Frontmatter -- Color Plates -- Introduction: The Case for Polypharmacology / Andrew L Hopkins -- Polypharmacology: A Safety Concern in Drug Discovery. The Relevance of Off-Target Polypharmacology / Bruce D Car -- Screening for Safety-Relevant Off-Target Activities / Laszlo Urban, Steven Whitebread, Jacques Hamon, Dmitri Mikhailov, Kamal Azzaoui -- Pharmacological Promiscuity and Molecular Properties / Jens-Uwe Peters -- Kinases as Antitargets in Genotoxicity / Stephan Kirchner -- Activity at Cardiovascular Ion Channels: A Key Issue for Drug Discovery / Ian M Bell, Mark T Bilodeau, Armando A Lagrutta -- Prediction of Side Effects Based on Fingerprint Profiling and Data Mining / Jacques Migeon -- Polypharmacology: An Opportunity for Drug Discovery. Polypharmacological Drugs: 3Magic Shotguns4 for Psychiatric Diseases / Wesley K Kroeze, Bryan L Roth -- Polypharmacological Kinase Inhibitors: New Hopes for Cancer Therapy / Annalisa Petrelli -- Polypharmacology as an Emerging Trend in Antibacterial Discovery / Lynn L Silver -- A 3Magic Shotgun4 Perspective on Anticonvulsant Mechanisms / Matt T Bianchi, Kathy Chuang -- Selective Optimization of Side Activities (SOSA): A Promising way for Drug Discovery / Thierry Langer, Camille-Georges Wermuth -- Selected Approaches to Polypharmacological Drug Discovery. Selective Multitargeted Drugs / Richard Morphy -- Computational Multitarget Drug Discovery / Jeremy A Horst, Adrian Laurenzi, Brady Bernard, Ram Samudrala -- Behavior-Based Screening as an Approach to Polypharmacological Ligands / Dani Brunner, Vadim Alexandrov, Barbara Caldarone, Taleen Hanania, David Lowe, Jeff Schneider, Jayaraman Chandrasekhar -- Multicomponent Therapeutics / Alexis A Borisy, Grant R Zimmermann, Joseph Lèhr -- Case Studies. Discovery of Sunitinib as a Multitarget Treatment of Cancer / Catherine Delbaldo, Camelia Colichi, Marie-Paule Sablin, Chantal Dreyer, Bertrand Billemont, