Über die Autorinnen und Autoren

Olga Genilloud obtained her Ph.D. in Chemistry (Biochemistry and Molecular Genetics) in 1988 from the Universidad Complutense de Madrid, Spain. After a short stay at the Microbiology Department at Harvard Medical School in Boston, in 1989 she joined the Centro de Investigacion Basica de Espana (CIBE), at Merck Sharp and Dohme in Spain, where she has led for nineteen years the discovery of bacterial natural products as new leads for drug development. In February 2009 she was appointed Scientific Director of Fundacion MEDINA. She is a member of many different scientific societies and has extensive experience in the coordination and management of international scientific working groups and is actively contributing to different Master and Pre-doctoral teaching programs. M¬ Francisca Vicente has a Ph.D. in Biology and Molecular Genetics (1986, Universidad Autonoma de Madrid) and more than 10 years experience in R&D, managing teams and working in the multidisciplinary environment of multinational pharmacy (Merck Sharp and Dohme, Spain) and other research centres (Institute Pasteur, and Hospital Necker, France). She has been in charge of the design, implementation, and supervision of many R&D projects. She is experienced in identifying and managing the economic resources for developing new scientific and technological projects. She has coordinated and managed national and international research groups. Her teaching experience was gained by giving practical and theoretical classes in different masters and university programs. In February 2009, she joined the Fundacion MEDINA as Area Head of the Screening and Target Validation Department.

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This book offers an integrated review of recent trends in natural products drug discovery and the key lead candidates that are outstanding for their chemistry and biology as a starting point in novel drug development. The editors focus on different trends that have and will continue to have a major impact on the multiple stages of modern drug discovery mainly from NPs that have not been included in other works. This is complemented by a series of case studies written by leading experts from industry and academia on key molecules and their derivatives that have been chosen for their novelty in chemistry, biology and clinical applications. The book demonstrates the current confluence of different disciplines in chemical biology and synthetic chemistry supported by a more profound knowledge of systems biology that ensures the concurrency and synergisms of expertise from different research fields that impact in the discovery of novel molecules. In the first section the chapters reflect recent approaches to exploit the biosynthetic potential of microbial resources (including genome mining, metagenomic and epigenetic approaches), as well as biosynthetic chemistry tools to respond to product supply and novel screening alternatives that have lead to the discovery of novel chemistry. The second part reviews, in the form of case studies, some examples of bioactive molecules in the important therapeutic areas of antiinfectives, oncology and antiparasitics. The editors have attained more than twenty years experience in drug discovery from microbial natural products in the large pharma environment and can present from their perspective a dynamic area of research in constant evolution. The book will be essential reading for pharmaceutical scientists in industry and academia, medicinal chemists, pharmacologists and microbiologists.

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Drug Discovery from Natural Products

The Royal Society of Chemistry

Contents

Section 1 New Approaches to Exploit Natural Products Chemistry, 
1.1 Semisynthesis/Synthesis de novo of Natural Products to Cope with Supply Issues, 
Chapter 1 Semisynthesis Approach of Ecteinascidin 743 (ET-743, Yondelis®) Carmen Cuevas and Andrés Francesch, 5, 
Chapter 2 Chondramides and Chivosazoles – Two Metabolites Which Interfere with the Actin Cytoskeleton Lynette A. Smyth, Tobias Brodmann and Markus Kalesse, 17, 
Chapter 3 Class III Lantibiotics – an Emerging Family of Thioether-Containing Peptides Bartlomiej Krawczyk, Joanna M. Krawczyk and Roderich D. Süssmuth, 42, 
Chapter 4 Mutant Manufacturers Andreas Kirschning, Simone Eichner, Jekatherina Hermane and Tobias Knobloch, 58, 
Chapter 5 Progress in Enhancing the Neurotrophic Effects of Natural FKBP Ligands Guy T. Carter, 79, 
1.2 Engineering Natural Product Synthetic Pathways and Genome Mining, 
Chapter 6 Biosynthesis of Indolocarbazole Alkaloids and Generation of Novel Derivatives by Combinatorial Biosynthesis Carmen Méndez, Francisco Moris and José A. Salas, 99, 
Chapter 7 New Lantibiotics from Natural and Engineered Strains Sonia I. Maffioli, Paolo Monciardini, Margherita Sosio and Stefano Donadio, 116, 
Chapter 8 Mining Microbial Genomes for Metabolic Products of Cryptic Pathways D. Oves-Costales and G. L. Challis, 140, 
Chapter 9 Mining Cyanobacterial Genomes for Drug-Like and Bioactive Natural Products John A. Kalaitzis and Brett A. Neilan, 159, 
Chapter 10 Epigenetic Approaches to Natural Product Synthesis in Fungi Alexandra A. Soukup and Nancy P. Keller, 198, 
Section 2 New Methodologies and Screening Technologies for the Exploitation of Microbial Resources, 
Chapter 11 Novel Approaches to Exploit Natural Products from Microbial Resources Olga Genilloud and Francisca Vicente, 221, 
Chapter 12 Discovery and Development of Platensimycin and Platencin Sheo Singh, 249, 
Chapter 13 Coupling Chemical Genomics and Natural Products: The Discovery of Parnafungins and Novel Antifungal Leads Hao Wang, Craig A. Parish, Deming Xu and Terry Roemer, 278, 
Section 3 Novel Microbial Natural Products and Derivatives, 
Chapter 14 Natural Products: New Agents against MDR Tuberculosis Ujjini Manjunatha, Fumiaki Yokokawa, Meera Gurumurthy and Thomas Dick, 307, 
Chapter 15 Retapamulin: a First-in-Class Pleuromutilin Antibiotic Rodger Novak, 326, 
Chapter 16 Epothilones as Lead Structures for New Anticancer Drugs Bernhard Pfeiffer, Fabienne Zdenka Gaugaz, Raphael Schiess and Karl-Heinz Altmann, 339, 
Chapter 17 The Contribution of Marine Chemistry in the Field of Antimalarial Research Ernesto Fattorusso and Orazio Taglialatela-Scafati, 374, 
Future Challenges, 391, 
Subject Index, 394,