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Zhang et al screened three
2024-04-13
Zhang et al. screened three thousand compounds library and found two active 3,5,6-substituted indolin-2-one molecules. Further, they designed various derivatives of this scaffold and among them compound 23 from the series was found active with 1.8 μM on Aurora-B kinase luminescent assay [53]. Jeffe
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br Materials and methods br Results
2024-04-13
Materials and methods Results Discussion Despite the relative complexity of immunotherapy, such treatment may have an important role, in conjunction with other therapies in the treatment of cancer refractory to conventional treatments alone. Clinical studies have recently shown that adding
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br Introduction AMP activated protein kinase
2024-04-12
Introduction AMP-activated protein kinase (AMPK) has been found to be a key character against cardiovascular diseases and cellular stress. When activated by certain stress, AMPK regulates sugars and fatty acids that are good or detrimental to the heart. For example, targeting AMPK phosphorylation
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br Results The newly synthesized leucine
2024-04-12
Results The newly synthesized leucine ureido derivatives were firstly evaluated for their enzymatic inhibition using porcine kidney APN (Microsomal, Biocol) with bestatin as the positive control (Table 1). One isoleucine ureido derivative 14 and phenylglycine ureido derivative 15 were also synthe
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MD was the recipient of the Intergroupe Francophone
2024-04-12
MD was the recipient of the Intergroupe Francophone de Cancérologie Thoracique (IFCT) Alain Depierre Grant in 2014. JP was the recipient of the ARISTOT (Association de Recherche, d’Information Scientifique et Thérapeutique en Oncologie Thoracique) grant in 2016. Conflicts of interest statement
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br Introduction Psychostimulant abuse and
2024-04-12
Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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br Discussion With recently improved understanding of the ro
2024-04-12
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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Our initial approach to identify hits was two
2024-04-12
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI PF-5274857 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 Results br Discussion Dopamine regulates behavioral respo
2024-04-12
Results Discussion Dopamine regulates behavioral responses to nicotine in Drosophila (Bainton et al., 2000), but neurochemical measurements of dopamine after nicotine stimulation had not been made. Here, we demonstrate for the first time that the stimulation of nAChRs causes dopamine release i
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Thirty six of the analogs synthesized showed ATX inhibition
2024-04-11
Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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Several genes related to metabolism post transcriptional
2024-04-11
Several genes related to metabolism, post-transcriptional regulation, chromatin structure, and signaling pathways are required for the sexual development and virulence of G. zeae (Baldwin et al., 2010, Bluhm et al., 2007, Ding et al., 2009, Han et al., 2007, Hou et al., 2002, Jenczmionka et al., 200
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In this study we found that
2024-04-11
In this study, we found that ACL silencing is sufficient to impair myoblast differentiation and that this effect is accompanied by a decrease in MYOD early in the myogenic process and by a subsequent decline in fast MyHC protein CM-272 at a later stage of differentiation (Figure 4J). Furthermore, o
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br Conclusions and clinical relevance Astrogliosis and
2024-04-10
Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic WM-2474 is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonists or ADK inhib
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The diagnosis of ICP is currently based on the presence
2024-04-10
The diagnosis of ICP is currently based on the presence of pruritus, raised fasting serum TBS levels above 10μmol/L, and/or elevated serum transaminases (in the absence of diseases that cause cholestasis or pruritus) as well as spontaneous relief of signs and symptoms within four to six weeks after
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Among the most important Ca regulatory mechanisms are
2024-04-10
Among the most important Ca regulatory mechanisms are the Plasma Membrane Calcium ATPase (PMCA) and Sarcoplasmic Reticulum Calcium ATPase (SERCA). These pumps belong to the family of P-ATPases, which share the formation of an acid-stable phosphorylated intermediate as part of their reaction cycle. P
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