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Lipases and Phospholipases in Drug Development: From Biochemistry to Molecular Pharmacology

Gunter Muller (Editor), Stefan Petry (Editor)
ISBN: 978-3-527-60570-5
354 pages
March 2006
Lipases and Phospholipases in Drug Development: From Biochemistry to Molecular Pharmacology (3527605703) cover image


Lipases and Phospholipases are key control elements in mammalian metabolism. They share many common features that set them apart from other metabolic enzyme classes, most importantly their association with biological membranes. Their potential as drug targets for the treatment of metabolic diseases is widely recognized, and the first lipase inhibitor drugs have been successfully introduced.
Providing drug developers with a firm foundation for lipase-centered drug design, the editors of this volume have assembled experts from different scientific disciplines to create a comprehensive handbook for all pharmaceutical chemists, biochemists and physiologists working with lipases.
The authors examine fundamental aspects of lipase function in vitro and in vivo, explaining how this knowledge may be used to develop lipase assays. They also treat the physiological roles of lipases in normal and disordered metabolism, as well as strategies to target lipases for the treatment of diabetes, obesity and related disorders. Additional topics include the application of phospholipases for liposome-based drug delivery and their use as diagnostic tools.
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Table of Contents


List of Contributors.

1. Purification of Lipase (P. Vasudevan).

2. Phospholipase A1: Structures, Physiological and Patho-physiological Roles in Mammals (K. Inoue, et al.).

3. Rational Design of a Liposomal Drug Delivery System Based on Biophysical Studies of Phospholipase A2 Activity on Model Lipid Membranes (K.Jorgensen, et al.).

4. Phospholipase D (J. Exton).

5. Sphingomyelinases and Their Interaction with Membrane Lipids (F. Goñi & A. Alonso).

6. Glycosyl-phosphatidylinositol Cleavage Products in Signal Transduction (Y. León & I. Varela-Nieto).

7. High-throughput Screening of Hormone-sensitive Lipase and Subsequent Computer-assisted Compound Optimization (S. Petry, et al.).

8. Endothelial Lipase: A Novel Drug Target for HDL and Atherosclerosis? (K. Badellino, et al.).

9. Digestive Lipases Inhibition: an In vitro Study (A. Tiss, et al.).

10. Physiology of Gastrointestinal Lipolysis and Therapeutical Use of Lipases and Digestive Lipase Inhibitors (H. Lengsfeld, et al.).

11. Physiological and Pharmacological Regulation of Triacylglycerol Storage and Mobilization (G. Müller).

Subject Index.

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Author Information

Günter Müller is senior scientist for Biochemistry at Aventis Pharma Germany, Frankfurt am Main, and honorary lecturer for genetics at the University of Munich. He was born in Peissenberg (Germany) and studied anthropology, zoology, genetics and biochemistry at the Ludwig-Maximilians-University in Munich, finishing his PhD thesis under the supervision of R. Zimmermann in 1987. After post-doctoral fellowships at the universities of Ulm and Heidelberg, he joined the pharmaceutical industry in 1990 and received his habilitation at the University of Munich in 1996. He is interested in molecular mechanisms in both lower eukaryotes and mammalian cells, and their use as drug targets for metabolic disorder.

Stefan Petry is senior scientist in Medicinal Chemistry at Aventis Germany, Frankfurt am Main. He was born in Kaiserslautern (Germany) and studied Chemistry and Biochemistry at the Albert-Ludwigs-University in Freiburg, including his PhD thesis under the supervision of Jochen Lehmann on photo-affinity labeling of carbohydrate binding proteins. He joined the pharmaceutical industry in 1994. At Aventis he is responsible for projects in the field of diabetes. In particular, he is interested in the development of small molecules which interact with signal transduction processes or influence lipid metabolism.

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Buchkurzvorstellung mit farbigem Cover in:

GIT Laborfachzeitschrift August 2004
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