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A rational approach for the design of new steroid compounds
2023-08-18
A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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Accumulating data suggest that ROS trigger autophagy but in
2023-08-18
Accumulating data suggest that ROS trigger autophagy but, in turn, autophagy reduces ROS levels [23]. Our results are in agreement because 27-OH mediated autophagy induction interms of LC3 II formation and Beclin 1 protein expression was suppressed by treating the promonocytic cells with the antioxi
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Previous studies have demonstrated that the expression of th
2023-08-18
Previous studies have demonstrated that the expression of the Aurora B gene is maximally increased at G2/M phage during mitosis (Honda et al., 2003, Fu et al., 2007, Goldenson and Crispino, 2015), and exhibits an extraordinary upregulation in a number of human cancers (Fu et al., 2007, Kollareddy et
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br Materials and methods br Results
2023-08-18
Materials and methods Results Discussion Proteomics analyses generate mountains of data, expression information for hundreds or thousands of proteins in a single experiment (Wojcik and Schächter, 2000). Recently proteomics and bioinformatics provide new understandings about the processes in
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CPI-169 Receptor Subtypes and Their Function Critical Apprai
2023-08-18
Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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Since immunoassays cannot specifically quantify each apelin
2023-08-18
Since immunoassays cannot specifically quantify each apelin peptide, a more reliable approach, mass spectrometry (MS) has been used recently to quantify and characterize apelin fragments in plasma. Using this technology, Zhen et al. showed that [Pyr-1]-apelin-13 was the major apelin form present in
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No starting dose adjustment is needed
2023-08-18
No starting dose adjustment is needed for mild or moderate renal impairment and mild hepatic impairment (Child-Pugh A classification) though use in patients with severe hepatic impairment (Child-Pugh classification Class C, 10–15 points score) is not recommended.8, 9, 10, 13 Drug interaction & ad
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Based on their different sources the APN
2023-08-17
Based on their different sources, the APN inhibitors (APNIs) can be divided into the natural products and synthetic compounds. Bestatin (1, Fig. 1), isolated from the Streptomyces oliuoreticuli by Umezawa et al., is the first reported and only marketed natural dipeptidomimetic inhibitor of APN. Afte
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br Conflict of interest statement br
2023-08-17
Conflict of interest statement Introduction Currently, adenocarcinoma is the most common histological subtype of lung cancer. Activating mutations and translocations with a potential for targeted therapy are reported predominantly in non-smokers. ALK rearrangement is found in less than 5% of u
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We start with a basic description of
2023-08-17
We start with a basic description of the MT-SGL model. Consider a multi-task learning (MTL) setting with k tasks. Let p be the number of covariates, shared across all the tasks, and n be the number of samples. Let denote the matrix of covariates, be the matrix of responses with each row correspond
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ALK fusion positive NSCLC is clinically actionable
2023-08-17
ALK fusion-positive NSCLC is clinically actionable because it can be targeted by several FDA-approved drugs, including the first generation TKI crizotinib, which is a dual inhibitor to MET and ALK [15], and the second generation inhibitors, alectinib and ceritinib, both of which are highly-selective
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br Introduction br Rac dependent ROS
2023-08-17
Introduction Rac1-dependent ROS and novobiocin mg regulation in neuronal functions NOX-mediated ROS have an important role as physiological messengers. One remarkable example regarding such a function is during axonal formation. In this line, increased p40phox/NOX2 levels and co-localization
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XAP044 Toxicity is the main reason for the failure at all
2023-08-17
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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isoxsuprine receptor The results show that a tonic action of
2023-08-17
The results show that a tonic action of ACh on respiration is lacking. However, it is clear that muscarinic cholinergic mechanisms can modulate both eupneic breathing and the cough reflex. When these mechanisms are brought into action is obscure and only tentative proposals can be advanced. ACh in t
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It is already established in the literature
2023-08-17
It is already established in the literature that products synthesized by 5-LO, such as lipoxin A4, can activate PPARγ in a setting of experimental stroke [43]. Interestingly, experiments using 5-LO knockout mice in an endotoxemia model to mimic septic conditions, demonstrated reduced multiple organ
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