isomeric phenyloxazole not only exhibited
2020-02-20
The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand describes it (as seen in compound pairs – and –) decreased AC
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The development of C S mutation
2020-02-20
The development of C797S mutation has been reported in vivo in a small cohort (15 subjects) of EGFR T790M positive patients progressing after Osimertinib: this tertiary mutation was found, using a droplet digital PCR (ddPCR) assay, in 40% of patients after AR to this agent, while 33% of the cases ex
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br Experimental Procedure br Acknowledgment This work was
2020-02-20
Experimental Procedure Acknowledgment This work was supported by Ministry of Education, Singapore (MoE Tier-2) grant (R-154-000-625-112) and R154-000-A72-114 (AcRF Tier 1 grant) respectively. We acknowledge the Advanced Photon Source Beamline 24-ID-C, Argonne National Laboratory, USA. D.N. is
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We propose two different pathways for the production
2020-02-20
We propose two different pathways for the production of this species: either that described by Dooley [24], where the phenol ring is first activated by binding of its oxygen to copper, or one where a copper-peroxo species would directly react with an active site tyrosine residue (Scheme 1B). This se
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Why then is leading strand DNA synthesis reduced relative
2020-02-20
Why then is leading-strand DNA synthesis reduced relative to lagging-strand synthesis in rad53-1 mutant alpha-Endorphin under replication stress? To gain insight into this question, we first determined whether the firing of late origins in rad53-1 mutant cells contributes to compromised leading-str
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Recently naphthoquinone derivatives have shown promising
2020-02-20
Recently, naphthoquinone derivatives have shown promising results as antiparasitic lead compounds [28]. Conjugated hybrid compounds could be an effective path to discovery of new drugs by associating two different pharmacophore groups with different mechanisms of action in a single molecule [29,30],
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Proteases as multifunctional enzymes play key
2020-02-20
Proteases, as multifunctional enzymes, play key roles in controlling a wide variety of cellular and extracellular processes in plants and animals, including protein degradation and processing, germination, complement activation, inflammation, responses to environmental stimuli, senescence and so on.
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AQP protein expression was determined by Western blot analys
2020-02-20
AQP4 protein expression was determined by Western blot analysis. Briefly, protein samples (50μg) from brains or astrocytes were separated by 12% SDS–polyacrylamide gel electrophoresis and transferred to nitrocellulose membranes. The membranes were reacted with a rabbit polyclonal antibody against AQ
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In recent years there has been a dramatic
2020-02-20
In recent years there has been a dramatic increase in identification and optimization of potent CRTh2 antagonists which may not only inhibit the recruitment and activation of Th2 cells but also accelerate apoptosis and clearance of these cells from inflamed tissue, thereby promoting the resolution o
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Mitophagy is a selective autophagic process which leads to
2020-02-20
Mitophagy is a selective autophagic process which leads to the degradation of damaged mitochondria in response to metabolic or environmental stress conditions. In this study, we found that LFS-01 treatment significantly enhances p62 in a time-dependent manner. We found that the upregulation of p62 i
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Alternatively procedural factors may have
2020-02-20
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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In the present study we investigated
2020-02-20
In the present study, we investigated the role played by CRF1 and CRF2 receptors located within the mouse PAG on the anxiogenic and antinociceptive effects produced by local infusion of CRF. To block CRF receptors, we used the selective CRF1 and CRF2 10Panx antagonists, respectively, NBI 27914 ((5-c
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