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In view of the ubiquitous distribution of
2023-10-17
In view of the ubiquitous distribution of the arachidonate 12S-lipoxygenase isoforms and the variety of cellular reactions influenced by the resulting arachidonate metabolites, these products widely play important roles in many biological systems. The development of new type-specific inhibitors of t
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br Experimental procedure br Funding The present study
2023-10-17
Experimental procedure Funding The present study was supported by the Grant Russian Foundation for basic research (project no. 16-04-01517). Introduction 5-HT, a monoaminergic neurotransmitter, is synthesised from l-tryptophan catalysed by the enzymes tryptophan hydroxylase (Tph) and aroma
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br Conclusions and clinical relevance
2023-10-17
Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic Temozolomide is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonists or ADK
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The synthesis and secretion of
2023-10-17
The synthesis and secretion of adrenal androgens is apparently unique to humans and nonhuman primates, and requires the expression of key mediators such as CYP17 [26]. Endocrine control of CYP17 expression in rhesus monkeys is comparable to that in humans [27]. An analysis of baboon cDNA for CYP17 s
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In plants altered expression of
2023-10-17
In plants, altered expression of Aurora kinases results in impaired meiotic divisions followed by the formation of aneuploid or polyploid progenies [21]. This observation is interesting from an evolutionary point of view because it can be assumed that, during evolution, the influence of biotic and a
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br ASK in Huntington s disease and other polyglutamine
2023-10-17
ASK1 in Huntington's disease and other polyglutamine diseases The polyglutamine (polyQ) diseases are a group of inherited neurodegenerative disorders caused by the expansion of cytosine-adenine-guanine (CAG) trinucleotide repeats in the coding regions of specific genes, leading to the production
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Hsp also called FK binding
2023-10-16
Hsp56 (also called FK506-binding protein 52, FKBP52) is one of the steroid receptor-associated immunophilins with tetratricopeptide repeat domains, which serve as binding sites for Hsp90 (Peattie et al., 1992). Hsp56 is elevated in breast cancer compared with normal breast tissue (Ward et al., 1999)
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br Discussion Hepatic dysfunction in the metabolic syndrome
2023-10-16
Discussion Hepatic dysfunction in the metabolic syndrome is a driver of negative patient outcomes that requires more therapeutic options. The complexity of liver alterations in this disease – elevated de novo synthesis of fatty acids and cholesterol, reduced clearance of circulating atherogenic L
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ALDHs also act as opposite roles in the
2023-10-16
ALDHs also act as opposite roles in the initiation and development of carcinoma. For example, ALDH2, as a key enzyme which oxidises acetaldehyde, participates in alcohol metabolism and is associated with alcohol-mediated carcinogenesis [37]. It has been reported that up to 8% of the world's populati
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The finding that OCT is expressed in the nucleus accumbens
2023-10-16
The finding that OCT3 is expressed in the nucleus accumbens (Gasser et al., 2009) suggests that inhibition of this transporter may underlie previously described effects of glucocorticoids on extracellular DA concentrations and indicates that DA clearance in this region is not mediated exclusively by
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Kif15-IN-1 australia Adiponectin belongs to the CTRP C
2023-10-16
Adiponectin belongs to the CTRP (C1q/TNF-related protein) superfamily. Except for adiponectin, 15 additional members have been identified (CTRP1-15) (Schaffler and Buechler, 2012). Of all the CTRPs, CTRP9 has the highest identity to adiponectin in globular domain (Wong et al., 2009). The structure o
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While A Rs communicate mainly with the D R subtype
2023-10-16
While A1Rs communicate mainly with the D1R subtype [36], A2AR and D2R interaction occurs mainly in basal ganglia. D2Rs colocalizes with A2ARs in this Dehydroepiandrosterone sale area where they are preferentially localized postsynaptically in the soma and dendrites of GABAergic striatopallidal neur
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Our initial approach to identify
2023-10-16
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI Ketoprofen library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility was
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br Experimental section br Results and discussion br Conclus
2023-10-16
Experimental section Results and discussion Conclusion Acknowledgements This work was financially supported by Recruitment Program of Global Experts, and the Director Foundation of XTIPC, CAS, Grant No. 2015RC011. This work was also financially supported by Natural Science Foundation of
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Aurora A or B selective
2023-10-16
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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