Title: Purine nucleoside phosphorylases as targets for transition-state analog design
Abstract: Among the most powerful enzyme-targeted drugs are those that bear a strong resemblance to the transition state of the chemical reaction undergoing catalysis. This chapter illustrates that experimental determination of enzymatic transition-state structure permits chemically stable analogs to be designed. Mimics of these transition states exhibit binding affinities exceeding those of the substrates by factors of greater than 106. To appreciate this approach to drug design, it is necessary to understand the nature of transition-state formation and how it relates to the strong binding interactions between enzymes and transition-state analogs.
Publication Year: 2010
Publication Date: 2010-05-31
Language: en
Type: book-chapter
Indexed In: ['crossref']
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Cited By Count: 4
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