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Moreover mice exposed to high cholesterol
2024-08-05
Moreover, mice exposed to high-cholesterol diet have mildly activated astrocytes, increased expression of ApoE and aquaporin-4 in the hippocampus, and altered levels of proteins associated with Aβ metabolism (Chen et al., 2016), which is related to a higher demand for cholesterol transport and the n
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To validate the identified phosphorylation sites in the mous
2024-08-05
To validate the identified phosphorylation sites in the mouse heart, we analyzed HEK 293T Erlotinib transfected with Adrb1 based on the hypothesis that protein residues phosphorylated both in vivo and in vitro are more likely to be physiologically relevant. All of the phosphorylation sites identifi
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Senexin B br Aberrantly enhanced adenosine signaling in reti
2024-08-05
Aberrantly enhanced adenosine signaling in retina of oxygen-induced retinopathy Current therapeutic development of ROP focuses on directly targeting VEGF and HIF-1α signaling pathway (Cavallaro et al., 2014, Penn et al., 2008, Mintz-Hittner et al., 2011, Hartnett and Penn, 2012). However, cellula
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br Introduction Fungi are an inexhaustible source of natural
2024-08-03
Introduction Fungi are an inexhaustible source of natural products mainly due to their wide distribution in the nature, estimated to range from 1.5 to 5.1 million species in the world [1]. Secondary metabolites from fungi represent a substantial fraction of drugs and drug models in pharmaceutical
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In order to increase the oral
2024-08-03
In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral evofosfamide of abiraterone acetate (156), it is recommended that this drug should be taken on a
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Thus one possible target for CRPC
2024-08-03
Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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In conclusion AXL overexpression preexisted in a subgroup of
2024-08-03
In conclusion, AXL overexpression preexisted in a subgroup of treatment-naive lung adenocarcinoma specimens harboring an activating EGFR mutation or in those with wild-type EGFR. Anti-AXL therapeutics delivered up front in combination with the EGFR inhibitor might overcome intrinsic or acquired resi
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For the NSCLC patients with EGFR activating mutations
2024-08-03
For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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Compound was docked into the
2024-08-03
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the d
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Transient transfection with ATR kinase dead D A and ATM
2024-08-03
Transient transfection with ATR kinase-dead (D2475→A) [30] and ATM kinase-dead (D2870→Ala and N2875→K) [31] constructs was performed using Fugene 6 (Roche Applied Science, Indianapolis). Three microliters of fugene 6+1μg plasmid was used in transfections using 6-well plates at 2×105 cells/well and a
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Furthermore low affinity sites that share
2024-08-03
Furthermore, low-affinity sites that share no structural homology with the aforementioned sites have been described in the transmembrane domain. It has been discovered that, in α1βγ2 receptors, potentiation of GABA-activated currents by high concentrations of diazepam is biphasic, with a high- and a
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celltiter blue The following are the supplementary data rela
2024-08-03
The following are the supplementary data related to this article. Competing interest Ethics approval and consent to participate Authors' contributions Acknowledgements The authors thank Dr. D. R. Kaplan for kind advice and materials derived from NB primary cell lines, Dr. F. D. Miller f
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Although the gene that encodes DHFR
2024-08-03
Although the gene that encodes DHFR has been strongly conserved during evolution, subtle differences in the active sites of bacterial, human and parasite E-4031 have been exploited to develop DHFR inhibitors specific to particular pathogens 1, 3. For example, pyrimethamine and cycloguanil bind stro
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Dyphylline The reception of antiangiogenic treatment in neur
2024-08-03
The reception of antiangiogenic treatment in neuro-oncology has yet to achieve the wide success rapidly accomplished for other malignancies. In 1984, mutated receptor tyrosine kinase became a culprit for aberrant tumorigenesis signal, providing a target for monoclonal Dyphylline (mAbs) and small-mol
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br Conflicts of interest br Funding br
2024-08-02
Conflicts of interest Funding Introduction Brassicaceae is an economically important family of plants containing rapeseed, cabbage, broccoli, brussels, radish and mustard. Among them rapeseed plays a crucial role, because of its application in food and also in fuel industry. According to th
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