Annual Reports in Medicinal Chemistry

Section I: Central Nervous System Diseases – ROBICHAUD

1. Voltage-Gated Calcium Channel Antagonists for the Central Nervous System

James C. Barrow and Joseph L. Duffy

2. Recent Developments in Glycine Transporter-1 Inhibitors

Christopher L. Cioffi, Shuang Liu and Mark A.Wolf

3. Modulators of Transient Receptor Potential Ion Channels

Rajagopal Bakthavatchalam and S. David Kimball

4. 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

5. High Affinity Niacin Receptor GPR109A Agonists

Hong C. Shen and Steven L. Colletti

6. Recent Advances in Acetyl CoA Carboxylase (ACC) Inhibitors

Matthew P. Bourbeau, John G. Allen, and Wei Gu

7. Enzymatic Targets in the Triglyceride Synthesis Pathway

Dmitry O. Koltun and Jeff Zablocki

8. Inhibitors of HIF Prolyl Hydroxylases

Michael H. Rabinowitz, Terrance D. Barrett, Mark D. Rosen, Hariharan Venkatesan

Section III: Inflammation / Pulmonary / GI - BARRISH/Weinstein

9. Opioid Receptor Antagonists for Gastrointestinal Dysfunction

R. William Hipkin and Roland E. Dolle

10. CFTR Modulators for the Treatment of Cystic Fibrosis

Sabine Hadida, Frederick Van Goor and Peter D. J. Grootenhuis

11. Targeting B-cells in inflammatory disease

Kevin S. Currie

12. Modulators of Toll-Like Receptor (TLR) Signaling

Mark Spyvee, Lynn Hawkins, and Sally Ishizaka

Section IV: Oncology - McAlpine

13. Janus Kinase 2 (JAK2) inhibitors for the treatment of myeloproliferative neoplasm (MPN)

Ashok V. Purandare, Matthew V. Lorenzi and Louis J. Lombardo

14. Development of poly(ADP-ribose)polymerase (PARP) inhibitors in oncology

Philip Jones

15. Epigenetic Targets and Cancer Drug Discovery

Patrick M. Woster, Ph.D

Section V: Infectious Diseases - Primeau

16. HIV-1 Integrase Strand Transfer Inhibitors

Brian A. Johns

17. Recent Advances in Drug Discovery for Neglected Tropical Diseases Caused by Infective Kinetoplastid Parasites

Robert T. Jacobs and Charles Ding

18. Recent Advances in the Inhibition of Bacterial Fatty Acid Biosynthesis

Vincent Gerusz

Section VI: Topics in Biology - LOWE

19. Back to the Plaque: Emerging Studies That Re-Focus Attention on the Neuritic Plaque in Alzheimer’s Disease

Dr. Robert B. Nelson

20. Targeting Methyl Lysine

Stephen V. Frye, Tom Heightman and Jian Jin

21. Chemical Proteomic Technologies for Drug Target Identification

Kieran F. Geoghegan and Douglas S. Johnson

22. NIH Translational Programs for Assisting Pre-Clinical Drug Discovery and Development

Raj N. Misra

Section VII: Topics in Drug Design and Discovery - DESAI

23. Role of Physicochemical Properties and Lipophilic Ligand Efficiency (LipE or LLE) in addressing Drug Safety Risks

Martin P. Edwards and David A. Price

24. Reducing the Risk of Drug Attrition Associated with Physicochemical Properties

Paul D. Leeson and James R. Empfield

25. Compound Collection Enhancement and Paradigms for High Throughput Screening - an Update

Stevan W Djuric, Irini Akritopoulou-Zanze, Philip B Cox and Scott Galasinski

26. 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

27. 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

28. To Market, To Market – 2009

Shridhar Hegde and Michelle Schmidt

• Covers findings related to cardiovascular, inflammation, and pulmonary diseases
• Examines issues in oncology, from mTor inhibitors to drug targets
• Incorporates up-to-date information on drug design and discovery, including delivery to market