Annual reports in medicinal chemistry. Volume 46 [electronic resource] / edited by John E. Macor
- Published
- Oxford : Academic Press, 2011.
- Physical Description
- 1 online resource (472 pages)
- Additional Creators
- Macor, John Eugene
Access Online
- ScienceDirect: ezaccess.libraries.psu.edu
- Contents
- Machine generated contents note: pt. I Central Nervous System Diseases / Albert J. Robichaud -- 1.Progress in the Medicinal Chemistry of Group III Metabotropic Glutamate Receptors / Dario Doller -- 1.Introduction -- 2.Group III Orthosteric Ligands -- 3.mGlu4 Receptor Allosteric Ligands -- 4.mGlu6 Receptor Ligands -- 5.mGlu7 Receptor Ligands -- 6.mGlu8 Receptor Ligands -- 7.Conclusions -- References -- 2.Recent Advances Toward Pain Therapeutics / Darrell A. Henze -- 1.Introduction -- 2.Sodium Channel Blockers -- 3.NGF/TrKA Pathway Interference -- 4.FAAH Inhibitors -- 5.Conclusions -- References -- 3.Central Modulation of Circadian Rhythm via CK1 Inhibition for Psychiatric Indications / Scot Mente -- 1.Introduction -- 2.Description of Circadian Clock -- 3.CK1 Inhibitors -- 4.Preclinical Animal Models -- 5.Conclusions -- References -- 4.Recent Progress in the Discovery of Kv7 Modulators / Britt-Marie Swahn -- 1.Introduction -- 2.Kv7.1 Channels -- 3.Kv7.2--Kv7.5 Channels -- 4.Conclusion -- References -- pt. II Cardiovascular and Metabolic Diseases / Andy Stamford -- 5.Bile Acid Receptor Modulators in Metabolic Diseases / Yanping Xu -- 1.Introduction -- 2.FXR Agonists -- 3.TGR5 Agonists -- 4.FXR/TGR5 Dual Agonists -- 5.Clinical Studies and Outlook -- References -- 6.Recent Advances in Mineralocorticoid Receptor Antagonists / Deepak S. Lala -- 1.Introduction -- 2.Aldosterone and MR Biology -- 3.RAAS Pathway, MR Antagonists versus ACE, ARB Therapy -- 4.Structural Features of the Ligand Binding Domain of MR -- 5.Current Medicinal Chemistry Efforts -- 6.Conclusions -- References -- 7.SGLT2 Inhibitors for Type 2 Diabetes / Tae Weon Lee -- 1.Introduction -- 2.SGLT2 Physiology -- 3.Clinical Trials -- 4.SGLT2 Inhibitors -- 5.Conclusion -- References -- pt. III Inflammation/Pulmonary/Gastrointestinal Diseases / David S. Weinstein -- 8.Recent Advances in the Discovery and Development of CRTh2 Antagonists / Laurence E. Burgess -- 1.Introduction -- 2.CRTh2 Antagonists -- 3.Conclusions -- References -- 9.Developments and Advances in Gastrointestinal Prokinetic Agents / Jeffrey M. McKenna -- 1.Introduction -- 2.Key Clinical Developments -- 3.Recent Medicinal Chemistry Developments -- 4.Conclusions -- References -- 10.Targeting Th17 and Treg Signaling Pathways in Autoimmunity / Mark S. Sundrud -- 1.Introduction -- 2.Current Targets and Molecules in Development -- 3.Conclusions -- References -- 11.Advances in the Discovery of C5a Receptor Antagonists / Juan C. Jaen -- 1.Introduction -- 2.Peptide and Large Molecule Agents -- 3.Macromolecules -- 4.Small Molecule Agents -- 5.Clinical Update -- 6.Marketed Agents -- 7.Conclusion -- References -- pt. IV Oncology / Shelli R. McAlpine -- 12.Inhibition of Translation Initiation as a Novel Paradigm for Cancer Therapy / Michael Chorev -- 1.Introduction -- 2.State of the Art -- 3.Conclusions -- References -- 13.The Discovery and Development of Smac Mimetics---Small-Molecule Antagonists of the Inhibitor of Apoptosis Proteins / Stephen M. Condon -- 1.Introduction -- 2.Organization of Inhibitor of Apoptosis Proteins -- 3.Smac, XIAP, and Caspase-9: Structure and Mechanism -- 4.Structure-Activity Relationships of Smac Mimetics -- 5.Bivalency and Smac Mimetic Function -- 6.Recently Described Smac Mimetics -- 7.Preclinical and Clinical Evaluation -- 8.Conclusion -- References -- 14.Case History: Discovery of Eribulin (Halaven[™]), a Halichondrin B Analogue That Prolongs Overall Survival in Patients with Metastatic Breast Cancer / Yoshito Kishi -- 1.Introduction -- 2.Halichondrin B -- 3.Eribulin Drug Discovery Program -- 4.From Discovery to Development -- 5.Conclusion -- References -- pt. V Infectious Diseases / John L Primeau -- 15.Emerging New Therapeutics Against Key Gram-Negative Pathogens / K. Dembowsky -- 1.Introduction -- 2.New Compounds from Known Classes -- 3.Novel Compound Classes -- 4.Conclusion -- References -- 16.Hepatitis C Virus---Progress Toward Inhibiting the Nonenzymatic