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Book Reviews Aspartic Proteinases. Physiology and Pathology. By M. Fusek and V. Vetvicka. CRC Press, Inc., Boca Raton, FL. 1995. xii + 308 pp. 16 × 24 cm. ISBN 0-8493-7660-2. $179.95. This book provides a summary of information of research on aspartic proteinases and focuses primarily on important members of these enzymes which impact human physiology. It does not cover enzyme methodology but rather seeks to address in specific details the issues of human physiology (including localization, physiological syntheses, secretion, post-translational activation, and activation of zymogens) and human pathology (regulation of expression in normal and pathophysiological states). It is not necessarily a comprehensive theses but rather serves as a concise introduction and review for readers without preliminary knowledge of the field. It provides extensive primary references, including publications to early 1995. After a brief introductory chapter which discusses the classification of proteinases, a long chapter is devoted to the overview of structures and functions of aspartic proteinases. For the discussion on structures, sequences and references for known members (including names, species, tissue localization, and sequence alignment) are provided, together with a discussion on the evolution of these enzymes and their secondary and tertiary structures as derived from the primary sequences. Crystal structures and active site topology are discussed as known. For the discussion on function, the characteristic properties of these enzymes together with the catalytic mechanism and the specificity and subsite preferences are elaborated. The effects by natural protein and low molecular weight inhibitors are also briefly presented. Chapters III-IX then seek to describe seven different groups of aspartic proteinases in individual chapters: pepsin A and gastricsin (as important enzymes for food digestion), renin (as a rate-limiting protease in the renin-angiotensin cascade and its importance in the consideration of treatment of hypertension), cathepsin D (as an intracellular proteinase localized in the lysosomes for protein catabolism), cathepsin E (as often found within endoplasmic reticulum and least well characterized), aspartic proteinases of Candida yeasts (in these opportunistic pathogens which are the major cause of fungal infections in immunocompromised patients), aspartic proteinases of Plasmodium falciparum (as required in the nutritional need of the malarial parasites), and HIV and retroviral proteinases (as indispensible enzymes for viral maturation and infection). The pharmacology of enzyme inhibition and the clinical potential are well described particularly for renin and HIV protease. The book covers the subject of enzyme inhibitors, including renin inhibitors and HIV protease inhibitors, only very superficially. The focus of the book is primarily on introduction to research status and understanding of physiology and pathology. Diagrams and illustrations (especially enzyme structures) are not of very high quality. At $179.95, the book is rather expensive, although it would
serve as a good introduction to aspartic proteinases and many members with important human physiology. Suvit Thaisrivongs Pharmacia & Upjohn, Inc. Structural, Analytical and Medicinal Chemistry Kalamazoo, Michigan 49001 JM960185D S0022-2623(96)00185-9
Cardiovascular Regulation. Edited by David Jordan and Janice Marshall. Portland Press, London. 1995. ix + 159 pp. 19 × 25 cm. ISBN 1-85578-024-0. $35.00. This book is divided into eight chapters ranging in length from 14 to 24 pages. The chapter titles are Central Nervous Integration of Cardiovascular Regulation, Aspects of the Integration of the Respiratory and Cardiovascular Systems, Cardiovascular Changes Associated with Behavioural Alerting, Cardiovascular Changes Associated with Sleep, Regulation of Blood Volume, Cardiovascular Responses to Exercise: Central and Reflex Contribution, Metabolic Control of Blood Flow with Reference to Heart, Skeletal Muscle and Brain, and Changing Perspectives on Microvascular Fluid Exchange. Many of the chapters of this book delve into areas that are infrequently reviewed in “standard” references on cardiovascular medicine. For instance, an entire chapter on behavioral alerting describes in detail the cardiovascular responses that occur following stress. Descriptions of the changes in blood pressure, heart rate, etc. that occur following a stress (e.g., mental arithmetic) and the mechanisms of these changes are discussed. Also, a chapter is devoted to describing the complex cardiovascular adaptations that occur during the different phases of sleep. Another chapter discusses the various mechanisms by which fluid turnover occurs and the importance of fluid turnover on cardiovascular responses and regulation as well as the methodology used for measuring fluid pressures in different tissues. This multiauthored book is well written, and appropriate, up to date references are used. The abundant use of relevant figures and tables adds to the high quality of this text. This book is not limited to human only studies; appropriate cardiovascular studies in animals are included as well. This book is recommended for any researcher interested in the intricate mechanisms involved in the regulation of cardiovascular function.
