Annual Reports in Medicinal Chemistry

Offers critical reviews of important topics in medicinal chemistry together with an emphasis on topics in the biological sciences, which provide the basis for various therapies. This title covers findings related to cardiovascular, inflammation, and pulmonary diseases. It examines issues in oncology, from mTor inhibitors to drug targets.

Section I: Central Nervous System Diseases - ROBICHAUD Voltage-Gated Calcium Channel Antagonists for the Central Nervous System James C. Barrow and Joseph L. Duffy Recent Developments in Glycine Transporter-1 Inhibitors Christopher L. Cioffi, Shuang Liu and Mark A.Wolf Modulators of Transient Receptor Potential Ion Channels Rajagopal Bakthavatchalam and S. David Kimball Defining Neuropharmacokinetic Parameters in CNS Drug Discovery to Determine Cross-species Pharmacologic Exposure-Response Relationships Christopher L. Shaffer Section II: Cardiovascular and Metabolic Diseases - STAMFORD High Affinity Niacin Receptor GPR109A Agonists Hong C. Shen and Steven L. Colletti Recent Advances in Acetyl CoA Carboxylase (ACC) Inhibitors Matthew P. Bourbeau, John G. Allen, and Wei Gu Enzymatic Targets in the Triglyceride Synthesis Pathway Dmitry O. Koltun and Jeff Zablocki Inhibitors of HIF Prolyl Hydroxylases Michael H. Rabinowitz, Terrance D. Barrett, Mark D. Rosen, Hariharan Venkatesan Section III: Inflammation / Pulmonary / GI - BARRISH/Weinstein Opioid Receptor Antagonists for Gastrointestinal Dysfunction R. William Hipkin and Roland E. Dolle CFTR Modulators for the Treatment of Cystic Fibrosis Sabine Hadida, Frederick Van Goor and Peter D. J. Grootenhuis Targeting B-cells in inflammatory disease Kevin S. Currie Modulators of Toll-Like Receptor (TLR) Signaling Mark Spyvee, Lynn Hawkins, and Sally Ishizaka Section IV: Oncology - McAlpine Janus Kinase 2 (JAK2) inhibitors for the treatment of myeloproliferative neoplasm (MPN) Ashok V. Purandare, Matthew V. Lorenzi and Louis J. Lombardo Development of poly(ADP-ribose)polymerase (PARP) inhibitors in oncology Philip Jones Epigenetic Targets and Cancer Drug Discovery Patrick M. Woster, Ph.D Section V: Infectious Diseases - Primeau HIV-1 Integrase Strand Transfer Inhibitors Brian A. Johns Recent Advances in Drug Discovery for Neglected Tropical Diseases Caused by Infective Kinetoplastid Parasites Robert T. Jacobs and Charles Ding Recent Advances in the Inhibition of Bacterial Fatty Acid Biosynthesis Vincent Gerusz Section VI: Topics in Biology - LOWE Back to the Plaque: Emerging Studies That Re-Focus Attention on the Neuritic Plaque in Alzheimer's Disease Dr. Robert B. Nelson Targeting Methyl Lysine Stephen V. Frye, Tom Heightman and Jian Jin Chemical Proteomic Technologies for Drug Target Identification Kieran F. Geoghegan and Douglas S. Johnson NIH Translational Programs for Assisting Pre-Clinical Drug Discovery and Development Raj N. Misra Section VII: Topics in Drug Design and Discovery - DESAI Role of Physicochemical Properties and Lipophilic Ligand Efficiency (LipE or LLE) in addressing Drug Safety Risks Martin P. Edwards and David A. Price Reducing the Risk of Drug Attrition Associated with Physicochemical Properties Paul D. Leeson and James R. Empfield Compound Collection Enhancement and Paradigms for High Throughput Screening - an Update Stevan W Djuric, Irini Akritopoulou-Zanze, Philip B Cox and Scott Galasinski The Role of Fluorine in the Discovery and Optimization of CNS Agents: Modulation of Drug-Like Properties Kevin J. Hodgetts, Kerry J. Combs, Amy M. Elder and Geraldine C. Harriman Patents in Drug Discovery: Case Studies, Examples, and Simple Steps Medicinal Chemists Can Take to Protect Hard-Won Intellectual Property Charles J. Andres, Jr. and Richard L. Treanor Section VIII: Trends and Perspectives To Market, To Market - 2009 Shridhar Hegde and Michelle Schmidt