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In order to improve the methodology of the synthesis of
2024-04-26
In order to improve the methodology of the synthesis of steroidal derivatives, our goal was the investigation of aza-Michael addition of different N-nucleophiles to 16-dehydropregnenolone in the presence of [DBU][OAc] as catalyst and reaction medium. Michael addition of electron deficient steroidal
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In this scenario the receptor tyrosine
2024-04-26
In this scenario, the receptor tyrosine kinase inhibitors (TKI), sunitinib, an anti-angiogenic agent, was tested in phase III trial, leading to a longer progressing free survival when compared to interferon (median: 11 vs. 5mo, respectively, hazard ratio (HR) = 0.42; 95% CI: 0.32–0.54; Praas inhibit
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The Rv c EQ protein was purified from ml
2024-04-26
The Rv2477c-EQ2 protein was purified from 600 ml induced cultures following the same protocol described above. Elution of the mutant protein from the affinity resin was done using 200 mM imidazole. After concentration and buffer-exchange of protein as described above, the purity of the protein was c
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Of the many different types
2024-04-26
Of the many different types of DNA lesions, DNA double strand breaks (DSBs) are amongst the most deleterious. It has been suggested that a single unrepaired DSB may be sufficient to induce cell death (Bennett et al., 1993), whereas misrepaired DSBs can result in loss of genetic information, potentia
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In the pituitary of R quelen mRNA
2024-04-26
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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CB-839 Chlorogenic acid an abundant polyphenol
2024-04-26
Chlorogenic CB-839 (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) as compared with nor
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br Introduction Endothelial progenitor cells EPCs present a
2024-04-26
Introduction Endothelial progenitor cells (EPCs) present a class of blood cells with an ability to form new blood vessels relying on pre-existing vessels, which contribute to postnatal angiogenesis [1], [2]. A wide range of studies have demonstrated that EPCs play a critical role in angiogenesis
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Since at least prospective cohort studies have
2024-04-26
Since 2005, at least 14 prospective cohort studies have been conducted to clarify inconsistencies in the field, ten of which suggested a direct correlation between antibiotic use and atopy or wheezing later in life [51–60], three found no association [61–63], and one found positive association only
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Zinc Pyrithione mg Since the first studies of betaine aldehy
2024-04-25
Since the first studies of betaine aldehyde oxidation in rats [13], the participation of betaine in the detoxification of homocysteine has well described, considering the activity of other Zinc Pyrithione mg as betaine homocysteine methyltransferase and methionine synthase. But, there is a lack of
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Young et al described the role of adenine monophosphate acti
2024-04-25
Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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src kinase inhibitor br Discussion With recently improved un
2024-04-25
Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e
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In the late s Solvay Pharmaceuticals
2024-04-25
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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All consecutive patients who were confirmatively diagnosed w
2024-04-25
All consecutive patients who were confirmatively diagnosed with MP-PPE and TPE, respectively, between January 2008 and December 2016 at Kyungpook National University Hospital, a tertiary referral hospital in South Korea, an area with an intermediate prevalence of active tuberculosis, were enrolled.
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The most potent compounds within the
2024-04-25
The most potent compounds within the current series of compounds were therefore , , , , and , with CHIR-98014 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 against the 17α-OHas
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Steroidal CYP inhibitors can further be classified based on
2024-04-25
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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