Dennis M. Ackerman Solvay Pharmaceuticals 901 Sawyer Road Marietta, Georgia 30062 JM9601866 S0022-2623(96)00185-0
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Book Reviews
Free Radicals in Organic Chemistry. By Jacques Fossey, Daniel Lefort, and Janine Sorba. John Wiley & Sons, Inc., New York. 1995. xiv + 307 pp. 16 × 24 cm. ISBN 0-471-95496-9. $39.95 (pbk).
Lithium Chemistry: A Theoretical and Experimental Overview assumes a graduate level background in quantum and experimental physical chemistry. It provides a useful guide to lithium studies for graduate students and researchers in the fields of organic, inorganic, and organometallic chemistry.
This is an English translation of Les radicaux libres en chimie organique which was originally published in French in 1993. It provides a complete summary of free radical chemistry in four major sections: (I) General Concepts and Basic Principles, (II) Reactions: Classifications and Mechanisms, (III) Applications in Synthesis, and (IV) References and Tables, which are comprised of 26 chapters. Chapter 16, “Free Radicals in Biochemistry” reviews important radical reactions involved in biological processes and energy production and will be of particular interest to medicinal chemists. Chapter 25 “References” provides sources of general reviews of the major topics in free radical organic chemistry. This book is intended primarily for organic chemistry students; it provides an introduction to the structure, formation, and reactivity of free radicals, examples of organic reaction pathways involving free radicals, descriptions of recent developments in the field, and an overview of the many applications of free radicals in organic chemistry. In summary, it is a useful text for teaching this area of chemistry which continues to develop rapidly. Staff JM9602625 S0022-2623(96)00262-2
Lithium Chemistry. A Theoretical and Experimental Overview. Edited by Anne-Marie Sapse and Paul von Rague´ Schleyer. John Wiley & Sons, Inc., New York. 1995. x + 595 pp. 16 × 24 cm. ISBN 0-47154930-4. $69.95. The chemistry of lithium, the lightest and least reactive of the alkali metals, is somewhat unique. Anomalous properties of lithium include the lithium bond (similar to the hydrogen bond), formation of aggregates, and complexation by crown ethers. This book reviews the field of lithium chemistry in 11 chapters: (1) Bonding, Structures and Energies in Organolithium Compounds; (2) Theoretical Studies of Aggregates of Lithium Compounds; (3) Comparison of Lithium and Hydrogen Bonds; (4) Lithium Atom Matrix Reactions with Small Molecules; (5) NMR of Organolithium Compounds; (6) Aspects of Thermochemistry of Lithium Compounds; (7) From “Carbanions” to Carbenoids: The Structure of Lithiated Amines and Lithiated Ethers: (8) Complexes of Inorganic Lithium Salts; (9) Structures of Lithium Salts of Heteroatom Compounds; (10) Synthetic Ionophores for Lithium Ions; and (11) Preparation and Reactions of Polylithiumorganic Compounds. Extensive references follow each chapter, and the book concludes with a thorough index. Thus, a complete, useful, and up-to-date overview of current theories and experimental data relating to lithium chemistry is provided.
Staff JM960263X S0022-2623(96)00263-4
Antisense Therapeutics. Edited by Sudhir Agrawal. Humana Press, Totowa, NJ. 1996. xiv + 276 pp. 16 × 23.5 cm. ISBN 0-89603-305-8. $99.50. Antisense Therapeutics is the latest volume of the Methods in Molecular Medicine series. It reviews recent discoveries in the field of antisense oligonucleotide therapeutics and the effects of these agents in a variety of in vivo paradigms. The antisense nucleic acids inhibit gene expression in a sequence specific manner by hybridizing to a target gene through Watson-Crick base pairing and thus inhibiting the expression of diseaserelated genes. Thus, these oligonucleotides possess equisite specificity and affinity which are so important in drug therapy. In this book major contributors to antisense therapeutics research describe their findings ranging from design to synthesis to biology and in vivo applications in 14 chapters. Included among the topics reviewed are (1) antisense therapeutics in viral infections, (2) efficacy in animal models, (3) delivery across the blood-brain barrier, (4) methods of administration, (5) arresting tumor growth in nude mice, and (6) antisense oligonucleotides in cardiovascular diseases. The references following each chapter are appropriate and timely; the subject index is comprehensive. The up-to-date account of research with antisense nucleotides provided by this book enables an appreciation of the exciting possibilities this field offers for the development of new uniquely selective therapeutic agents via precisely designed inhibitors of the expression of disease-associated genes. Staff JM960264P S0022-2623(96)00264-6
