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This review is an overview on
2021-11-09
This review is an overview on the ongoing trials involving anti-FGF-FGFR therapies (Wu et al., 2013). Pathway FGFR in cancer A recent study comparing more than 4800 tumor tissue samples has shown that 7.1% of all tumor types have genetic alterations in the FGF-FGFR axis. The aberrations perce
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We then explored the possible mechanisms by which
2021-11-09
We then explored the possible mechanisms by which integrin α5β1 was involved in the PHEV proliferation process. Normally, the virus activates integrin and induces its downstream protein activation to promote its own invasion and proliferation. Human papillomavirus type 16 (HPV16) binds to heparan su
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Cy3 azide We notice that previous reports
2021-11-09
We notice that previous reports of arsenic exposure are not completely consistent with each other, in terms of exposure-changed histone acetylations. In an early investigation, As exposure (7.5 μM) of HepG2 Cy3 azide increased H3K9ac after 24 h, when analyzed by methods of immunofluorescence and We
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br ABT aR aR methyl hexahydropyrrolo b pyrrol
2021-11-09
ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo
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It is important to mention
2021-11-09
It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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By combining the results of the melting
2021-11-08
By combining the results of the melting curve analysis of exon 5 and exon 6, the allelic setup of our 250 subjects was determined; the four allelic variants are shown in Table 1. However, GSTP1-1 *A/*C and GSTP1-1 *B/*D could not be distinguished from one another because both genotypes are character
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As GLO is the major detoxification
2021-11-08
As GLO1 is the major detoxification system of reactive dicarbonyls, it is plausible that differences in production and activity of the enzyme influences AGE production and the development and/or modulation of diabetic neuropathy. Glo1 exists as a copy number variant (CNV) in many inbred strains mice
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The ion conduction pathway reported herein accounts for
2021-11-08
The ion conduction pathway reported herein accounts for all known functional properties of EAAT/GltPh anion channels. Simulations reveal unitary current amplitudes and ion selectivities (Figures 3C and 3D) that resemble experimental results (Melzer et al., 2003, Wadiche and Kavanaugh, 1998). The cal
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An advantage of photolabeling with tritiated photoprobes fol
2021-11-08
An advantage of photolabeling with tritiated photoprobes followed by microsequencing with Edman degradation is the ability to both identify the photolabeled isoxazole receptor and to quantify photoincorporation which enables assessment of pharmacological specificity and allosteric interactions with
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Stimulation of FPR by bacterial
2021-11-08
Stimulation of FPR by bacterial N-formyl peptides induces basophil and mast apexbio dilution release of immunogenic compounds such as histamine [21], [31]. Furthermore, we demonstrated that histamine plays a role in F-MITs-induced sepsis-like symptoms since cimetidine, a histamine H2-receptor antag
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Attractively existing reports suggest that cellular
2021-11-08
Attractively, existing reports suggest that cellular ferroptosis also probably plays vital role in liver fibrosis [[62], [63], [64]]. Carlson BA et al. illuminated that the ferroptosis regulator GPX4 was important for hepatocyte survival and proper liver function [62]. Sun X et al. showed that Nrf2
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Accordingly and in animal models a high
2021-11-08
Accordingly and in animal models, a high-fat diet rich in CO (CO-HFD) impeded ventricular function and induced cardiac cell death and remodeling, at least, by down-regulating cell antioxidant defense systems and induction of oxidative stress [28], [29], [30], [31]. Interestingly, long chain fatty ac
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The ability to metastasize is the defining character of a
2021-11-08
The ability to metastasize is the defining character of a cancer and the leading cause for resultant mortality. It is hypothesized that a rare subset of cancer cells, often operationally referred to as “cancer stem cells” (CSCs), are responsible for sustaining cancer metastasis and recurrence [1]. T
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Among the various epigenetic mechanisms involved in EwS path
2021-11-08
Among the various epigenetic mechanisms involved in EwS pathogenesis, we focused on the PRC enzyme EZH2, since it is a direct target of EWSR1-FLI1 and a critical mediator of malignant cell growth.24, 30 Our observation that the inhibition of EZH2 in GD2neg EwS UM 171 induces GD2 expression leads us
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Sometime ago we have described diamino triazines
2021-11-08
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by ibmx and zymosan. In this work we describe new derivative
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