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Although the presence of calcium in RHA P active
2021-08-27
Although the presence of calcium in RHA-P active site is confirmed by the homology modeling, some additional observations can be made following the metal depletion and reconstitution experiments performed on RHA-Phis. EDTA-treated RHA-Phis recovers its activity in the presence of divalent cations su
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Apoptosis type I programmed cell death is considered
2021-08-27
Apoptosis, type I programmed cell death, is considered to be involved in the pathogenesis of various liver diseases, such as autoimmune hepatitis [[5], [6], [7], [8], [9], [10]] and hepatocellular carcinoma [11,12]. Apoptosis is activated by a variety of extrinsic or intrinsic pathways factors. Prev
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The lack of robust immunocompetent animal models permissive
2021-08-26
The lack of robust immunocompetent animal models permissive for HCV makes it hard to assess if the quantity and quality of vaccine-induced immunity is sufficient to confer protection. Thus, it is difficult to predict to what extent antibody responses induced by current vaccination approaches, includ
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The synthesis of compounds a and b are
2021-08-26
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of Tanshinone I sale 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b
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Introduction Collagen deposition is a
2021-08-26
Introduction Collagen deposition is a common feature found in cancerous tissues and fibrotic organs/lesions. It is now well accepted that collagen deposition is not just a consequence of disease, but that it can also trigger a vicious cycle. Both chemical and physical signals elicited from collagen
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It has been shown that DAPK
2021-08-26
It has been shown that DAPK induces cell death through an increase in DAPK catalytic activity and subsequent phosphorylation of target proteins (Shang et al., 2005, Yamamoto et al., 2002), but its multidomain structure enables also a close physical interaction with other proteins (Bialik and Kimchi,
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Similarly LTD concentration dependently enhanced AQP express
2021-08-26
Similarly, LTD4 concentration-dependently enhanced AQP4 expression in astrocytes (Fig. 3). The LTD4-enhanced AQP4 expression was not affected by pranlukast but inhibited by Bay u9773, a non-selective CysLT1/CysLT2 receptor antagonist [33]. Because no selective CysLT2 receptor antagonists are current
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We neither observed changes in midazolam eCLmet
2021-08-26
We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c
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Our structures also provide new insights into
2021-08-26
Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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Preparation of the pyridyl ether analogs
2021-08-26
Preparation of the 2-pyridyl ether analogs (–) was accomplished by alkylation of alcohol with 2-bromopyridines in the presence of NaH to afford the desired pyridyl ether analogs in low to moderate yield. Preparation of the 3-pyridyl analog was carried out by conversion of alcohol to the tosylate,
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br Transparency document br Results and Discussion
2021-08-26
Transparency document Results and Discussion Experimental Procedures Acknowledgments The casein kinase 1 (CK1) family consists of at least seven different gene products, often referred to as isoforms (α, β, γ1, γ2, γ3, δ, ε, with splice forms described for CK1α, γ, and ε (reviewed in )
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NPC L expression is both tissue and species
2021-08-26
NPC1L1 expression is both tissue- and species-specific. Consistent with its function, NPC1L1 is mainly localized to the brush border membrane of enterocytes and the canalicular membrane of hepatocytes. NPC1L1, which is expressed in the liver of humans and rats but not mice, mediates cholesterol Phos
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ERR and ERR share high sequence homology
2021-08-26
ERRα and ERRγ share high sequence homology at their DNA binding domain (98% identity) and bind response elements in a similar fashion (Fig. 3 and Liu et al., 2005), yet ERRγ shows high variability in its capacity to stimulate the different response elements, whereas ERRα does not (Fig. 6A). For exam
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Although BPA has been proven to cause many health issues
2021-08-26
Although BPA has been proven to cause many health issues such as obesity and neurological toxicity (Rubin, 2011), the effects and mechanisms of BPA on the human tumorigenesis and cancer development are still not well illustrated. In the present study, we found that 10 to 10M BPA significantly promot
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Our study revealed elevated basal Akt
2021-08-25
Our study revealed elevated basal Akt phosphorylation in diet-induced obesity, the effect of which was reversed by ETAKO. Activation of Akt promotes cardiac hypertrophy via a number of cellular mechanisms including activation of its downstream targets such as mTOR and GSK3β [45, 46]. Short-term acti
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