Anti-Inflammatory Drug Discovery

Anti-Inflammatory Drug Discovery provides a comprehensive review of recent medicinal chemistry approaches to a variety of important therapeutic targets and provides a key reference for those interested in the prosecution of modern drug discovery programs directed at anti-inflammatory mechanisms of action. The editors, with extensive experience in this field, have selected key thought-leaders who will bring their experience to the medicinal chemistry literature for each target, ranging from components of the arachadonic acid cascade, to kinases, GPCRs, sphingolipids and others, to summarize its background biology and detail new insights, major advances and issues related to bringing new anti-inflammatory therapies to market. Consisting of five main sections key targets covered will include the AA Cascade: mPGES1, cPLA2, Leukotriene A4 Hydrolase, CRTH2; Kinases: P38/PDE4, MAPKAP Kinase 2 (MK2), Syk Kinase Inhibitors, Jak Kinases, IKK , Bruton's Tyrosine Kinase; GPCRs: CCR1, CCR2 Antagonists, CB2 Agonists; Sphingolipids: S1P1 Receptor Agonists, Sphingosine Lyase and Sphingosine Kinase 1 and a final miscellaneous section that looks at Non-Steroidal Dissociated Glucocorticoid Receptor Agonists. The book will be essential reading for pharmacologists, medicinal chemists and pharmaceutical scientists working in industry and academia. Professor Laufer has held the chair for Pharmaceutical/Medicinal Chemistry at the University of Tubingen since 1999. He received his Ph.D. from the University of Regensburg (1989) and obtained his Venia Legendi (habilitation) in Pharmaceutical Chemistry from the University of Mainz (1997). From 1990-99 he held senior research and executive positions in pharmaceutical industry. His research interests cover major aspects of anti-inflammatory drug discovery and development, including design, synthesis, biological screening, metabolism, and bioanalytics. The molecular targets that have been the focus of research in his laboratory are the key enzymes of the arachidonate cascade and protein kinases. Two drug candidates from his lab have reached clinical development stages (ML3000-Licofelone, a COX/LOX Inhibitor and CSB3595, a p38 MAPK/PDE4 inhibitor). Professor Laufer has authored 230 publications and is the inventor of 36 patent families. Jeremy I. Levin has been a Director of Medicinal Chemistry for Boehringer-Ingelheim in Ridgefield, Connecticut, since 2010. He received his B.A. from Johns Hopkins University in 1978 and a Ph.D. in organic chemistry with Professor Steven Weinreb at the Pennsylvania State University in 1983. Following a post-doctoral fellowship at the University of California at Irvine with Professor Larry Overman, he spent 25 years in the pharmaceutical industry at American Cyanamid (Lederle laboratories) and Wyeth Research. Dr. Levin has worked in a variety of therapeutic areas including CNS, inflammation and immunology, and oncology. He is the author/co-author of more than 75 papers and an inventor on more than 60 U. S. Patents. Table of Contents Preface; Section 1 (AA Cascade) mPGES1; cPLA2; Leukotriene A4 Hydrolase; CRTH2; Section 2 (Kinases) P38/PDE4; MAPKAP Kinase 2 (MK2); Syk Kinase Inhibitors; Jak Kinases; IKK; Bruton's Tyrosine kinase; Section 3 (GPCRs) CCR1; CCR2 Antagonists; CB2 Agonists; Section 4 (Sphingolipids) S1P1 receptor Agonists; Sphingosine Lyase and Sphingosine Kinase 1; Section 5 (Steroid Hormone Receptors) Non-Steroidal Dissociated Glucocorticoid Receptor Agonists; Index