Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agent (Hardcover)

Contributors vii

Preface ix

Part A _Enzymes – essential workhorses in pharmaceutical research 1

1 Assay Technologies for Proteases 3
Anuradha Roy, Gerald H. Lushington, James McGee, and Rathnam Chaguturu

2 Discovery and Development of Isozyme-Selective Inhibitors Involved in Lipid Metabolism 55
Taichi Ohshiro and Hiroshi Tomoda

3 Covalent Enzyme Inhibition in Drug Discovery and Development 81
Shujaath Mehdi

4 Preclinomics: Enzyme Assays and Rodent Models for Metabolic diseases 131
Wu-Kuang Yeh and Richard G. Peterson

Part B _Enzymes – indispensable tools for improving druggability 163

5 Enzymes and Targeted Activation of Prodrugs 165
Yanhui Yang, Yu Chen, Herve Aloysius, Daigo Inoyama, and Longqin Hu

6 Evolution of an Orally Active Prodrug of Gemcitabine 237
James R. McCarthy

7 Enzymatically Activated Phosphate and Phosphonate Prodrugs 253
Ivan S. Krylov and Charles E. McKenna

Part C E nzymes – powerful weapons for correcting Nature’s errors 301

8 Treatment Options for Mucopolysaccharidosis Type II (Hunter’s Syndrome) 303
Michael Beck

9 Enzyme Replacement Therapy for Fabry Disease 321
Ley Nadine Lacbawan, Wei Zheng, and Ozlem Goker-Alpan

10 Methods and Principles of Pancreatic Function Tests 335
Henrike von Schassen, Jutta Keller, and Peter Layer

Index 341