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Our last area of exploration was the piperidine
2021-09-22
Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th
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Though regulation of ghrelin interaction with
2021-09-22
Though regulation of ghrelin interaction with GHSR has not been described previously, a precedent for a similar regulatory mechanism exists in the form of the interaction between Agouti-Related Protein (AgRP) and melanocortin receptor subtypes MC3R and MC4R (Ollmann, 1997). AgRP is produced by hypot
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In stark contrast to this study Zhang
2021-09-18
In stark contrast to this study, Zhang and colleagues demonstrated that FFA4, along with FFA1, play roles in suppressing cell proliferation and promoting apoptosis in CRC GZD824 treated with omega-3 PUFA [53]. In this study design, in vivo CRC was induced in mice upon treatment with the genotoxic c
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In addition to removing proteins and organelles related
2021-09-18
In addition to removing proteins and organelles related to iron and lipid metabolism, an alternative mechanism by which autophagy promotes ferroptosis is through the formation of the BECN1-solute carrier family 7 member 11 (SLC7A11) complex [42,43]. SLC7A11 is the main component of the antiporter sy
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br Funding The research for this paper is conducted
2021-09-18
Funding The research for this paper is conducted as part of a PhD thesis at Pasteur Institute of Iran and it was financially supported by Pasteur Institute of Iran and the Iranian Centre for Communicable Diseases. Conflict of interest Acknowledgments Introduction The viral enzyme integr
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br Acknowledgments We would like to thank
2021-09-18
Acknowledgments We would like to thank Coordenação de Aperfeiçoamento de Pessoal do Ensino Superior (CAPES) and Conselho Nacional de Desenvolvimento Cientifico e Tecnológico (CNPq) for the grants and scholarships provide to the authors of this work. Introduction Human Immunodeficiency Virus t
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71 5 br Introduction Stroke is the second cause
2021-09-18
Introduction Stroke is the second cause of death worldwide and the first cause of acquired motor disability in adults [1], [2]. In sub-Saharan Africa, stroke is the first cause of admission in neurology departments [3]. In Cameroon, the in-hospital mortality of stroke is estimated at 26.8% [4]. A
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br Neurodystrophic effects of HO It
2021-09-18
Neurodystrophic effects of HO-1 It is well known that neonatal hyperbilirubinemia (jaundice) may lead to irreversible neurological injury in children (kernicterus). This outcome can be prevented by photodegradation of circulating bilirubin or treatment with metalloporphyrin inhibitors of HO enzym
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3-Bromopyruvic acid Biochemical and genetic studies indicate
2021-09-18
Biochemical and genetic studies indicate that the endosomal sorting complex required for transport (ESCRT) machinery is crucial for Hh exovesicle packaging and morphogen gradient function 39., 43., 44.. In vertebrates, ESCRT proteins promote the release of Shh exovesicles to maintain progenitor cell
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Importantly HDACi mediated effects are cell and HDAC specifi
2021-09-18
Importantly, HDACi-mediated effects are cell and HDAC specific; different effects and outcomes have been observed in different cell types, targeting different HDAC isoforms. While HDACi exhibit a strong proapoptotic potential in human leukemia 2478 mg 19, 20, 21, 22, they have a limited ability to
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Substrate affinity and specificity can
2021-09-18
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of Eplerenone bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of sho
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DNA methylation is a kind of epigenetic
2021-09-18
DNA methylation is a kind of epigenetic modifications that can be described as a heritable alteration in gene expression, without any changes in the DNA sequence. Recent evidences suggest that the regulation of DNA methylation status is a frequent and early event in prostate carcinogenesis. For exam
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As part of our discovery efforts
2021-09-17
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragmen
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Obestatin synthetized mainly in the gastrointestinal tract p
2021-09-17
Obestatin, synthetized mainly in the gastrointestinal tract, participates in the regulation of metabolic functioning at both central and peripheral levels (food intake, pancreatic activity or/and adipocytes proliferation) (Granata et al., 2008; Li et al., 2011). It is involved in the complex gut-bra
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Oxidative stress results from the disequilibrium between
2021-09-17
Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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