Viral Proteins / Makonen Belema -- 1.Introduction -- 2.HCV core (Capsid) Protein Inhibitors -- 3.HCV Entry Inhibitors -- 4.HCV p7 Inhibitors -- 5.HCV NS4A Inhibitors -- 6.HCV NS4B Inhibitors -- 7.HCV NS5A Inhibitors -- 8.HCV IRES Inhibitors -- 9.Conclusion -- References -- 17.The Emergence of Small-Molecule Inhibitors of Capsid Assembly as Potential Antiviral Therapeutics / William J. Hansen -- 1.Introduction -- 2.Capsid Assembly Inhibitors -- 3.CA Inhibition via Host Factor Modulation -- 4.Conclusion -- References -- pt. VI Topics in Biology / John Lowe -- 18.Molecular Mechanism of Action (MMoA) in Drug Discovery / David C. Swinney -- 1.Introduction-Molecular Mechanism of Action -- 2.Molecular Descriptors -- 3.Metric, Biochemical Efficiency -- 4.Strategies For An Optimal MMoA -- 5.Chemistry of Binding Kinetics -- 6.Conclusions -- Acknowledgment -- References -- 19.Aryl Hydrocarbon Receptor (AhR) Activation: An Emerging Immunology Target? / Peter G. Klimko -- 1.Introduction -- 2.Overview of the AhR -- 3.Effects on Immune Cell Function -- 4.Therapeutic Effects in Animal Models of Human Diseases -- 5.Conclusion -- References -- 20.Peptidyl Prolyl Isomerase Inhibitors / Prashi Jain -- 1.Introduction -- 2.Categories of Peptidyl Prolyl Isomerases -- 3.Small-Molecule Inhibitors -- 4.Macrocyclic Inhibitors -- 5.Conclusion -- References -- 21.MicroRNAs---Basic Biology and Therapeutic Potential / Graham J. Brock -- 1.Introduction -- 2.MicroRNAs in Human Disease -- 3.MicroRNAs as Potential Therapeutics -- 4.Conclusion -- References -- pt. VII Topics in Drug Design and Discovery / Manoj C. Desai -- 22.Induced Pluripotent Stem Cells as Human Disease Models / Eugeni Vaisberg -- 1.Introduction -- 2.iPSC Technology -- 3.iPSC Derivation and Production -- 4.Differentiation---Problems and Promise -- 5.Leads for Drug Discovery and Development -- 6.Stem Cell Modulators -- 7.Predictive Toxicology with iPSC -- 8.In vitro Clinical Trial -- 9.Personalized Medicine: Patient Profiling for Optimal Drug Efficacy -- 10.Conclusion and the Role of Small Molecule Chemistry -- Acknowledgment -- References -- 23.The Future of Drug Repositioning: Old Drugs, New Opportunities / Gunda I. Georg -- 1.Introduction -- 2.Perspectives of Drug Repositioning -- 3.New Strategies Toward Drug Repositioning -- 4.Case Studies of Drug Repositioning Strategies -- 5.Future Directions of Drug Repositioning -- 6.Conclusion -- References -- 24.Deuterium in Drug Discovery and Development / Roger D. Tung -- 1.Introduction -- 2.Deuterium Background -- 3.Deuterium Safety and Pharmacology -- 4.Deuterium-Containing Drugs -- 5.Deuterated Drugs as Clinical Agents -- 6.Patentability of Deuterated Drugs -- 7.Conclusions -- References -- 25.Drug-Induced Phospholipidosis / James Morelli -- 1.Introduction -- 2.Evolving Regulatory and Industry Views -- 3.Screening Methods -- 4.Examples of Project Responses to Finding PLD -- 5.Conclusion -- Acknowledgments -- References -- pt. VIII Trends and Perspectives -- 26.To Market, To Marlcet-2010 / Nils Lonberg -- Overview -- 1.Alcaftadine (0.25%) (Ophthalmologic, Allergic Conjunctivitis) -- 2.Alogliptin (Antidiabetic) -- 3.Bilastine (Antiallergy) -- 4.Cabazitaxel (Anticancer) -- 5.Ceftaroline Fosamil (Antibacterial) -- 6.Corifollitropin Alfa (Infertility) -- 7.Dalfampridine (Multiple Sclerosis) -- 8.Denosumab (Osteoporosis and Metastatic Bone Disease) -- 9.Diquafosol (Ophthalmologic, Dry Eye) -- 10.Ecallantide (Angioedema, Hereditary) -- 11.Eribulin Mesylate (Anticancer) -- 12.Fingolimod Hydrochloride (Multiple Sclerosis) -- 13.Laninamivir Octanoate (Antiviral) -- 14.Lurasidone (Antipsychotic) -- 15.Mifamurtide (Anticancer) -- 16.Peramivir (Antiviral) -- 17.Roflumilast (Chronic Obstructive Pulmonary Disorder) -- 18.Romidepsin (Anticancer) -- 19.Sipuleucel-T (Anticancer) -- 20.Tesamorelin Acetate (HIV Lipodystrophy) -- 21.Ticagrelor (Antithrombotic) -- 22.Vernakalant (Antiarrhythmic) -- 23.Vinflunine Ditartrate (Anticancer) -- 24.Zucapsaicin (Analgesic) -- References.
- Summary
- 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.
- Subject(s)
- Genre(s)
- ISBN
- 9780123860095 (electronic bk.)
0123860091 (electronic bk.) - Note
- AVAILABLE ONLINE TO AUTHORIZED PSU USERS.
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