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Since we found that the pharmacokinetic
2021-03-04
Since we found that the pharmacokinetic properties of KPT-185 were unsuitable when given subcutaneously or orally, it is not a candidate for in vivo therapy for NHL. However, the pharmacokinetic properties of KPT-276, a CRM1-inhibiting SINE structurally related to and with functional activities simi
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VE-821 Our results indicate that C CoA
2021-03-04
Our results indicate that C75-CoA is formed in the hypothalamus following stereotaxic injection of C75. Inhibition of hypothalamic CPT1 by C75-CoA in vivo, as seen in our experiments, is independent of the putative inhibition by malonyl-CoA, which may be formed after the action of C75 either on FAS
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br Introduction Esophageal squamous cell
2021-03-04
Introduction Esophageal squamous cell carcinoma (ESCC) is one of the most common types of cancer in East Asia and is a leading cause of cancer-related death worldwide.1, 2 Surgery is widely used for treatment in localized disease, where it can provide definitive management and potential cure. Tre
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Given its high frequency it is not surprising that
2021-03-04
Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant 4716 to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have been proved effe
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In the past few years DNA templated fluorescent
2021-03-04
In the past few years, DNA-templated fluorescent metal nanoparticles have been developed as ideal alternatives to organic dyes due to their facile synthetic process, outstanding optical properties, ultrafine size, and fine biological compatibility. Since the first successful demonstration of DNA-tem
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br DGKs bind and regulate
2021-03-04
DGKs bind and regulate other signalling proteins Based on the evidence noted above, DGKs achieve specificity of function through a combination of post-translational modifications, the availability of cofactors, and through the availability and access to substrate DAG. DGKs appear to achieve an ad
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Targeting both PARP and DHODH for anti
2021-03-04
Targeting both PARP-1 and DHODH for anti-cancer therapy would certainly be beneficial as these enzymes share a common role in the DNA replication and repair mechanisms which are involved in the hyper-proliferation of cancer cells. Since benzimidazole-containing compounds have been reported to show g
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Overall the DDR kinase domain has a typical
2021-03-04
Overall, the DDR1 kinase domain has a typical kinase domain structure and adequate sequence and/or structure similarity with other kinase domains, as shown in Fig. 2, which allow homology modeling of the active and inactive conformations. In addition to conformational changes to the activation loop
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An even more striking difference is observed
2021-03-04
An even more striking difference is observed when comparing active site residues, which are evolutionarily very well conserved in other soluble PPases 18, 19. In 31 known PPase sequences, 13 functionally important active site residues are conserved in all sequences, but only two of them (D70 and D97
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br Materials and methods Male
2021-03-04
Materials and methods Male Hartley guinea pigs (300–350g) were obtained from National Laboratory Animal Center, Taiwan. LTD4, LTC4, LTE4, LTB4, montelukast and BAY u9773 were purchased from Cayman Chemical, Ann Arbor, Michigan; Carbachol, atropine, l-serine, boric acid, l-cysteine and all buffer
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MTT results show that both pancreatic cell lines were quite
2021-03-03
MTT results show that, both pancreatic cell lines were quite sensitive to camptothecin (CPT), a well known topoisomerase I poison. Interestingly, CPT does not show any selectivity over cancer cell lines probably due to the duplication times for cancerous (MIA PaCa-2) and immortalized healthy (HPDEC)
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Some of the psychoactive actions
2021-03-03
Some of the psychoactive actions of nicotine are mediated by the nigrostriatal and mesolimbic pathways (Di Chiara, 2000, Di Chiara et al., 2004). The nigrostriatal pathway originates in the dopaminergic neurons located in the substantia nigra and terminates in the putamen and nucleus caudatus which
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POE specialises Rogers definition of engineering to systems
2021-03-03
POE specialises Rogers' definition of engineering [37] to systems engineering as: As such, systems engineering becomes a problem solving exercise, the problem being, given a physical environment E, to find the system S that Caspase-3/7 Inhibitor meets a real-world need N to the satisfaction of a gr
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Almost all previously published haplotype association studie
2021-03-03
Almost all previously published haplotype association studies have demonstrated the importance of haplotype reconstruction because the combinations of SNPs exert synergistic effects on protein function. Even synonymous polymorphisms within haplotypes can have functional consequences that are drastic
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benfotiamine The Fontan circulation When first described in
2021-03-03
The Fontan circulation When first described in 1971, the Fontan operation ushered in a new paradigm in the care of children born with the varied forms of complex congenital benfotiamine disease (CHD) characterized by a single effective pumping chamber.1., 2. This procedure, which creates a total ca
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