Design of Enzyme Inhibitors highlights how, what, and where enzymes have become critical in pharmaceutical and biotechnology research. This book provides an overview of new developments in enzyme technology and case studies of new enzyme inhibitor drugs. This text discusses enzymatic assays, including emerging assay technologies for key enzyme classes in pharmaceutical research. In addition to new developments in proteomics, this book includes two emerging technologies in Life Sciences, metabolomics and preclinomics. This volume reviews important progress on the chemical biology of enzymes in the post-genomic era.
HSIU-CHIUNG YANG, PhD, is Research Advisor at Eli Lilly and Company. She is the author or coauthor of over forty publications and holder of two patents.
WU-KUANG YEH, PhD, is Adjunct Professor at Indiana University Purdue University Indianapolis (IUPUI), and was Director of Research and Principal Investigator at PreClinOmics, Inc. The holder of six U.S. patents, Dr. Yeh is the author or coauthor of over 115 publications.
JAMES R. McCARTHY, PhD, is Research Professor in the department of chemistry and chemical biology at Indiana University Purdue University Indianapolis (IUPUI), and was a Distinguished Research Fellow at Eli Lilly and Company. He is the author or coauthor of over 130 publications and holder of over sixty patents.
A. Enzymes – essential workhorses in pharmaceutical research
1. Assay Technologies for Proteases
Anuradha Roy,Gerald H. Lushington, James McGee, Rathnam Chaguturu
2. Discovery and development of isozyme-selective inhibitors involved in lipid metabolism
Taichi Ohshiro, Hiroshi Tomoda
3. Covalent enzyme inhibitor in drug discovery and development
4. Preclinomics: Using Enzyme Assays and Rodent Models for Metabolic diseases
Wu-Kuang Yeh, Richard G. Peterson
B. Enzymes – indispensable tools for improving druggability
5. Enzymes and Targeted Activation of Prodrugs
Yanhui Yang, Yu Chen, Herve Aloysius, Daigo Inoyama, Longqin Hu
6. Evolution of an Orally Active Prodrug of Gemcitabine
James R. McCarthy
7. Enzymatically Activated Phosphate and Phosphonate Prodrugs
Ivan S. Krylov, Charles E. McKenna
C. Enzymes – powerful weapons for correcting Nature’s errors
8. Treatment options for mucopolysaccharidosis type II (Hunter’s symdrome)
9. Enzyme replacement therapy for Fabry disease
Ley Nadine Lacbawan, Wei Zheng,Ozlem Goker-Alpan
10. Methods and principles of pancreatic function tests