Activation of fungal silent gene clusters: A new avenue to drug discovery -- Total synthesis studies on macrocyclic pipecolic acid natural products: FK506, the antascomicins and rapamycin -- Application of natural product-inspired diversity-oriented synthesis to drug discovery -- Cheminformatics analysis of natural products: Lessons from nature inspiring the design of new drugs -- Chemical-genetic approaches for exploring the mode of action of natural products -- Epothilones as lead structures for new anticancer drugs - pharmacology, fermentation, and structure-activity-relationships -- Histone deacetylase inhibitors from microorganisms: the Astellas experience -- Ascomycete derivative to MS therapeutic: S1P receptor modulator FTY720 -- Artemisinin - an innovative cornerstone for anti-malaria therapy. The use of drug substances derived from plants, fungi, bacteria, and marine organisms has a long tradition in medicine. Together with their derivatives, and synthetic compounds deduced from natural product precursors, they represent a major part of today's pharmaceutical market. Within the fast developing discipline of molecular biology, natural products also play an important role as tool compounds in pathway screening and validation of target identification concepts. They provide innovative opportunities in drug discovery, leading to a detailed understanding of biological pathways and revealing the functions of involved enzymes or receptors. This book highlights new trends and aspects in natural products research. It discusses the biodiversity-driven approaches which are now of eminent importance in natural products research, addressing the question why natural products display such a complex chemical information, what makes them often unique and what their characteristics are. Practical questions such as supply of natural substances and production optimization strategies are also covered.