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br Conclusion br Competing interests
2020-04-17
Conclusion Competing interests Authors\' contributions Acknowledgements The work was supported by Aurigene Discovery Technologies (M) Sdn. Bhd., Industrial Doctoral Program sponsorship by Ministry of Higher Education, Malaysia and research grants by the University of Malaya, grant number
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Consistent with previous simulations on the DFG Asp
2020-04-17
Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation event
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Several in vivo human studies have produced conflicting
2020-04-17
Several in vivo human studies have produced conflicting results for evaluating the inhibition of OCs on the metabolism of CYP3A substrates. Balogh et al. [12] demonstrated an approximately 25% inhibition of CYP3A activities in vivo after the administration of an OC containing 30μg of ethinylestradio
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With the narrow SAR of
2020-04-17
With the narrow SAR of the tail favouring the ortho sulfone group, we examined the remaining position open to substitution at the pyrazole 3-position, in an attempt to at least moderate the excessive human PPB (). Lipophilic groups in this position maintained huge shifts in potency in the absence or
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The aim of the present study was to investigate
2020-04-17
The aim of the present study was to investigate the acute effects of THC on resting state JNJ-10198409 neurophysiology, and to examine the impact of COMT genotype on these effects. Thirty-nine healthy volunteers participated in a randomised, placebo-controlled, crossover pharmacological MRI study. A
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ClC is not only a chloride ion
2020-04-17
ClC-3 is not only a chloride ion channel but also a regulatory protein involved in the regulation of multiple signaling pathways. The PI3K/AKT/mTOR signaling pathway plays a crucial role in regulating cell growth, migration, invasion, and distant metastasis [13,14]. Although abnormal PI3K/AKT/mTOR a
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Before addressing point by point the aforementioned topics i
2020-04-17
Before addressing point-by-point the aforementioned topics in separate sub-sections it should be remarked that the strength of recommendations provided by guidelines is graded in three classes: I (evidence and/or general agreement that a given treatment or procedure is beneficial, useful,effective),
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br Role of ERK signaling in
2020-04-17
Role of ERK signaling in preventive and therapeutic potential of flavonoids in neurodegenerative diseases ERK is one of the main pharmacological targets of natural phenolic compounds and contributes to several therapeutic approaches including anti-atherogenic, anti-cancer, anti-colitis, anti-arth
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br Conclusion br Experimental NMR spectra
2020-04-17
Conclusion Experimental NMR spectra were recorded on a Jeol spectrometer at either 270 or 400 MHz for 1H spectra and either 68 or 100 MHz for 13C spectra. All chemical shifts are quoted in ppm relative to tetramethylsilane. In the assignment of signals the abbreviation DHN is used for 2,3-dihy
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tsa inhibitor The Penicillium strain used in this work was
2020-04-17
The Penicillium strain used in this work was isolated from Atlantic forest soil and previously screened as lipase producer (Tauk-Tornisielo et al., 2005). The immobilization was previously evaluated using hydrophobic supports, i.e. agarose based butyl-(But), phenyl-(Phe) and octyl-Sepharose (Oct), a
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Herein the interactions of etamicastat nepicastat
2020-04-16
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the AS8351 exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remains un
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Like compound substitution on compound contains amino and
2020-04-16
Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226. The
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It was demonstrated that the addition of
2020-04-16
It was demonstrated that the addition of 10-fold excess of α-synuclein without modifications (with respect to the molar concentration of tetrameric GAPDH) leads to partial inactivation of GAPDH after 1-h incubation by 20% (Fig. 4, curve 2) in Zanamivir to insignificant decrease of the specific acti
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Abrahamson and coworkers recently demonstrated a distinct
2020-04-16
Abrahamson and coworkers (2009) recently demonstrated a distinct role of the podocyte in preservation and production of mature GBM-components such as α3/4/5(IV)-chains. This group further verified that collagen receptors (integrins) are linked to the DAPI hydrochloride of podocytes. In accordance to
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Acknowledgements This work was supported in part by
2020-04-16
Acknowledgements This work was supported in part by a Scholarship Fund for Young Researchers by the Promotion and Mutual Aid Corporation for Private (2017 to S.K.), research grant from Japan Rett Syndrome Support Organization (2018 to S.K.), and MEXT-Supported Program for the Strategic Research Fou
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