Studies in Natural Products Chemistry. Volume 16. Stereoselective Synthesis (Part J). Edited by Atta-ur-Rahman. Elsevier, Amsterdam. 1995. xiv + 757 pp. ISBN 0-444-82264-X. $435.00. In a worthy extension of the excellent series of volumes on the synthesis of natural products, the present compendium includes 15 chapters covering a variety of important and interesting topics. Subject matters (and authors) are as follows: synthesis of the antibiotics actinobolin and bactolin (S. M. Weinreb); synthesis of (()-fredericamycin A (D. L. J. Clive et al.); synthesis and transformation of siastatin B (Y. Nishimura); use of cylic monoterpenoids in natural products synthesis (T. Money and M. K. C. Wong); synthesis of
Book Reviews
Journal of Medicinal Chemistry, 1996, Vol. 39, No. 13 2627
iridoids and related products (S. Isoe); synthesis of brassinosteroids (T. G. Back); organopalladium approaches to prostaglandins (R. C. Larock); transition metal organometallics in the synthesis of amino acids (G. R. Stephenson); palladium-mediated synthesis of alkaloids (J.-E. Ba¨ckvall and D. Tanner); recent progress in the synthesis of piperidine and indolizidine alkaloids (S. R. Angle and J. G. Breitenbucher); recent developments in aporphine synthesis (O. Hoshino); reactions of 1,4-benzoquinones with styrenyl systemsssynthesis of neolignans, pterocarpans, and benzofurans (T. A. Engler); biogenesis-like transformation of 4-substituted phenols by photooxygenation (K. Endo); furan in the synthesis of natural products (J. Raczko and J. Jurczak); enantiomerically pure γ-butyrolactones in natural products synthesis (S. S. C. Koch and A. R. Chamberlin); and fluoro β-lactamsssynthesis and application in asymmetric synthesis (J. T. Welch and R. Kawecki).
book particularly enjoyable to read. Merrifield provides a list of linkers (for peptide acids and amides) cleavable by acidic and nonacidic reagents. In addition, there is a table on solid-phase orthogonal schemes which I found to be a valuable source of information. Chapter 2 discusses in detail various coupling agents (including the more recent ones such as HATU) and also gives an account of strategies to form multiple disulfide bonds in peptides with examples (conotoxins and endothelin). Chapter 4 details the helical propensities of various amino acids and specific interactions that can stabilize helical conformations in peptides. In Chapter 5, the approaches to obtaining a reasonable starting model of the biologically active conformation of a peptide are detailed with examples (gramicidinA, cyclosporinA, somatostatin, and Angiotensin II). In Chapter 6, the benefits of imposing local and global conformational constraints with examples (CCK, oxytocin, glucagon, LHRH, somatostatin, angiotensin, R-melanotropin, and δ-opioid peptides) where this approach has proven valuable are discussed. Chapter 7 will be of interest to medicinal chemists involved in designing nonpeptide ligands for peptide receptors. Inhibitors of Serine proteinases obtained from natural sources, from semisynthetic methods, and from genetic engineering methods are described in Chapter 8. Design of helical bundles, β sheets and sequence-specific DNA-binding polypeptides is the subject of Chapter 9. Excellent illustrations to the power of combinatorial libraries in identifying enzyme inhibitors, antiviral compounds, antimicrobial peptides, and the concept of libraries from libraries are presented in Chapter 10. The nature of T- and B-cell epitopes and cross-reactivity studies between proteins and peptides using antipeptide and antiprotein antibodies are the subjects of Chapter 11. In the last chapter, Tam elaborates on the design and synthesis of multiple antigen peptides and applications of these in vaccines, immunoassays, epitope mapping, and serodiagnosis. Each chapter is well-referenced, and the book ends with a subject index. Valuable information is provided at a reasonable price. There are plenty of illustrations and tables throughout. This issue is a welcome addition to the libraries of all those involved in the synthetic, biophysical, and biological aspects of peptide chemistry.
