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A compound structurally similar to PF has been
2022-03-07

A cftr inhibitor structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)pheny
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Here we examine the impact of hypoxia
2022-03-07

Here we examine the impact of hypoxia on lake whitefish (Coregonus clupeaformis) during embryonic and larval development. Lake whitefish are a cold-water salmonid endemic to North America and are found from western Alaska, USA to eastern Labrador in Canada. Spawning occurs from late autumn to early
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The Hedgehog signaling pathway HH pathway hereafter is
2022-03-07

The Hedgehog signaling pathway (HH pathway hereafter) is vital for development and tissue homeostasis. [4] In recent years, studying the role of the HH pathway in carcinogenesis and cancer stemness has highlighted the HH inhibitors as putative cancer therapeutics [5]. However, clinical application
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For further understanding of the
2022-03-07

For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex
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Several studies have reported that the
2022-03-07

Several studies have reported that the genotype and allele frequencies of S267F vary considerably between different study groups and geographical regions (Ezzikouri et al., 2017, Hu et al., 2016, Lee et al., 2017, Li et al., 2014, Pan et al., 2011, Peng et al., 2015, Yang et al., 2016, Zhang et al.,
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br Patients and methods br
2022-03-07

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
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Concerning the molecular mechanisms underlying transcription
2022-03-07

Concerning the molecular mechanisms underlying transcriptional regulation of the GSTP1-1 gene expression we and others have characterized structural and functional properties of the human GSTP1-1 promoter. GSTP1-1 gene promoter activity is driven by a TATA-box [16] as well as Spl [16], [17], AP-1 [1
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br Consequence physiological function of ROS
2022-03-07

Consequence/physiological function of ROS-dependent inhibition of GSNOR Plants response to environmental changes induced by abiotic and biotic factors by enhanced accumulation of ROS resulting in temporary imbalance of the cellular redox homeostasis. This as oxidative stress/burst termed event tr
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In recent years several DPP
2022-03-07

In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic CGP41251 with a unique xanthine scaffold developed through high-throughpu
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Initial evidence that cell contact mediated transmission
2022-03-07

Initial evidence that cell-contact-mediated transmission of HIV-1 is relevant for the generation of latently infected VX-702 was suggested in the context of transmission from dendritic cells to resting CD4+ T cells (Evans et al., 2013, Kumar et al., 2015). As dendritic cells probe for antigens, the
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In summary we discovered azaindole substituted hydroxypyrido
2022-03-04

In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that
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To further investigate the molecular
2022-03-04

To further investigate the molecular mechanisms that underlie glycine's β-cell protective effects through its antioxidative activity in diabetes, we used a H2O2/high glucose-induced apoptosis cell model. Similar effects on ROS generation of high glucose and H2O2 support the in vivo results, suggesti
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The dorsal horn of the
2022-03-04

The dorsal horn of the spinal cord shows a high density of Ca2+-permeable AMPA receptors, particularly in the superficial spinal laminae (laminae I and II), where primary afferents carrying nociceptive and thermoreceptive inputs terminate and synapse on spinal second-order neurons (Engelman et al.,
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Although in in vitro analyses GANT sensitized
2022-03-04

Although in in vitro analyses GANT61 sensitized Daoy AVL-292 to RITA treatment, this was not fully reflected in the in vivo xenograft studies in nude mice, as the combinatorial treatment elicited a comparable reduction of tumor growth. However, the dual drug administration reduced within-group vari
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br Materials and methods Manganese chloride
2022-03-04

Materials and methods Manganese chloride (MnCl2·4H2O), glutamate, glutamine, Lucifer Yellow, polyclonal anti-GFAP and MTT assay kits were purchased from Sigma Chemical Co. (St. Louis, MO). Dulbecco's Modified Eagle's Medium-F12 (DMEM-F12) with Earle's salts, foetal bovine serum, penicillin, and s
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