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We found that several anticancer drugs inhibit HT receptor c
2024-09-24
We found that several anticancer drugs inhibit 5-HT3 BI 10773 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 is used frequentl
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Our previous studies found that some
2024-09-24
Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du
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In the mammalian brain synapse formation is followed by a
2024-09-24
In the mammalian brain, synapse formation is followed by a period of synapse refinement, and autophagy has been shown to play an important role in this process. For example, Tang and colleagues found that autophagy is required for the developmental pruning of dendritic spines, and that this pruning
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Recent studies showed that the
2024-09-24
Recent studies showed that the increased expression of Aurora B kinase directly proportional to the tumor invasion and metastasis [61]. The Aurora B kinase regulates the PI2K/Akt signaling pathway has a significant role in tumor invasion and metastasis that leads to phosphorylation of GSK3β on ser 9
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Screening a selection of analogues from this library
2024-09-24
Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to V5 Epitope australia 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demo
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br Animals Female Sprague Dawley SD rats aged
2024-09-24
Animals Female Sprague Dawley (SD) rats, aged 3 months with body weight between 180-210 g were housed in cages and acclimatized to standardized lab conditions (temperature 23 ± 2°C, humidity 50 ± 5% and 12 h light-dark cycles). The rats were fed with standard rodent food pellet (Harlan Diet, Ross
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br Acknowledgements This work is sponsored by the
2024-09-24
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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br Experimental All reagents were analytical grade and were
2024-09-24
Experimental All reagents were analytical grade and were used without further purification. The morphology was characterized using a field emission scanning electron microscope (Philips XL-30 FESEMFeSEM, ZEISS SUPRA 40VP, Germany). The hydrogel sample used for SEM analysis was freeze dried. All e
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br Nanoparticle Conjugated Topoisomerase Inhibitors
2024-09-24
Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5
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Our present result that week old PKA mice express
2024-09-24
Our present result that ≤2-week-old 150ΔPKA mice express normal LTP that does not depend on CP-AMPARs also supports the collective findings of previous work showing that LTP mechanisms are remarkably adaptable in juvenile animals compared with adults. In particular, GluA1 knockout, S845A/S831A, and
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Regarding androgens it is known that they are
2024-09-23
Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco
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br Oxidative microbe killing and
2024-09-23
Oxidative microbe killing and V-ATPase Oxidative killing of phagocytosed microorganisms is predominately achieved through the uptake of large quantities of molecular oxygen by the infected cell and the activity particularly of the NADPH oxidase complex on phagosomes (Savina et al., 2006) and the
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Demonstration of in vivo efficacy of potential chemopreventi
2024-09-23
Demonstration of in vivo efficacy of potential chemopreventive agents in animal models is necessary for their clinical development. Our present study provides experimental evidence that CuB 0.1μmol by oral administration (for 2weeks before the cancer cell injection, 5days per week) significantly inh
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As previously mentioned when hypoxia treated
2024-09-23
As previously mentioned when hypoxia-treated cells become re-oxygenated they sustain a significant amount of DNA damage which has been attributed to the formation of reactive oxygen species . This finding represents more than just an interesting in vitro phenomenon as within a tumor, cells have been
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The allosteric site of class
2024-09-23
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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