1.Methods for the evaluation of intestinal mucosal permeability.
Jing-Ting YAN ; Qi SUN ; Xiao-Li ZHANG ; Jing-Hua LIU ; Xiao-Yan FENG ; Jin-Xia ZHU
Acta Physiologica Sinica 2022;74(4):596-608
The intestinal mucosal barrier (IMB), which consists of mechanical barrier, chemical barrier, biological barrier and immune barrier, plays an important role in the maintenance of intestinal epithelium integrity and defense against invasion of bacteria, endotoxins and foreign antigens. Impaired IMB, characterized by increased intestinal mucosal permeability (IMP) and decreased transmembrane resistance (TR), has been implicated in the pathogenesis of various digestive, urinary, circulatory, neurological and metabolic dysfunctions. Electrophysiological recording of TR in the ex vivo intestinal tissues or cultured epithelial cell monolayers, or biochemical quantification of transepithelial movement of orally-administered molecular probes or specific endogenous protein molecules has frequently been used in the evaluation of IMB. In this paper, the composition and function of IMB will be summarized, with emphasis on the evaluation methods of IMP.
Cells, Cultured
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Inosine Monophosphate/metabolism*
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Intestinal Mucosa
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Permeability
2.The basic functions of inosine 5'-monophosphate dehydrogenase and its application in drug discovery.
You-Wen ZHANG ; Dan ZHANG ; Hua SUN
Acta Pharmaceutica Sinica 2014;49(3):285-292
Inosine 5'-monophosphate dehydrogenase (IMPDH) is a key enzyme of de novo GMP biosynthesis. The expression and activity of IMPDH can be affected by diseases and physiological process. It is the drug target for anticancer, antiviral, antimicrobial and immunosuppressive therapeutics. Not only catalytic action but the other biological functions of IMPDH also play an important role in diseases. The basic functions, mechanism of catalysis, classification of inhibitors, biological functions and the latest advances to IMPDH will be illustrated in this review. It is expected to be helpful to the discovery of new inhibitors and biological functions of IMPDH.
Animals
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Binding Sites
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Catalysis
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Drug Design
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Drug Discovery
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Enzyme Inhibitors
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classification
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pharmacology
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Humans
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IMP Dehydrogenase
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antagonists & inhibitors
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genetics
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metabolism
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Inosine Monophosphate
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metabolism
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Molecular Structure
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NAD
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metabolism
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Polymorphism, Genetic