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br Methods br Results br Discussion br Acknowledgements br
2024-06-17
Methods Results Discussion Acknowledgements This work was supported by the National Institutes of Health [Grant R21 NS081429], a Pilot Grant from the Vanderbilt Conte Center supported by the National Institutes of Health [Grant P50 M096972], and by the Department of Anesthesiology at V
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Steroidal CYP inhibitors can further be
2024-06-17
Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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However cancer and fibrotic diseases are
2024-06-17
However, cancer and fibrotic diseases are the most extensively studied disease states. ATX is connected to various cancers because it can stimulate chemokinesis and chemotaxis in melanoma cells. Upregulated ATX inhibitor of apoptosis proteins has been reported in breast cancer,, prostate cancer, t
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The Kelch like ECH associated protein
2024-06-17
The Kelch-like ECH-associated protein 1 (Keap1)-Nrf2 signaling pathway functions as one of the key regulator of the cellular defense system against oxidative stress [26]. Nrf2 is a redox-sensitive transcription factor, that is sequestered in the cytoplam by binding to Keap1; however, under oxidative
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br Acknowledgements br Introduction Thus damage to the
2024-06-17
Acknowledgements Introduction Thus, damage to the gtpase 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 dam
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ATM is generally regarded to be the principal mediator of
2024-06-17
ATM is generally regarded to be the principal mediator of the G1 Sodium valproate checkpoint, whereas the induction of the intra-S-phase and G2/M checkpoints are usually primarily related to ATR function. However, several studies have demonstrated that, depending on the cellular context and type of
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Despite these conflicting data about COX ER correlations
2024-06-17
Despite these conflicting data about COX-2/ER correlations, a large body of evidence supports that elevated COX-2 expression in breast cancer is a constant feature of high stage disease and a predictor of worse outcome. Upregulation of COX-2 protein has been identified in approximately 40% of cases
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br Under normal physiological conditions the
2024-06-17
Under normal physiological conditions, the agonist binds to AT1R on the surface of the plasma membrane and activates the receptor, mediating downstream signaling. Then, activated AT1R is phosphorylated by protein kinase C (PKC) [13] or G protein coupled receptor kinases (GPKs, such as GRK2 [13], G
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br Experimental section br Abbreviations PSA puromycin sensi
2024-06-14
Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino determining molarity deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS, N–hydr
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It was also shown that of crizotinib
2024-06-14
It was also shown that 15% of crizotinib resistance mechanisms can be due to an amplification of ALK gene while 30% are caused by a variety of secondary mutations (S1206Y, G1202R, L1196M, C1156Y, G1269A, L1152R, F1174L and 1151Tins) in ALK tyrosine kinase. These mutations can modify the conformation
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Adiponectin belongs to the CTRP
2024-06-14
Adiponectin belongs to the CTRP (C1q/TNF-related protein) superfamily. Except for adiponectin, 15 additional members have been identified (CTRP1-15) (Schaffler and Buechler, 2012). Of all the CTRPs, CTRP9 has the highest identity to adiponectin in globular domain (Wong et al., 2009). The structure o
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On the basis of the
2024-06-14
On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote
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Although the mechanisms of APP secretion are
2024-06-14
Although the mechanisms of APP secretion are well characterised (for review see Ref. [1]), production of soluble AChE species is less well understood although we have reported that a metalloproteinase can shed AChE similarly to APP [16], [17]. Recently it has also been demonstrated that cellular pre
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br COX and LOX in
2024-06-14
COX and 5-LOX in post-mortem AD brain Minghetti (2004) reviewed the findings on COX-2 mRNA levels in AD brains, pointing out that the available evidence demonstrated either decreased or increased levels, possibly because of the short half-life of COX-2 transcripts or individual variability. Histo
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We found that several anticancer drugs inhibit HT receptor
2024-06-14
We found that several anticancer drugs inhibit 5-HT3 Chlorprothixene synthesis 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). Irinotecan
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