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Therefore the rational design of target compounds
2024-05-09

Therefore, the rational design of target compounds is based on the hybrid of attractive phenotypic bis-indole (5, Fig. 1) and sulfonamide moieties, in which the indole core might anticipate in hydrophobic interaction, and the functionality of sulfonamide group may involve in H-bonding with the site
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Besides Arg overexpression our data revealed that AGEs
2024-05-09

Besides Arg2 overexpression, our data revealed that AGEs could decrease eNOS mRNA levels, which is considered a significant cause for attenuated NO production and vasodilation. It was found recently that AGEs significantly reduce eNOS expression levels and NO bioavailability in human carotid artery
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The enzyme Arginase ARG plays a role
2024-05-09

The enzyme Arginase 1 (ARG1) plays a role in the hepatic urea cycle by hydrolyzing L-arginine to L-ornithine and urea [13]. In the context of macrophages and MDSCs, ARG1 expression redirects L-arginine metabolism to abolish cytotoxic nitric oxide production [14], suppress T-cell function [15], [16],
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br Acknowledgements This work is sponsored
2024-05-09

Acknowledgements This work is sponsored by the National Natural Science Foundation of China (grant no. 31201963) and Youth Backbone Teachers Project in Henan Province Department of Education, China (grant no. 2016GGJS-061). Introduction Acute lymphoblastic leukemia (ALL) is a malignant disord
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The crucial role of AP
2024-05-09

The crucial role of AP-1 in establishing and maintaining cell type-specific gene expression programs and cell identity is further apparent during reprogramming of mouse embryo fibroblasts (MEFs) into iPSCs with either Oct4/Sox2/Klf4/cMyc (OSKM ) factors , or chemicals . Using ATAC-seq to profile ch
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Various antiangiogenic drugs have been analyzed over the las
2024-05-08

Various antiangiogenic drugs have been analyzed over the last few years; noteworthy, bevacizumab, a monoclonal antibody against VEGF-A, alone or in combination with cytotoxic agents showed interesting results in terms of radiographic response rates and progression-free survival in initial phase 2 st
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Several mechanisms of Cd induced carcinogenicity
2024-05-08

Several mechanisms of Cd-induced carcinogenicity have been reported and are comprehensively summarized by Hartwig [32]. As early as 1980, basic science studies supported a role for endocrine disruption of AR by Cd. Donovan et al. [33], using extracts of mouse prostate cytosol, showed Cd to be the mo
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br Introduction The structural similarities between puromyci
2024-05-08

Introduction The structural similarities between puromycin (1, Fig. 1) and the aminoacyl adenyl terminal of aminoacyl–tRNA allow it to terminate the protein synthesis process by causing premature release of a polypeptide from the ribosome [1], [2]. Tremendous progress in the study of puromycin an
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casein kinase 2 The lactam emerged as lead candidate due to
2024-05-08

The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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In this study we demonstrated that DRR protein
2024-05-08

In this study, we demonstrated that DRR1 protein level in GBM tissues was significantly higher compared to normal IWR-1-endo tissues. This data suggested that DRR1 might play a role in the tumorigenesis of glioma. To investigate whether DRR1 could accurately predict the outcome in patients with glio
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AdipoR and AdipoR have been reported
2024-05-08

AdipoR1 and AdipoR2 have been reported to be present in almost all type of tissues and low ion channels levels have been observed in white adipose tissue (Inukai et al., 2005). These receptors have been observed to become deregulated with the onset of obesity, resulting in a reduced level of APN ex
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It could be hypothesized that the adiponectin system is
2024-05-08

It could be hypothesized that the adiponectin system is regulated by gonadal steroid hormones. The lowest concentrations of adiponectin, AdipoR1 and AdipoR2 proteins in the endometrium and myometrium during the mid-luteal and late-luteal phases suggest that progesterone suppresses the expression of
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Whether similar mechanisms play a
2024-05-08

Whether similar mechanisms play a role in adiponectin signal transduction and whether additional proteins are recruited to adiponectin receptors via APPL1 has not been analysed so far. Although it has been clearly established that APPL1 is a downstream adaptor protein in adiponectin signal transduct
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Does dietary caffeine interfere with antinociception by
2024-05-08

(8) Does dietary caffeine interfere with antinociception by other modalities that alter pain (TENS, exercise, joint mobilization, water immersion therapy)? Caffeine and/or A1R antagonists inhibit antinociception by each of these modalities in preclinical studies, such that there is potential for int
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br A Rs which were cloned
2024-05-08

A3Rs, which were cloned and then pharmacologically identified in the early 1990s, are expressed in multiple organs and peripheral tissues including glycine receptors involved in inflammatory responses (Gessi et al., 2008, Borea et al., 2014). While low levels are expressed in the CNS, A3R agonist
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