4.Metabolomics used in the research of pediatrics.
Chinese Journal of Pediatrics 2010;48(6):442-445
Child
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Humans
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Metabolomics
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Pediatrics
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methods
7.Lead compound optimization strategy (2)--structure optimization strategy for reducing toxicity risks in drug design.
Hai-Long LIU ; Jiang WANG ; Dai-Zong LIN ; Hong LIU
Acta Pharmaceutica Sinica 2014;49(1):1-15
Idiosyncratic adverse drug reactions (IDR) induce severe medical complications or even death in patients. Alert structure in drugs can be metabolized as reactive metabolite (RM) in the bodies, which is one of the major factors to induce IDR. Structure modification and avoidance of alert structure in the drug candidates is an efficient method for reducing toxicity risks in drug design. This review briefly summarized the recent development of the methodologies for structure optimization strategy to reduce the toxicity risks of drug candidates. These methods include blocking metabolic site, altering metabolic pathway, reducing activity, bioisosterism, and prodrug.
Binding Sites
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Cytochrome P-450 Enzyme System
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metabolism
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Drug Design
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Drug Discovery
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methods
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Drug Recalls
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Drug-Related Side Effects and Adverse Reactions
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prevention & control
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Humans
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Structure-Activity Relationship
9.Ghrelin inhibit PAI-1 secretion induced by tumor necrosis factor-αvia p38MAPK in HepG2 cells
Liying DING ; Hong ZHAO ; Zhihong ZONG ; Jian LI ; Guoliang LIU
Journal of Chinese Physician 2008;10(3):327-329
Objective To investigate the effect of ghrelin on PAI-1 secretion in HepG2 cells induced by TNF-αand the effect of p-38 MAPK.Methods HepG2 cells were cultured.The concentration of TNF-α used to treat the HepG2 cells wag selected.The effect of ghrelin on PAI-1 secretion induced by TNF-α was detected by ELISA,the p-38 MAPK expression was investigated by Western blot.Results The concentration of PAI-1 was increased when cells were exposed to different concentration of TNF-α.The p-p38 MAPK expression was increased when the cells were exposed to TNF-α,ghrelin could inhibit the increase of PAI-1 secretioN induced by TNF-α.The expression of p-p38 MAPK was decreased when the cells were pretreated with ghrelin.Conclusion PAI-1 secretion were increased after TNF-α in-creasing.Ghrelin could inhibit PAI-1 secretion via p38 MAPK.