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Protein Crystallography in Drug Discovery. (Series Methods and Principles in Medicinal Chemistry Vol. 20.). Edited by Robert E. Babine and Sherin S

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brings with it a new set of problems, but
one hopes that they are more survivable
than the last ones. Replacement of old
processes by new ones is common in
the chemical industry, and through
ingenuity we ensure a constant regeneration of our technological basis.
As a supplement to teaching, this
book is excellent. The authors have
taken care to give a summary at the
end of each chapter, as well as a list of
important concepts, and a selection of
exercises that well exemplify the material in the chapter. As a stand-alone
text, I would find this difficult unless
the class were specifically focused on
this part of industrial chemistry. The
technical production is rather simple.
There are no color graphics, and the
reaction schemes and figures are very
basic. There are a few typographical
issues, but what text is free of them?
Not surprisingly, given the background
of the authors, aspects of the pharmaceutical and fine-chemical process
industries are not covered. However,
industrial chemistry of the sort described here can provide many more colorful stories and spectacular examples of
how the principles of organic chemistry
lead to good manufacturing practices.
Who knows—perhaps another book is
in the offing? In any case, don$t wait,
Green and Wittcoff is a great book to
have on the shelf now.
Jay S. Siegel
Laboratorium fr Prozessforschung
Universitt Zrich
Zrich (Switzerland)
Protein Crystallography in Drug
(Series: Methods
and Principles in
Medicinal Chemistry, Vol. 20.). Edited
by Robert E. Babine
and Sherin S. AbdelMeguid. Wiley-VCH,
Weinheim 2004.
262 pp., hardcover
E 139.00.—ISBN
The determination of three-dimensional
structures is now an indispensable part
of any study of biological macromolecules, whether the aim is to understand
biological phenomena at the molecular
level or to develop drugs for controlling
such processes. The latter objective is an
increasingly important driving force for
industrially motivated biostructural
research, since the first introduction, in
the early 1980s, of a structure-based
drug: captopril, which inhibits the
enzyme ACE controlling blood pressure. Protein crystallography and NMR
spectroscopy have been used very successfully in “classical” areas of structure-based drug development, as exemplified by a number of HIV protease
inhibitors and by the anti-influenza
agent zanamivir. Furthermore, increasingly complex protein assemblies such
as the ribosome ortarget proteins identified in helth threats such as anthrax,
tuberculosis, or the SARS virus come
now into the focus of structure-based
drug-design programs. The editors of
Protein Crystallography in Drug Discovery have identified a gap in the literature
and set out to fill it: although there were
many recent monographs on protein
crystallography and others on the development of drugs in silico, there were
very few that dealt with the intersection
of these two by discussing specific methods and strategies of protein crystallography in drug design.
As the editors, Robert E. Babine
and Sherin S. Abdel-Meguid, acknowledge in their preface, this multi-author
book of limited size dealing with a wide
variety of topics, some of which are
very specialized, can only cover a part
of the field. Consequently, the work can
9 2004 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
be divided into two subject areas that
are treated to different extents.
The first group of chapters illustrates
the present situation in rational drug
design, by describing work in six target
areas: kinases, proteasomes, ribosomes,
cathepsin K, CDK4, and nuclear hormone receptors. These chapters are
mostly of a length and style typical of
concise, detailed, and informative
reviews. However, there are noticeable
differences in the authors$ viewpoints
regarding rational drug design, depending on whether their background is in
academic or industrial research. The
chapters on the design of drugs for ribosome and proteasome targets, which
have been written by academically oriented scientists, give only rather general
and superficial insights into their subjects (perhaps partly because of the
complexity of these large-molecule targets), whereas the contributions from
industrial researchers have a somewhat
different quality. In these, the authors
concentrate on describing in detail the
chemical and structural problems that
have arisen in different industrial drugdevelopment programs. It is mainly
from these chapters that the reader can
appreciate the enormous intellectual
and material resources that must be
mobilized to achieve breakthroughs by
rational drug design in industry.
Unfortunately, the second part the
book, which is concerned with methods,
does not fulfill the expectations raised
by the first part, especially since it occupies only a third of the whole work.
Although the chapters on the co-crystallization of serin proteases with ecotin,
and on the construction of orthogonal
receptor–ligand pairs, are certainly
very interesting, the rest of the contributions (on structural genomics, microcrystallization, and crystallization by
mutagensis) do not provide very rewarding reading, as the choice is unbalanced,
and some of them contain little
hard information. This part especially
confirms the editors$ comment at the
beginning that the choice of articles
was determined by the availability of
Another unsatisfactory aspect of the
book as a whole is the variation from
chapter to chapter in the quality and
clarity of the structural formulas, which
could have been avoided by some editoAngew. Chem. Int. Ed. 2004, 43, 6407 – 6409
rial work. Also, the book could have
been improved by including two or
three introductory chapters to give readers with only limited previous knowledge some understanding of the nature
and strategies of protein crystallography
Angew. Chem. Int. Ed. 2004, 43, 6407 – 6409
in pharmaceutical research. However,
parts of the book will certainly be very
useful for specialists in the area of structure-based drug design, provided that
they do not expect to find here a more
method-orientated collection of articles.
Lars-Oliver Essen
Fachbereich Chemie
Philipps-Universitt Marburg (Germany)
DOI: 10.1002/anie.200485156
9 2004 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
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discovery, medicina, crystallographic, series, method, roberts, babine, chemistry, drug, protein, edited, sherin, vol, principles
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