C.G. Wermuth, N. Koga, H. Koning,
and B.M. Metcalf, eds.
Blackwell Science, 1992 [ISBN 0-632-03408-4]
A timely volume devoted to articles on the design and
development of new chemical molecules for the treatment, cure or prevention
of human and animal diseases. It is recognized that three critical stages
govern the development of new drugs: the improvement of the compound
in terms of potency, selectivity and safety; and the adaptation of the
molecules to its clinical use. This book looks in detail at theses three
stages concentrating on the quest for new lead discovery in Part 1.
Protein structure - function relationships are outlined in Part 2, which
deals with cloning and structural studies on receptors and enzymes,
detection of new enzymes and receptors by hybridization techniques,
and signal transduction and mechanisms. Knowledge of protein structure
and mechanism of signal transduction are an absolute requisite for medicinal
chemists dealing with drug design. Part 3 covers structure - activity
relationships dealing with pharmacophore mimickry modelling, design
and peptidomimetics, and optimization. Finally, Part 4 is devoted to
chemical formulation and to specific administration devices in order
to ascertain optimal bioavailability of the active molecules and to
render them chemically efficient.
Contents
Past Approaches to Discovering New Drugs; Reflections
and Perspectives; Trends In New Lead Identification: A Structural Approach;
From Membrane to Genomic Pharmacology or from Short-Term to Long-Term
Effects; Future Applications of Oligonucleotides in Antiviral and Antitumoral
Chemotherapy; Molecular Biology of Drug Receptors and the Advent of
Reverse Pharmacoly; A Structural Basis for Proteinase-Protein Inhibitor
Interaction; New Approaches to Isolation, Expression and Molecular Modelling
of Proteases; New Era of Biochemistry: Cytokine Signal Network and its
Implication for Biomedical Research; Molecular Mechanisms of Regulatory
Signal Transduction; Molecular Diversity of Signal Transduction Systems:
A Puzzle for Pharmacologists of Today and Tomorrow; The Future of Computer-Aided
Drug Design; Pharmacophore Identification Based on Molecular Electrostatic
Potentials (MEPS); New Rational Approaches for Structure-Activity Relationships
and Drugs Design; Rational Design of Peptidomimetics: Structural and
Pharmacological Aspects; Non-Peptide Ligands for Peptide Receptors;
Peptidometic Research, Design and Synthesis; Peptidomimetics as Tools
for the Initiation and Analysis of Peptide and Protein Secondary Structure:
the Prospects for Unnatural Proteins by Design; On the Future QSAR;
Computer-Assisted Drug Design in the 21st Century; Trends in Design
of Prodrugs for Improved Drug Delivery; Antibody-Based Drug Targeting
Approaches: Perspectives and Challenges; Novel Drug-Delivery Systems;
Lipid Microsphere Preparations and Lecithinized Peptides For Drug-Delivery
Systems.