Specific enzyme-induced decapsulation

Little difficulty exists in finding chemotherapeutic agents that kill pathological cells; the problem lies in identifying agents that do so without damaging normal cells as well. One possible route to selectivity plays on the fact that certain pathological cells produce excessive amounts of a partic...

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Bibliographic Details
Published inJournal of the American Chemical Society Vol. 113; no. 14; pp. 5467 - 5468
Main Authors Menger, F. M, Johnston, D. E
Format Journal Article
LanguageEnglish
Published Washington, DC American Chemical Society 01.07.1991
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Summary:Little difficulty exists in finding chemotherapeutic agents that kill pathological cells; the problem lies in identifying agents that do so without damaging normal cells as well. One possible route to selectivity plays on the fact that certain pathological cells produce excessive amounts of a particular enzyme (e.g., bone cancer/alkaline phosphatase, neuroblastoma/acetylcholinesterase). If such an enzyme is capable of breaking open specially designed vesicles that encapsulate a cytotoxic drug, then selective therapeutic activity toward the enzyme-exuding cell can be achieved. We describe herein compound I which, in concert with acetylcholinesterase (AcE), models the above process.
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ObjectType-Article-1
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ISSN:0002-7863
1520-5126
DOI:10.1021/ja00014a056