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br Conclusions This report describes the discovery of
2020-12-18
Conclusions This report describes the discovery of a new class of host-directed antiviral agents characterized by a 1-aryl-4,6-diamino-1,2-dihydrotriazine scaffold, responsible for a host (human) DHFR inhibition mechanism. Host-targeting antivirals represent an alternative and emerging strategy t
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Gene amplification PCR amplifications were performed
2020-12-18
Gene amplification. PCR amplifications were performed using genomic DNA from the different organisms studied as template and two degenerate oligonucleotides (PP1 and PP2) as primersPP1 corresponded to the sense codons of the amino Methylprednisolone motif AGGI(A/S)EM, and PP2 to the antisense seque
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As we all known hypoxia is a hallmark
2020-12-17
As we all known, hypoxia is a hallmark of tumour microenvironment, which is a key regulator of tumour growth and metastasis [4]. Hypoxia meditates a series of cellular responses including angiogenesis by activating transcriptional factor hypoxia inducible factor (HIF), which is consist of an obligat
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The requisite extended benzyl alcohols and and final potenti
2020-12-17
The requisite extended benzyl alcohols –, , and and final potential DFG-out binding hybrid inhibitors – and – were prepared as shown in , . Benzaldehyde was alkylated with -methoxybenzyl chloride and then reduced with sodium borohydride to give benzyl alcohol . Pyridine derivative was prepared by
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Various domains of the HSA molecule have also
2020-12-17
Various domains of the HSA molecule have also been used to make bioconjugates with increased stability, better targeting properties, and/or extended half-lives in blood. For example, domain I of HSA has been used in the preparation of antibody conjugates. This was achieved through the use of a cyclo
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Since its inception ADEPT approach has been widely
2020-12-17
Since its inception, ADEPT approach has been widely reported by many groups using a variety of enzymes and prodrugs (see reviews) [12], [14]. Both mammalian and non-mammalian enzymes have been utilised. Of the mammalian variety, human β-glucuronidase in combination with many prodrugs [17], [18] and
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A further quandary concerning rediscoveries arises in habita
2020-12-17
A further quandary concerning rediscoveries arises in habitats modified and frequented by humans, where rediscovered species may occur through accidental or deliberate introductions (Metcalf et al., 2007) rather than having persisted despite adverse conditions. Confusion regarding origin could evoke
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To further define the importance of CYP
2020-12-17
To further define the importance of CYP3A for OSC metabolism in vivo, a strong CYP3A inhibitor ketoconazole was used to test whether CYP3A would affect its metabolism. As expected, the biotransformation of OSC to SC was significantly decreased by ketoconazole at all three substrate concentrations. H
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Over the past decade targeting DNA
2020-12-16
Over the past decade, targeting DNA repair proteins has emerged as an effective tool to enhance chemosensitivity of malignant cells [9]. However, identification and selection of the proper target of DNA repair pathways is critical to increase cytotoxic activity of chemotherapeutic agents in cancer c
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Primases are classified into two
2020-12-16
Primases are classified into two major groups: first, the DnaG primases, found in bacteria and bacteriophages, and second, the archaeoeukaryotic primases. Remarkably, bacterial and archaeoeukaryotic primases have no structural similarity and, presumably, evolved independently (Leipe et al., 1999). T
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Cdc which is involved in
2020-12-16
Cdc42, which is involved in filopodium formation, and Rac1, which is involved in lamellipodium formation, engage in cross-talk with one another [25,26,30,31]. In general, filopodium formation precedes lamellipodium formation, and filopodium formation (Cdc42 activity) suppresses lamellipodium formati
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br Acknowledgements br Membrane bound proton
2020-12-16
Acknowledgements Membrane-bound proton-translocating inorganic pyrophosphatases (H-PPase; EC 3.6.1.1) belong to a recently identified category of proton pumps, distinct from F-, P-, and V-ATPases, which utilize pyrophosphate hydrolysis as the driving force for H movement across biological membr
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The aim of this study was to
2020-12-16
The aim of this study was to evaluate the role of aberrant methylation of promoter regions of tumor suppressor genes in the clonal evolution from MGUS to MM. Thus, we analyzed in MGUS, SMM, and symptomatic MM patients, the methylation status of 4 genes—p15, p16, p53, and DAPK—whose promoter hypermet
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Elevated production of cysLTs in
2020-12-16
Elevated production of cysLTs in 1,3-PBIT dihydrobromide and rhinitis in general and aspirin-sensitive disease in particular10, 11, 26, 27 has been implicated in causing epithelial cell activation and excessive mucus secretion, which characterize these diseases.2, 28 It is of particular interest, t
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Recent pharmaceutical research in the
2020-12-16
Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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