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br ARIs in the prevention
2024-06-21
5ARIs in the prevention of prostate cancer Prostate cancer continues to be a leading cause of male deaths worldwide. In 2009, it was estimated there would be 192,280 new cases of prostate cancer with a predicted 27,360 deaths [25]. Because androgens, and specifically DHT, play a large role in bot
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Because of its role in tumor growth proliferation
2024-06-21
Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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br Introduction S http www apexbt com media diy images
2024-06-21
Introduction Systemic lupus erythematosus (SLE) is a group of systemic autoimmune disorders characterized by anti-nuclear Kasugamycin hydrochloride australia (ANA), rashes and photosensitivity, joint inflammation, nephritis, and other clinical criteria. SLE develops through the breakdown of three
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Over the past decade extensive research has been directed to
2024-06-21
Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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This study evaluated the anti
2024-06-21
This study evaluated the anti-tumor influences of LA against HepG2 Cinobufagin in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed toward the mitochondrial-me
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Apelin induced G i activation has been demonstrated as
2024-06-21
Apelin induced Gαi activation has been demonstrated as a benefiting effect on cardiac contractility [12], [38], [39], and a vasodilator activity that protects against angiotensin-II-induced cardiovascular fibrosis and atheroma [40], [41]. In contrast, stretch causes hypertrophy through diminishing G
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AP was originally described as a
2024-06-21
AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi
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br Acknowledgments br Introduction Alzheimer s disease AD is
2024-06-21
Acknowledgments Introduction Alzheimer's disease (AD) is a severe neurodegenerative disorder primarily affecting the elderly population. Senile plaques in the brain, one of the pathological hallmarks of AD, are formed by the accumulation of aggregated β-amyloid (Aβ) with an extensive β-sheet s
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Application of the broad acting HTR antagonist
2024-06-20
Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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The biology of the A BR is complex
2024-06-20
The biology of the A2BR is complex and needs to be considered contextually as the expression and effect of receptor engagement varies according to time post hypoxic injury, cell type and downstream signaling pathway. For example, A2BR expression is dynamic - low under basal and increasing under isch
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The hippocampus is the primary brain structure
2024-06-20
The hippocampus is the primary brain structure involved in learning and memory. The role of hippocampal synaptic plasticity in neurological processes in cognition and depression has been extensively demonstrated. Synaptophysin is a critical substance in synaptogenesis, which is necessary for learnin
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The most potent compounds within the current
2024-06-20
The most potent compounds within the current series of compounds were therefore , , , , and , with 8-Methoxypsoralen synthesis possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM aga
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The synthesis and secretion of adrenal androgens
2024-06-20
The synthesis and secretion of adrenal androgens is apparently unique to humans and nonhuman primates, and requires the expression of key mediators such as CYP17 [26]. Endocrine control of CYP17 expression in rhesus monkeys is comparable to that in humans [27]. An analysis of baboon cDNA for CYP17 s
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Our previous studies found that some steroid mimetic
2024-06-20
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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br Acknowledgements We thank Dr Stefan Schulte Merker and
2024-06-20
Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific
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