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A rational approach for the
2025-02-14
A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime
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A role for YAP in mediating resistance to
2025-02-14
A role for YAP in mediating resistance to EGFR inhibition has also been described [28], [29]. In line with these evidences, we observed increased YAP activation in all the generated EGFR TKI–resistant cells, testified by decreased phosphorylation on the inhibitory serine 127, enhanced nuclear locali
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High-throughput antiviral screening The ATX LPA signaling ax
2025-02-14
The ATX–LPA signaling “axis” [5] has been implicated in a perplexing variety of physiological and pathophysiological processes, including vascular and neural development [5], [26], [27], [28], [29], tumor progression and metastasis [30], [31], lymphocyte trafficking [22], bone development [32], neur
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br Acknowledgements br Introduction Thus
2025-02-14
Acknowledgements Introduction Thus, damage to the VER155008 may produce severe consequences (National Research Council, 1992). Indeed, though the nervous system has several compensatory and adaptive mechanisms, it is vulnerable to toxic insult, due to its inability to regenerate after lethal
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br Aurora kinases br Wnt signaling pathway The
2025-02-14
Aurora kinases Wnt signaling pathway The signal transduction pathway of Wnt/β-catenin signaling pathway plays an important role in embryogenesis to control cell differentiation and tumorigenesis [39]. A recent report indicates that 90% of colorectal cancer occur due to the activation of the Wn
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How does the ATM to ATR switch occur
2025-02-14
How does the ATM-to-ATR switch occur at DSBs? The progressive attenuation of ATM activation could be attributed to the loss of DNA structures that activate ATM, or to the generation of DNA structures that interfere with ATM activation. Our finding that SSOs do not directly affect the binding of puri
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br Regulatory mechanisms of ASK activity
2025-02-14
Regulatory mechanisms of ASK1 activity The functions of ASK1 in disease ASK1 inhibitor As mentioned above, ASK1 plays a pivotal role in the pathogenesis of various diseases; hence, an ASK1 inhibitor has therapeutic potential. Although inhibitors of the ASK1 downstream kinases p38 and JNK ar
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Chlorogenic acid an abundant polyphenol found in coffee and
2025-02-14
Chlorogenic 5 alpha reductase inhibitor (7), an abundant polyphenol found in coffee and the human diet, has various biological activities including antioxidant and anticancer effects [54]. Jiang et al. reported that compound 7 had a selective cytotoxic activity on human oral tumor cells (HSG, HSC-2
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Hsp also called FK binding protein FKBP is one of
2025-02-14
Hsp56 (also called FK506-binding protein 52, FKBP52) is one of the steroid receptor-associated immunophilins with tetratricopeptide repeat domains, which serve as binding sites for Hsp90 (Peattie et al., 1992). Hsp56 is elevated in breast cancer compared with normal breast tissue (Ward et al., 1999)
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Since artemisinin shows low solubility and poor
2025-02-14
Since artemisinin shows low solubility and poor oral bioavailability [8], [9], derivatizations of artemisinin were carried out and yielded different semisynthetic antimalarial drugs such as artemether and sodium artesunate. Artemether (decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano [4.3-
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Optical coherence tomography angiography is another promisin
2025-02-14
Optical coherence tomography angiography is another promising method for the assessment of corneal neovascularization. This relatively new modality is not yet widely used in part because of current limitations in the definition of images produced, lack of functional information, and inability to det
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In addition a substantial knowledge
2025-02-14
In addition, a substantial knowledge has been gained about the main properties of AT1R, such as ligand preference, signaling, regulation, and trafficking. However, it is less known how AT1R and other plasma membrane receptors affect each other’s function, and how these crosstalk mechanisms can be ut
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It has been reported that leukotrienes and their
2025-02-13
It has been reported that leukotrienes and their receptors, e.g. the cysteinyl leukotriene receptor 1 (CysLT1) may promote CCG 203971 receptor injury (Ding et al., 2007) and that increased 5-LOX expression and activity lead to production of brain-toxic molecules (Khan et al., 2010). However, differ
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br Conflict of interest br Acknowledgments br Introduction I
2025-02-13
Conflict of interest Acknowledgments Introduction Inflammation is a protective response of the microcirculation to harmful stimuli. Yet, excessive inflammation is potentially harmful and a characteristic of many chronic diseases [1]. 5-Lipoxygenase (5-LO, EC1.13.11.34) contributes to the in
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We showed that activation of the ATM ATR pathway
2025-02-13
We showed that activation of the ATM/ATR pathway leads to over-replication through suppression of CDK1 activity, consistent with previous findings that suppression of CDK1 activity is involved in the polyploidization of megakaryocyte and trophoblast cells [36], [37], [38], [39]. Suppression of CDK1
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