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A robust meta analysis of
2020-11-27
A robust meta-analysis of 22 randomized clinical trials found that application of ischemic preconditioning strategies reduce ventricular arrhythmias [3]. Additionally, it was demonstrated that remote ischemic perconditioning (perRIC) induces immediate cardioprotection during ongoing ischemia by atte
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br RING type E s and their substrates
2020-11-27
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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In the context of E ligase drug discovery it is
2020-11-27
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 me
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Herein the interactions of etamicastat nepicastat and zamica
2020-11-27
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the 5 03 mg exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remains
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Acridine Orange hydrochloride After incorporation of random
2020-11-27
After incorporation of random Acridine Orange hydrochloride by TdT during heavy-chain rearrangements, both TdT and pol λ may perform in trans polymerase activity (in unknown proportions), whereas synthesis of the complementary strand can only be achieved by pol λ using its gap-filling activity, whic
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br Conclusion br Conflict of interest br Author
2020-11-27
Conclusion Conflict of interest Author contributions Acknowledgements Piyamas Kanokwongnuwut was supported by the Development and Promotion of Science and Technology Talent Project (DPST), Royal Thai Government Scholarship. Funding for the work was provided by the Attorney General’s Depa
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Other factors also contribute to replication fork
2020-11-27
Other factors also contribute to replication fork progression in DNA damage conditions. For instance, the cullin Rtt101 has a role in fork movement through alkylated DNA, probably associated to a damage tolerance mechanism [52], and TORC signaling is also important for fork progression in response t
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To examine the influence of aromatic
2020-11-27
To examine the influence of aromatic motifs on the bridging lysine esters we analysed DNA alkylating activity of the set of compounds 1–6. The lysine derivatives were chosen as it is relatively easy to prepare different esters and thereby study the impact of different groups on the reactivity toward
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br Materials and methods br Results
2020-11-27
Materials and methods Results Discussion To date, several reports have suggested an involvement of DGK in bipolar disorder. A splice variant at the COOH-terminus of DGKβ has been related to bipolar disorder [15] and DGKβ KO mice showed hyperactive behavior [17]. For the other DGK isoforms,
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br Conclusion The present work describes the
2020-11-27
Conclusion The present work describes the synthesis of 18 naphthoquinonolyl-1,2,3-triazole compounds based on natural product modification with antiplasmodial activity. Lapachol derivatives disclosed higher activity than the natural product. Six of these final modified lapachol 1,2,3-triazole com
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In this context we initiated a
2020-11-26
In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in SJB3-019A replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines, structu
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In anticipation of an approach based on modification
2020-11-26
In anticipation of an approach based on modification of the cyclohexylacetic TAME australia subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1, alth
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On the other hand the IL promoter activity
2020-11-26
On the other hand, the IL-8 promoter activity induced by the signalling cascade of the CysLT1-G300S receptor is higher than that of the WT receptor. The chemokine IL-8 is mainly involved in the recruitment and activation of neutrophils and we have previously shown that this chemokine gene is a targe
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Opiate withdrawal promotes the activation of the corticotrop
2020-11-26
Opiate withdrawal promotes the activation of the corticotropin-releasing factor (CRF) system, a major coordinator of neuroendocrine and behavioral responses to stressors. For instance, early (8–48 h) morphine withdrawal is associated with increased CRF mRNA expression in the central nucleus of the a
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A-740003 synthesis br Conclusion br Introduction Interleukin
2020-11-26
Conclusion Introduction Interleukin (IL)-18 [1] is a member of the IL-1 cytokine family activating corner stones of inflammatory signaling, among others nuclear factor (NF)-κB and p38 mitogen-activated protein kinase. Striking similarities exist between IL-1β and IL-18 including processing by
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