Enzyme Technologies – Pluripotent Players Discovering Therapeutic Agents

<p>Contributors vii</p>
<p>Preface ix</p>
<p>Part A —Enzymes essential workhorses in pharmaceutical research 1</p>
<p>1 Assay Technologies for Proteases 3<br /> Anuradha Roy, Gerald H. Lushington, James McGee, and Rathnam Chaguturu</p>
<p>2 Discovery and Development of Isozyme–Selective Inhibitors Involved in Lipid Metabolism 55<br /> Taichi Ohshiro and Hiroshi Tomoda</p>
<p>3 Covalent Enzyme Inhibition in Drug Discovery and Development 81<br /> Shujaath Mehdi</p>
<p>4 Preclinomics: Enzyme Assays and Rodent Models for Metabolic diseases 131<br /> Wu–Kuang Yeh and Richard G. Peterson</p>
<p>Part B —Enzymes indispensable tools for improving druggability 163</p>
<p>5 Enzymes and Targeted Activation of Prodrugs 165<br /> Yanhui Yang, Yu Chen, Herve Aloysius, Daigo Inoyama, and Longqin Hu</p>
<p>6 Evolution of an Orally Active Prodrug of Gemcitabine 237<br /> James R. McCarthy</p>
<p>7 Enzymatically Activated Phosphate and Phosphonate Prodrugs 253<br /> Ivan S. Krylov and Charles E. McKenna</p>
<p>Part C E nzymes powerful weapons for correcting Nature s errors 301</p>
<p>8 Treatment Options for Mucopolysaccharidosis Type II (Hunter s Syndrome) 303<br /> Michael Beck</p>
<p>9 Enzyme Replacement Therapy for Fabry Disease 321<br /> Ley Nadine Lacbawan, Wei Zheng, and Ozlem Goker–Alpan</p>
<p>10 Methods and Principles of Pancreatic Function Tests 335<br /> Henrike von Schassen, Jutta Keller, and Peter Layer</p>
<p>Index 341</p>