Annual reports in medicinal chemistry

• 

  Año 2012, Número 47

  • Personal Essays

    • Reflections on Medicinal Chemistry at Merck, West Point

      Paul Anderson

      págs. 3-11

      

    • My Path in Seeking New Medicines

      Peter R. Bernstein

      págs. 13-24

      

    • Tales of Drug Discovery

      M. Ross Johnson

      págs. 25-34

      

  • Part I: Central Nervous System Diseases

    • Recent Developments in Targeting Neuroinflammation in Disease

      Allent T. Hopper, Brian M. Campbell, Henry Kao, Sean A. Pintchovski, Roland G.W. Staal

      págs. 37-53

      

    • Secretase Inhibitors and Modulators as a Disease-Modifying Approach Against Alzheimer's Disease

      Harrie J.M. Gijsen, François P. Bischoff

      págs. 55-69

      

    • mGluR2 Activators and mGluR5 Blockers Advancing in the Clinic for Major CNS Disorders

      Sylvain Célanire, Guillaume Duvey, Sònia Poli, Jean-Philippe Rocher

      págs. 71-88

      

    • NMDA Antagonists of GluN2B Subtype and Modulators of GluN2A, GluN2C, and GluN2D Subtypes�Recent Results and Developments

      Kamalesh B. Ruppa, Dalton King, Richard K. Olson

      págs. 89-103

      

    • Recent Advances in the Development of PET and SPECT Tracers for Brain Imaging

      Lei Zhang, Anabella Villalobos

      págs. 105-119

      

  • Part II: Cardiovascular and Metabolic Diseases

    • Case History: EliquisTM (Apixaban), a Potent and Selective Inhibitor of Coagulation Factor Xa for the Prevention and Treatment of Thrombotic Diseases

      Donald J.P. Pinto, Pancras C. Wong, Ruth R. Wexler, Robert M. Knabb

      págs. 123-141

      

    • AMPK Activation in Health and Disease

      Iyassu K. Sebhat, Robert W. Myers

      págs. 143-157

      

    • Type-2 Diabetes and Associated Comorbidities as an Inflammatory Syndrome

      Juan C. Jaen, Jay P. Powers, Tim Sullivan

      págs. 159-175

      

    • Beyond PPARs and Metformin: New Insulin Sensitizers for the Treatment of Type 2 Diabetes

      Philip A. Carpino, David Hepworth

      págs. 177-192

      

  • Part III: Inflammation/Pulmonary/GI

    • Recent Advances in the Discovery and Development of Sphingosine-1-Phosphate-1 Receptor Agonists

      Alaric J. Dyckman

      págs. 195-207

      

    • Bifunctional Compounds for the Treatment of COPD

      Gary Phillips, Michael Salmon

      págs. 209-221

      

    • Inflammatory Targets for the Treatment of Atherosclerosis

      Robert O. Hughes, Alessandra Bartolozzi, Hidenori Takahashi

      págs. 223-235

      

  • Part IV: Oncology

    • Nanotechnology Therapeutics in Oncology-Recent Developments and Future Outlook

      Paul F. Richardson

      págs. 239-252

      

    • Small-Molecule Antagonists of Bcl-2 Family Proteins

      Sean P. Brown, Joshua P. Taygerly

      págs. 253-266

      

    • Notch Pathway Modulators as Anticancer Chemotherapeutics

      Vibhavari Sail, M. Kyle Hadden

      págs. 267-280

      

    • Anaplastic Lymphoma Kinase Inhibitors for the Treatment of ALK-Positive Cancers

      Kazutomo Kinoshita, Nobuhiro Oikawa, Takuo Tsukuda

      págs. 281-293

      

  • Part V: Infectious Diseases

    • Recent Advances in the Discovery of Dengue Virus Inhibitors

      Jeremy Green, Upul Bandarage, Kate Luisi, Rene Rijnbrand

      págs. 297-317

      

    • Nonfluoroquinolone-Based Inhibitors of Mycobacterial Type II Topoisomerase as Potential Therapeutic Agents for TB

      Pravin S. Shirude, Shahul Hamed

      págs. 319-330

      

    • HCV Inhibition Mediated Through the Nonstructural Protein 5A (NS5A) Replication Complex

      Robert Hamatake, Andrew Maynard, Wieslaw M. Kazmierski

      págs. 331-345

      

  • Part VI: Topics in Biology

    • Antibody-Drug Conjugates for Targeted Cancer Therapy

      Victor S. Goldmacher, Thomas Chittenden, Ravi V.J. Chari, Yelena V. Kovtun, John M. Lambert

      págs. 349-366

      

    • 3D Cell Cultures: Mimicking In Vivo Tissues for Improved Predictability in Drug Discovery

      Indira Padmalayam, Mark J. Suto

      págs. 367-378

      

    • Virally Encoded G Protein-Coupled Receptors: Overlooked Therapeutic Opportunities?

      Nuska Tschammer

      págs. 379-392

      

    • Recent Advances in Wnt/ß-Catenin Pathway Small-Molecule Inhibitors

      Daniel D. Holsworth, Stefan Krauss

      págs. 393-409

      

  • Part VII: Topics in Drug Design and Discovery

    • Targeted Covalent Enzyme Inhibitors

      Mark C. Noe, Adam M. Gilbert

      págs. 413-439

      

    • Drug Design Strategies for GPCR Allosteric Modulators

      Jeffrey P. Conn, Scott D. Kuduk, Darío Doller

      págs. 441-457

      

    • Progress in the Development of Non-ATP-Competitive Protein Kinase Inhibitors for Oncology

      Campbell McInnes

      págs. 459-474

      

  • Part VIII: Trends and Perspectives

    • New Chemical Entities Entering Phase III Trials in 2011

      Gregory T. Notte

      págs. 477-498