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001 2 In summary we have discovered
2022-03-12
In summary, we have discovered the first examples of movement of Asp189 upon binding to fXa inhibitors. A series of novel and potent fXa inhibitors with a phenyltriazolinone P moiety were identified. Although the general binding mode compared to our previously-reported fXa inhibitors was maintained,
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The present study was designed to clarify the distribution
2022-03-11
The present study was designed to clarify the distribution and the function of the endothelin receptors in the guinea-pig urinary bladder. We found that endothelin-1 produced a clear tonic contraction via both L-Carnitine inner salt subtypes, the endothelin ETA and ETB receptor, and that sarafotoxi
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br Materials and methods br
2022-03-11
Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of 49 9 concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites, and that the fraction of t
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Although no data exist on Ptc gene expression
2022-03-11
Although no data exist on Ptc52 gene droperidol in other plant species, the expression pattern presented in this study shows perceptibly low levels of transcript accumulation in tomato seeds and roots, low levels in the stem, flower and green fruit, and high levels in the leaves. This coincides wit
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Acknowledgements We appreciated the contributions of Ana Car
2022-03-11
Acknowledgements We appreciated the contributions of Ana Carolina Galha, Selma XSL Pinheiro and Islene Azevedo for technical assistances. In addition, we wish to thank Adilson José de Almeida (in memoriam), Moyra M Portilho, Vanessa A Marques and Letícia P Scalioni, for data analysis during the set
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br Patients and methods br Results br
2022-03-11
Patients and methods Results Discussion The positivity of serum anti-HBc is the most commonly used marker to confirm the history of HBV infection. Quantification of serum anti-HBc has been explored as a marker of HBV-induced hepatitis and the adaptive immune response against HBV infection a
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Acknowledgments The authors thank Partners
2022-03-11
Acknowledgments The authors thank Partners Healthcare for financial support. This work was also supported in part by NIH Grant R01CA122608 to J.M.G.H. Introduction The phosphorylation of histone H3 is recognized as a hallmark of mitosis. Histone H3 phosphorylation at Thr3 (H3T3ph) acts as a mit
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Although resembling a differential symbiotic relationship
2022-03-11
Although resembling a differential symbiotic relationship, interplay between prostate tumour CAFs promotes PKM2/HIF-1-driven transcriptional regulation in prostate cancer cells that exploit lactate produced by CAFs and undergo epithelial-to-mesenchymal transition (EMT) [21]. Although recent observat
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The physiological role of lactate induced antilipolytic effe
2022-03-11
The physiological role of lactate-induced antilipolytic effects is less clear. It has been speculated that GPR81 mediates the inhibition of lipolysis during intensive exercise, a condition which results in high systemic lactate plasma concentrations 9, 10. Owing to oxygen shortage resulting from in
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In the present study we
2022-03-11
In the present study, we conducted a search for other possible endogenous ligands for GPR35. We focused on lysophospholipids because of the homology (30%) between GPR35 and GPR55 whose endogenous ligand is lysophosphatidylinositol (LPI) [9], especially 2-arachidonoyl LPI [10]. Notably, the GPR35 gen
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The facts mentioned above indicate that
2022-03-11
The facts mentioned above indicate that glycine function in brain is tightly regulated or pathologically altered mostly by glycine transporters. Modification of cytosolic regions of transporters, which interconnect them with intracellular regulatory pathways, could be one of the ways to provoke brai
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moclobemide In our study we evaluated adenovirus type Ad
2022-03-11
In our study we evaluated adenovirus type 5 (Ad5) as a vehicle for delivering Cre recombinase in conditional transgenic mouse based on the Cre-loxP system, in order to achieve GlyT1 gene modulation in a specific thalamic region in the adult animal. GlyT1 is a sodium- and chloride-coupled glycine tra
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Several groups studied CTD mouse models which
2022-03-11
Several groups studied CTD mouse models, which largely mimicked the symptoms (i.e. impaired cognition and autistic-like behaviour) of the human disease (Kurosawa et al., 2012; Baroncelli et al., 2016; Stockebrand, 2018). The CRT-1 knockout mice showed a drastic deterioration in the GABAergic system,
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In experiments using D to displace binding of specific
2022-03-11
In experiments using D22 to displace binding of specific high-affinity radioligands for DAT, NET, and SERT in mouse kobe2602 tissue, we observed a ranking with D22 displacement efficiency in the order of DAT > SERT > NET (IC50 values being ~ 11 (DAT), 26 (SERT), and 101 (NET) µM; Fig. 1, Fig. 2, Fi
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Accordingly a bioassay guided approach was been used
2022-03-11
Accordingly, a bioassay-guided approach was been used to study the bioactive compounds in VAS contribute to the α-glucosidase inhibitory and antioxidant activity. The 95% ethanol extraction of VAS was successively partitioned with petroleum ether, ethyl acetate and n-butanol. Ethyl acetate fraction
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