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All desired compounds with a carboxylic acid substituent at
2023-10-19

All desired compounds with a carboxylic Vinpocetine substituent at N1 position of the quinoxalinone scaffold and a variety of aromatic substituents at C3 position were obtained by the syntheses starting from methoxy-substituted 3-chloro-quinoxalin-2(1)-ones () prepared as previously. As shown in ,
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Gratifyingly compound also demonstrated improved physicochem
2023-10-19

Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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br Does TIPARP contribute to the
2023-10-19

Does TIPARP contribute to the diverse species sensitivity to TCDD toxicity? In chick embryo hepatocytes TIPARP was reported to mediate the TCDD-dependent suppression of hepatic gluconeogenesis, by reducing cellular NAD+ levels and reducing PCK1 expression, suggesting that ADP-ribosylation enhance
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It is well known that TCDD is the most
2023-10-19

It is well-known that TCDD is the most potent ligand of AhR and it regulates gene expression, such as CYP1A1, via activation of AhR (Mimura and Fujii-Kuriyama, 2003). Besides Tomblin et al. (2016) have recently shown that TCDD via AhR regulated L-type amino pop over to this website transporter 1 ex
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AMPK is an essential player in adiponectin signaling
2023-10-19

AMPK is an essential player in adiponectin signaling pathway that regulates energy metabolism. The fact that suppression of AMPK activity by compound C largely diminished candesartan-mediated inhibition of NFκB via blocking AT1 also suggests that the AT1-mediated effect is at least partly resulted f
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H-Lys(Z)-OH receptor In addition to the data
2023-10-19

In addition to the data provided by the Ki16425 treatment in the K/BxN arthritis model, new findings from the study of two new LPA receptor antagonists confirm the involvement of the LPA pathway in the pathogenesis of experimental arthritis. In the study by Miyabe et al., the authors reported the tr
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br Viral manipulation of host factors
2023-10-19

Viral manipulation of host factors to oppose anti-viral autophagy To escape or manipulate autophagy, some viruses developed strategies that are based on the recruitment of host-cell endogenous factors. The non-enveloped double-stranded DNA virus adenovirus is rapidly endocytosed after attachment.
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Aurora A or B selective
2023-10-19

Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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br Funding This study was supported by
2023-10-19

Funding This study was supported by Grant UM1-CA186690 (NCI-CTEP) and R01CA204173 (CJB). This project used the UPCI Cancer Pharmacokinetics and Pharmacodynamics Facility (CPPF) and was supported in part by award P30-CA47904 and R50CA211241. Introduction Despite the efficacy of platinum based
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Several studies have explored the relationship between
2023-10-18

Several studies have explored the relationship between dental implants and MRONJ development. López-Cedrún JL et al. [13] reported that BRONJ developed after implant treatment in nine patients who were taking bisphosphonates orally. The mean interval between the initiation of treatment and the onset
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Infections inflammation and corneal transplant can all cause
2023-10-18

Infections, inflammation, and corneal transplant can all cause corneal neovascularization via upregulation of inflammatory cytokines, which attract myeloid 6015 into the cornea. These myeloid cells establish a cycle of cytokine secretion and further myeloid cell recruitment in the cornea. There are
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Evidence from basic science studies suggests that Cd may
2023-10-18

Evidence from basic science studies suggests that Cd may play a role in prostate cancer through disruption of the androgen receptor (AR). AR, a hormone-activated transcription factor, is the key driver of prostate cancer progression [6]. Ironically, the AR is also required for normal prostate growth
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br Acknowledgements This work was supported by National Natu
2023-10-18

Acknowledgements This work was supported by National Natural Science Foundation of China (Nos. 21376172, 21528601 and 21621004) and the Natural Science Foundation of Tianjin from Tianjin Municipal Science and Technology Commission (Contract No. 16JCZDJC32300). Introduction Alzheimer’s disease
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Modulating the ability of tumor cells to detoxify ROS is
2023-10-18

Modulating the ability of tumor THZ531 receptor to detoxify ROS is a key mechanism by which cysteine metabolism affects tumor cell survival. One study observed hypermethylation of cysteine dioxygenase (CDO1) in 60% of tested breast cancer samples, leading to increased ROS detoxification and tumor c
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br Preliminary remarks Expression of the
2023-10-18

Preliminary remarks Expression of the transcription factor aryl hydrocarbon receptor (AHR) and the AHR-repressor (AHRR) are both strikingly high in the Irinotecan of barrier organs skin and gut [1,2]. It is generally assumed that this reflects their role in linking environmental factors to an ad
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