• Optimization of the B ring specifically

  2024-11-22

  

  Optimization of the B-ring specifically targeted preventing the oxidation of the ring system (). As described above, the 4-position of the phenyl ring provides the appropriate vector towards bulk solvent. - and -linked substitutions at the 4-position of the B-ring from the 4-fluoro-nitrophenyl inter

• Because of its role in tumor growth proliferation

  2024-11-22

  

  Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t

• While the yeasts and see

  2024-11-22

  

  While the yeasts and (see Glossary) each contain only one Aurora homolog, Ipl1p (increase in ploidy 1) and Ark1 (Aurora-related kinase 1), respectively 5, 6, , and Xenopus laevis contain two Aurora kinases: Aurora A and Aurora B [4]. Mammals have three Aurora kinases, A, B, and C (Figure 1). In an

• Recent progress has been made in translating animal findings

  2024-11-22

  

  Recent progress has been made in translating animal findings on memory performance and amnestic effects – that are largely determined by tonically active receptors in which α5 contributes to the benzodiazepine binding site. Based on the observation that deletion of this subunit led to improved spati

• br AR signaling and urothelial cancer

  2024-11-21

  

  AR signaling and urothelial cancer progression As shown in other types of malignancies, such as prostate cancer cells, it has been documented that androgens induce AR expression and its nuclear translocation as well as ARE promoter activity in urothelial cancer cells (Chen et al., 2003, Izumi et 

• A has been reported to decrease

  2024-11-21

  

  Aβ has been reported to decrease insulin receptors and impair insulin signaling in neurons, preventing phosphorylation of Akt and glycogen synthase kinase 3β (GSK-3β), downstream of insulin signaling, and to increase phosphorylation of tau protein causing neurofibrillary tangles (Tokutake et al., 20

• dub ubiquitin br Conclusions br Material and methods br Conf

  2024-11-21

  

  Conclusions Material and methods Conflicts of interest Acknowledgements Introduction Currently more than 30 human proteins are implicated in a range of degenerative disorders owing to their misfolding and misassembly into various aggregate structures and leading to at least 20 serious

• The present study determined the

  2024-11-21

  

  The present study determined the effect of DCA on VSMC calcification in vitro and in atherosclerotic ApoE-/- mice in vivo. We found that CPI-455 receptor non-toxic concentrations of DCA, did not affect VSMC viability, induced calcification of VSMC in culture and increased atherosclerotic vascular c

• br Discussion AhR is a receptor that

  2024-11-21

  

  Discussion AhR is a receptor that binds to a great variety of lipophilic compounds, in particular those containing at least one aromatic ring (Abel and Haarmann-Stemmann, 2010, Guyot et al., 2013, Hahn, 2002). The main known function of this receptor is to induce the metabolism of these compounds

• This chemistry paved way for multi gram synthesis of which

  2024-11-21

  

  This chemistry paved way for multi-gram synthesis of which was utilized for extensive piperazine benzamide SAR exploration. Depicted in , the two-step operation towards final targets involved standard amide coupling conditions with EDC or HATU followed by Boc deprotection under acidic conditions.

• br Concluding remarks Following the disappointing

  2024-11-21

  

  Concluding remarks Following the disappointing outcomes of Aβ immunotherapy trials for AD [62], the current prevailing concept is that disease-modifying therapy must be initiated from the presymptomatic stage of the disease because of the presumed incurability of chronic diseases once they become

• br Discussion Here we focused on seven

  2024-11-21

  

  Discussion Here, we focused on seven plant alkaloids extracted from yokukansan. These alkaloids individually inhibited 5-HT-mediated 5-HT3A and 5-HT3AB receptor currents weakly. Simultaneous administration of these alkaloids, however, inhibited the 5-HT3A and 5-HT3AB receptor currents strongly. T

• dan shen br New AMPK activators Fenofibrate is a drug

  2024-11-21

  

  New AMPK activators Fenofibrate is a drug of the fibrate class used for the treatment of dyslipidemia [53] but is also an agent that could alleviate DN-induced alterations through AMPK activation (Fig. 2). Streptozotocin-induced diabetic rats treated with fenofibrate improved in not only renal fu

• The H N mutation in exon

  2024-11-20

  

  The H373N mutation in exon 6 has not previously been reported [3], [4], [5], [6]; thus, this mutation appears to be a novel mutation. The functional expression study demonstrated that the H373N mutation results in almost complete loss of enzymatic activity. Thus, it is highly likely that the H373N m

• The present study indicates elevated ATX activity

  2024-11-20

  

  The present study indicates elevated ATX activity as a highly sensitive and specific biomarker to differentiate ICP from other pregnancy-related liver disorders or pruritic dermatoses. In MPTP hydrochloride to the current gold standard for diagnosis, total fasting serum bile salt levels, ATX appear

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