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.

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Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

Contenu

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