Maurice Shamma Department of Chemistry The Pennsylvania State University University Park, Pennsylvania 16802 JM960265H S0022-2623(96)00265-8
Peptides: Synthesis, Structures and Applications. Edited by Bernd Gutte. Academic Press, San Diego, CA. 1995. xiv + 511 pp. 16 × 23.5 cm. ISBN 0-12-310920-5. $69.95. This book is a compilation of 12 chapters written by various experts on a variety of topics in peptide science ranging from synthetic methodologies in peptide chemistry, conformational aspects, peptide vaccines, and structure-activity relationships to combinatorial peptide libraries. The individual chapters are entitled (1) The History of Peptide Chemistry (by Theodor Wieland); (2) Amide Formation, Deprotection, and Disulfide Formation in Peptide Synthesis (by Yoshiaki Kiso and Haruaki Yajima); (3) Solid-Phase Peptide Synthesis (by Bruce Merrifield); (4) R-Helix Formation by Peptides in Water (by J. Martin Scholtz and Robert L. Baldwin); (5) Peptide Conformation: Stability and Dynamics (by Garland Marshall, Denise D. Beusen, and Gregory Nikiforovich); (6) Structure-Function Studies of Peptide Hormones: An Overview (by Vector J. Hruby and Dinesh Patel); (7) Neuropeptides: Peptide and Nonpeptide Analogs (Andrzej W. Lipkowski and Daniel B. Carr); (8) Reversible Inhibitors of Serine Proteinases (by Herbert R. Wenzel and Harald Tschesche); (9) Design of Polypeptides (by Bernd Gutte and Stephan Klauser); (10) Soluble Chemical Combinatorial Libraries: Current Capabilities and Future Possibilities (by Richard A. Houghten); (11) Epitope Mapping with Peptides (by Hans Rudolf Bosshard); and (12) Synthesis and Applications of Branched Peptides in Immunological Methods and Vaccines (by James P. Tam). The chapters are of uniformly high quality and are of current interest. The historical perspectives on the evolution of peptide chemistry as a science by Theodor Wieland (Chapter 1), and on the solid-phase synthesis (Chapter 3) by its inventor Bruce Merrifield, make the
Ram Dharanipragada Hoechst Marion Roussel, Inc. 2110 E. Galbraith Road Cincinnati, Ohio 45215 JM960266+ S0022-2623(96)00266-X
Technology Transfer. Making the most of your intellectual property. By Neil F. Sullivan. Cambridge University Press, Cambridge, England. 1995. 15 × 23 cm. xiv + 221 pp. ISBN 0-521-46616-4. $24.95 (pbk). This book is intended to aid scientists in evaluating the commercial potential of their research and to guide them toward marketing their discoveries. In providing a step-by-step guide to the commercialization of research, it addresses protection of the intellectual prop-
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Journal of Medicinal Chemistry, 1996, Vol. 39, No. 13
Book Reviews
erty, commercial development via licensing and business initiation, and financing and managing a new company. Each step in the process from discovery to marketing through a private company is considered in detail with a multitude of practical considerations. Appendices define some commonly used business terms, provide addresses useful for company information and start up and sources of marketing advice, and list references to additional reading. The addresses provided are restricted to Europe. Technology Transfer is recommended reading for scientists having research with potential commercial application. Although a small book such as this could not possibly consider all circumstances in such a broad undertaking, it does provide a perspective on relevant parameters.
Annual Review of Neuroscience. Volume 19, 1996. Edited by W. Maxwell Cowan. Annual Reviews, Inc., Palto Alto, CA. 1996. ix + 644 pp. 16 × 23 cm. ISBN 0-8243-2419-6. $52.00.
Staff JM960334S S0022-2623(96)00334-2
Books of Interest Methods in Molecular Biology. Volume 59. Protein Purification Protocols. Edited by Shawn Doonan. The Humana Press, Totowa, NJ. 1996. x + 405 pp. 16.5 × 23 cm. ISBN 0-89603-336-8. $64.50 (pbk).
Encyclopedia of Common Natural Ingredients Used in Food, Drugs, and Cosmetics. Second Edition. By Albert Y. Leung and Steven Foster. John Wiley & Sons, Inc., New York. 1996. xxxv + 649 pp. 18.5 × 26.5 cm. ISBN 0-471-50826-8. $150.00. JM960261C S0022-2623(96)00261-0
Human Cell Culture Protocols. (Methods in Molecular Medicine). Edited by Gareth E. Jones. Humana Press, Inc., Totowa, NJ. 1996. xiv + 545 pp. 16 × 23.5 cm. ISBN 0-89603-335-X. $79.50. WHO Model Prescribing Information. Drugs Used in Sexually Transmitted Diseases and HIV Infection. World Health Organization, Geneva, Switzerland. 1995. 97 pp. 14.5 × 21 cm. ISBN 92-4140105-2. $22.50. JM9603330 S0022-2623(96)00333-0
