2.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
8.Construction and application of storehouse for medical camp in emergency support brigade
Jiming ZHANG ; Cunhe LIN ; Ling WANG ; Hai YU ; Leihan LIU
Chinese Medical Equipment Journal 2004;0(09):-
The framed storehouse and the open rolling shutter door equipment are designed and manufactured for the infrastructure construction.The multipurpose and moved frame operating platform is designed and manufactured according to the demands of loading and unloading as a whole for part medical equipments.In this way,the shortage of the storehouse space is solved and the usual training and moving become easier.
9.Nuclear Factor Kappa B and Liver Injury
Hai LIN ; Zexin LI ; Jiangwei LIU ; Yongjiu ZHANG
Chinese Journal of Bases and Clinics in General Surgery 2003;0(06):-
Objective To summarize the role of nuclear factor kappa B(NF-?B) in the occurrence and progression of various sorts of liver injury.Methods Literatures on the structures,property of molecular biology and function of NF-?B,as well as its relationships with liver injury were collected and reviewed.Results NF-?B was an important nuclear factor existed in cells widely distributed in most cell types.The activation of NF-?B was induced by various sorts of liver injury.The activated NF-?B could affect the liver injury by regulating cytokines,adhesion molecules,and activating factor involving in immunologic reaction,inflammatory reaction and the apoptosis.Conclusion NF-?B plays an important role during the occurrence and progression of liver injury,and may become a new target in the treatment of liver injury.
10.Efficacy and safety of cladribine in treatment of patients with refractory/relapsed acute myeloid leukemia
Lijuan RU ; Hai LIN ; Yehui TAN ; Yanping YANG ; Shanshan LIU ; Xiangui LIU ; Wenjing LIU ; Sujun GAO
Journal of Leukemia & Lymphoma 2016;25(12):739-742
Objective To investigate the efficacy and safety of cladribine in the treatment of patients with refractory/relapsed acute myeloid leukemia (AML). Methods The data of 8 patients with refractory/relapsed AML treated with regimens containing cladribine at a dose of 5 mg/m2 per day for 5 consecutive days were retrospectively analyzed. The efficacy and adverse reactions were observed during treatment. Results Among the 8 patients, 5 patients achieved complete remission (CR), 1 patient achieved partial response (PR), and 2 patients obtained non remission (NR). The adverse reactions could be tolerated. Conclusion Regimen containing cladribine is an effective treatment procedure for the patients with refractory/relapsed AML, and its adverse reactions can be tolerated, which requires further clinical study.