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Data from our in vitro studies using BEAS B cells
2019-11-26

Data from our in vitro studies using BEAS-2B cells showed a biphasic response of cells to NNK. The initial phase of decrease in CRM1 expression in NNK-exposed cells was observed in our previous study. In this study, we further showed that p-p53 (Thr55) expression was also decreased during this initi
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On the basis of the findings described above a series
2019-11-26

On the basis of the findings described above, a series of heterotricyclic analogs were designed and synthesized. The human CRF1 receptor binding and antagonist activity data for newly designed heterotricyclic core antagonists 28–33 are described in Table 3. Most of the tricyclic core analogs listed
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Another option is to use the thiol
2019-11-26

Another option is to use the thiol groups of cysteine residues, which can be modified by use of PEG-maleimide and vinyl sulfone. However, changes in PEGylation interactions or reaction conditions can result in changes in the functional properties of the therapeutic proteins [[50], [51], [52]]. A st
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Nearly years ago the first two enzymes
2019-11-26

Nearly 60years ago, the first two histamine-2 receptor antagonist which catalyze the phosphorylation of proteins were discovered [1]. Protein phosphorylation was originally identified as a regulatory mechanism for the control of glycogen metabolism. Today it is clear that protein phosphorylation re
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Cholesterol homeostasis is maintained through a tight regula
2019-11-26

Cholesterol homeostasis is maintained through a tight regulation between endogenous de novo synthesis, dietary absorption, utilization and excretion of bile salts. The NLG-8189 of cholesterol from the intestine constitutes the central part of cholesterol homeostasis in the body [41]. In particular,
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br Disclosure statement br Acknowledgment
2019-11-26

Disclosure statement Acknowledgment This work was supported by the National Natural Science Foundation of China (81270704, 81330018). Background Over-expression of cyclooxygenase-2 (COX-2) is common in many malignancies including non-small cell lung cancer (NSCLC) and is associated with po
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AH 7614 br ET Antagonist for the Future
2019-11-26

ET Antagonist for the Future: Macitentan and Atresentan Macitentan is an insurmountable antagonist, resulting from structure-activity studies to improve the efficacy and tolerability of bosentan, and gained approval in the United States in 2013 for the treatment of PAH. Actelion describes the com
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We postulate that OT contained in
2019-11-26

We postulate that OT contained in milk during early postnatal development causes a mild enteroprotective preconditioning of the ER (Fig 9). This is perhaps akin to a mechanism shown by others [50], [51], [52], which is characterized by selective activation of the IRE1a/XBP1/eIF2a (via PKR) UPR pathw
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BIBW 2992 br Results and discussion br Conclusion
2019-11-26

Results and discussion Conclusion Recent studies showed that EGFR signaling is involved in inflammatory response in several inflammatory conditions. The normal inflammatory macrophage BIBW 2992 show EGFR-dependent production of inflammatory mediators. Nevertheless, the development of EGFR inhi
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Recently a non proteolytic role of COP
2019-11-26

Recently, a non-proteolytic role of COP1 in stabilizing PIF3 proteins in the dark has been revealed . Previous studies have shown that the endogenous levels of PIF3 protein in etiolated seedlings were nearly undetectable . Ling found that the GSK3-like kinase BRASSINOSTEROID-INSENSITIVE 2 (BIN2) pla
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br Materials and methods br Results and discussion
2019-11-25

Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul
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5-Methoxy-CTP br Chemistry Scheme shows the
2019-11-25

Chemistry Scheme 1 shows the synthesis of compounds 15-1–15-33 from commercially available 2-(4-aminophenyl)acetonitrile (8a). Protection of the starting material 8a with di-t-butyl dicarbonate afforded 9. The reaction of 9 with methyl 1-chloroisoquinoline-4-carboxylate in the presence of sodium
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Besides the assessment of toxicological effects immediately
2019-11-25

Besides the assessment of toxicological effects immediately after exposure, we also studied the potential recovery of the exposed organisms, through the quantification of ChE activity at specific time intervals after placing organisms in clean test medium. Recovery from chemical challenge, in this c
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br Role of ERK signaling in preventive and
2019-11-25

Role of ERK signaling in preventive and therapeutic potential of flavonoids in neurodegenerative diseases ERK is one of the main pharmacological targets of natural phenolic compounds and contributes to several therapeutic approaches including anti-atherogenic, anti-cancer, anti-colitis, anti-arth
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br Methods and materials br Results
2019-11-25

Methods and materials Results Discussion Many small molecules have been individually explored to enhance endothelial barrier both in vitro and in vivo, including S1P, forskolin, cAMP analogs, ROCK inhibitors, statins, and imatinib [[10], [11], [12],25,26]. In the current study, we applied t
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