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Sunitinib Actin is capable of polymerizing spontaneously How
2023-09-05

Actin is capable of polymerizing spontaneously. However, this process is relatively slow and kinetically unfavorable in cells. Formation of Sunitinib dimers and trimers, which can easily disassemble due to their instability, is a rate-determining step in actin polymerization [5], [6]. The shape and
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In conclusion we have demonstrated that diaryl
2023-09-05

In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi
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Based on the observation that antipsychotic drugs
2023-09-04

Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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The syntheses of a and b are
2023-09-04

The syntheses of 27a and 27b are shown in Scheme 5. Substituted naphthalene 21c was brominated using N-bromosuccinimide (NBS) and 2,2′-azobis(2-methylpropionitrile) (AIBN) to yield 25, which was subjected to lactam cyclization to form 26a and 26b, respectively. Deprotections of each 4E1RCat yielded
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Because R gene is positively
2023-09-04

Because 5α-R2 gene is positively regulated by T and in the prostate gland (Torres et al., 2003), and our BPA-treated rats showed decreased circulating T and probably intraprostatic androgen levels, it might be responsible for the decrease of 5α-R2 expression. However, in a previous work using castra
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In the pituitary of R quelen
2023-09-04

In the pituitary of R. quelen mRNA levels of cyp19a1b were found to be higher in males than females, suggesting a sex-specific function, and perhaps a local action to regulate gonadotropins or other pituitary hormone secretion (Olivereau and Callard, 1985; Zhang et al., 2014). Interestingly, the hig
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br Acknowledgement br Introduction Estrogens play
2023-09-04

Acknowledgement Introduction Estrogens play an important role in the development and progression of breast cancer (McGuire et al., 1976; Clemons and Goss, 2001). 17β-Estradiol (E2), the most biologically active estrogen in breast tissue, functions via its nuclear receptors, estrogen receptor (
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Interestingly metabolic dysfunction is also observed in amyo
2023-09-04

Interestingly, metabolic dysfunction is also observed in amyotrophic lateral sclerosis (ALS). Patients and mouse models of familial ALS exhibit higher levels of resting melanocortin 1 receptor expenditure and lower fat-free mass, indicating a hypermetabolic phenotype. Lim et al. (2012) found that r
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br Depletion of serum amino acids Currently the
2023-09-04

Depletion of serum amino acids Currently, the only anticancer agents that directly target amino Terbinafine metabolism are bacterial l-asparaginases (from Escherichia coli and Erwinia chrysanthemi), which are FDA-approved for treatment of pediatric and adult ALL. A potential complication of usin
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To further clarify the vascular
2023-09-04

To further clarify the vascular cell types expressing AR subtypes, double immunofluorescence staining for ARs and vascular endothelial buy b12 receptor or vascular smooth muscles was performed. As shown in Fig. 3, Fig. 4, overlay images show the expression of all ARs subtypes that we examined in vas
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The acetylcholinesterase AChE inhibitor tacrine THA exerts n
2023-09-04

The acetylcholinesterase (AChE) inhibitor, tacrine (THA), exerts neuroprotective effects in time- and does-dependent manners against glutamate neurotoxicity (Takada-Takatori et al., 2006a, 2006b) and amyloid-β protein toxicity in PC12, a pheochromocytoma line (Wang et al., 2002; Xiao et al., 2000).
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Despite functional studies demonstrating the role of
2023-09-04

Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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br Acknowledgements We thank Dr Stefan
2023-09-01

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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Although we have achieved a great deal of success
2023-09-01

Although we have achieved a great deal of success in the development of tools to understand autophagy in health and disease, highly specific reagents for autophagy manipulation and deep knowledge of autophagy is required to advance the research in therapeutic treatment. Better disease (ischemia) ani
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opiate receptors br Innate immune mechanisms that confront v
2023-09-01

Innate immune mechanisms that confront viral infection Autophagy induction by virus sensing Antiviral xenophagy and virophagy The presence of viral particles within autophagosomal structures has been visualized in only rare instances. This is the case for HSV-1 when it is devoided of ICP34.
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