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Aldose reductase AR is an NADPH dependent aldo
2023-03-22
Aldose reductase (AR), is an NADPH-dependent aldo-keto reductase very well studied as a catalyst of glucose conversion to sorbitol in the polyol pathway [11], [12]. In the diabetic lens characterized by chronically high levels of glucose, AR is responsible for production of high levels of sorbitol a
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The second evidence comes from the
2023-03-22
The second evidence comes from the results obtained by patch-clamp recordings carried out at the endplate region of isolated mouse FDB fibers, where adenosine and the P1R agonist NECA significantly affected the NPo, the open frequency and the time constant τ of the adult nAChR channels. It is genera
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Ultraviolet UV spectroscopy is commonly used for
2023-03-22
Ultraviolet (UV) spectroscopy is commonly used for screening potential ADA inhibitors [15]. In the UV method, the ADA reaction is calculated by measuring the decrease in absorbance of the substrate at 265 nm or increase in absorbance of the product at 248 nm. However, AD and inosine share a very clo
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The next level of possible
2023-03-22
The next level of possible correlation and comparison between the α7 and 5HT3 receptors is at the subunit arrangement and protein folding. Crystal structures of the nicotinic and serotoninergic racecadotril synthesis receptors [45], [46] reinforced the concept of similarities between these families
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The srd a isoforms showed unique
2023-03-22
The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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We found that several anticancer drugs inhibit HT receptor c
2023-03-22
We found that several anticancer drugs inhibit 5-HT3 Phorbol 12,13-dibutyrate mg current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinoteca
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In conclusion AXL overexpression preexisted in a subgroup of
2023-03-22
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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Introduction Mitotic kinases play an essential role in mitos
2023-03-22
Introduction Mitotic kinases play an essential role in mitosis, Aurora and other mitotic kinases are often observed over-expression in human solid and many hematologic cancers. As one of serine/threonine kinases, Aurora kinase family is involved in centrosome maturation, mitotic spindle formation,
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Intriguingly androgens may also have
2023-03-20
Intriguingly androgens may also have an indirect effect on AR gene expression through inhibition of the GATA2 transcription factor gene (He et al., 2014) (Table 1). Using ChIP-seq, GATA2 was found to bind to a regulatory element 5.5 kb upstream of the TSS of the AR gene and enhanced transcription, w
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br Acknowledgments and Disclosures br Alzheimer s disease as
2023-03-20
Acknowledgments and Disclosures Alzheimer's disease as a synaptic pathology Alzheimer's disease (AD) is a chronic neurodegenerative Darunavir Ethanolate disorder and the most common cause of dementia in the elderly. Progressive depositions of amyloid plaques and neurofibrillary tangles togethe
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br Development of lorlatinib from crizotinib
2023-03-20
Development of lorlatinib from crizotinib (1) to a clinical candidate (6) Xalkori (1, PF-02341066, crizotinib), was the first-in-class ALK inhibitor approved by the Unites States Food and Drug Administration (FDA) in 2011 as a first-line treatment for ALK+- NSCLC patients. This section describes
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To further demonstrate the significance
2023-03-20
To further demonstrate the significance of Nrf2 activation in the prevention of EGF-induced CRC growth by AR inhibitor, we examined the effect of fidarestat on EGF-induced cell viability in Nrf2-ablated cells. Our results suggest that AR inhibitor prevented the EGF-induced cell viability in control
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Most of the identified aldose
2023-03-20
Most of the identified aldose reductase inhibitors possess undesirable effects like poor pharmacokinetic properties, hypersensitivity and Steven-Johnson Syndrome [1]. However, the main side effect is the lack of selectivity relative to aldehyde reductase (ALR1, EC 1.1.1.2). ALR1 plays the important
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Bafetinib br Acknowledgements This work was supported
2023-03-20
Acknowledgements This work was supported by grants from the Program for Changjiang Scholars and Innovative Research Team in University (IRT_14R28), the National Basic Research Program of China (973) (Grant No.: 2013CB733602), the Major Research Plan of the National Natural Science Foundation of C
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Plant material and growth conditions Arabidopsis thaliana ec
2023-03-20
Plant material and growth conditions. Arabidopsis thaliana ecotype Columbia was grown on a mixture of soil, vermiculite, and perlite (4:2:1) with a 16h light/8h dark Cilomilast mg in a temperature-controlled growth room (22°C), unless indicated otherwise. Molecular cloning and plant transformation
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