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From The CriticsReviewer: Mark Kearley, PhD(Creighton University)
Description: This book is a good overview of the structure and inhibition strategies of those proteases which are associated with infectious diseases. Due to the tremendous effort of academic and industrial researchers, the area of protease inhibition is continually evolving but this book is an excellent review of the field up to 1998.
Purpose: The editor's goal is to use protease inhibition as a vehicle for illustrating how the drug discovery process has changed in the past decade. Modern technology now allows us to identify potential drug targets before they are isolated and their structures known. Thus the hunt for potential drugs can begin much sooner than in previous decades. Computer modeling is also a powerful tool for today's drug researchers.
Audience: The editor does not specify an intended audience, but this book would be useful for researchers involved in the field of protease inhibition, biochemists interested in proteases, and medicinal chemists. The writing in this book is quite advanced and thus is not recommended for undergraduates or even first or second year graduate students.
Features: In Chapters 1, 2, and 3, the same general formula is used for presentation: introduction, enzyme structure, substrate specificity, mechanism of action, and inhibitors. This strategy is very logical and makes for an easy read. For various reasons, the remaining chapters do not follow this formula and thus some of them are more difficult to read. Throughout the book, the figures are very helpful, especially those that are in color. In Chapter 1 the inhibition of the HIV protease which is one of the best success stories for this new method of drug discovery is described. However the chapter author does not fully develop the idea of drug discovery. The structures of many HIV protease inhibitors are given (13 pages) but there is not a lot of background information given about them. For example, Saquinavir is a substrate-based inhibitor by Hoffman-LaRoche. It is mentioned in the book for its unique decahydroisoquinoline moiety in the Pl region, but there is no mention of its evolution. Why was a decahydroisoquinoline moiety used? Were there any precursors to Saquinavir or was it a first generation drug? Were computers useful in the design of Saquinavir?
Assessment: This book is a fine overview of protease structure and inhibition. The early chapters are especially well-organized and easy to read, but the entire book is worthwhile. The editor attempts to provide an insight into the changes that have occurred in the field of drug discovery in the past ten years, but in this regard the book falls short.