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The inhibition of ACLY induces an
2024-05-14
The inhibition of ACLY induces an anticancer effect that has been reported to be involved in mitochondrial reactive oxygen species (ROS) generation [14], [16], dual blockade of mitogen-activated protein kinase and phosphatidylinositol-3-kinase/AKT pathways [11], and the glycolytic phenotype of tumor
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Analysis of ASK crystal structures as well as
2024-05-14
Analysis of ASK1 crystal structures as well as an investigation of how BMS-626529 4 might bind were undertaken to understand opportunities for engaging Gln756. To this end a docking model derived from PDB 3VW622 was used to predict the binding mode of amide 4 in the ASK1 active site as shown in Fig
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Colistin Sulfate receptor The first objective of the
2024-05-14
The first objective of the present study was to investigate the impact of ageing on arginase activity in tissues which exhibit age-related impairments in their function. The second objective was to determine whether l-arginine supplementation modulated the effect of ageing on arginase activity. The
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APJ receptor expression is altered in various cardiovascular
2024-05-14
APJ receptor expression is altered in various cardiovascular diseases, and both increases as well as decreases in APJ receptor expression have been reported. A decrease in mRNA and protein levels of APJ receptors was observed in patients with ischemic heart disease or idiopathic dilated cardiomyopat
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fty720 Enhancers are short regions of DNA that are bound
2024-05-14
Enhancers are short regions of DNA that are bound by DNA-binding proteins (TFs) to increase the likelihood of a particular gene to be expressed. Importantly, enhancers can be identified, and classified, by their patterns of chromatin accessibility and of enrichment in certain histone modifications.
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The current results also demonstrated tendencies toward decr
2024-05-13
The current results also demonstrated tendencies toward decreased serum Aβ40 levels and increased Aβ42 levels during the 1-year follow-up. These tendencies are consistent with the results of a previous study that evaluated Aβs in the CSF of patients with late-life depression (Pomara et al., 2016). T
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The lactam emerged as lead candidate
2024-05-13
The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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Although several ARIs have reached various phases
2024-05-13
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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Many of the cellular processes regulated by AKT activation
2024-05-13
Many of the cellular processes regulated by AKT activation are also controlled by other intracellular pathways such as the MAPK pathway, the PLCγ pathway, but also, directly or indirectly, by signaling pathways not linked to RTK transmembrane receptors, such as growth factor-linked signaling affecti
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We aim to evaluate the AK
2024-05-13
We aim to evaluate the AK in regulating adenosine signaling in the retina. It was reported that the degree of ceramidase injury directly depends on expression levels of AK and the resulting extracellular levels of adenosine (Boison, 2006). Indeed, transgenic mice overexpressing AK are highly suscep
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Our initial approach to identify hits was
2024-05-13
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI muscarinic receptor antagonists library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for pro
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Additional evidence for a putative role of COXs and LOX
2024-05-13
Additional evidence for a putative role of COXs and 5-LOX in AD derives from pharmacological studies using inhibitors of these enzymes (for review, see Firuzi and Praticò, 2006). In addition to helping delineate the pathobiological mechanisms of AD, these results raise hope for discovering novel the
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Eicosanoids are locally acting signaling lipids that are
2024-05-13
Eicosanoids are locally acting signaling lipids that are produced from C20 polyunsaturated fatty acids (PUFAs), including arachidonic BAMB-4 (AA, C20:4), eicosapentaenoic acid (C20:5) and eicosatrienoic acid (C20:3) (Dennis and Norris, 2015; Funk, 2001; Stables and Gilroy, 2011). According to their
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In order to increase the oral bioavailability abiraterone
2024-05-13
In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral bms-690514 of abiraterone acetate (156), it is recommended that this drug should be taken on an
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Despite functional studies demonstrating the role of HT in u
2024-05-13
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,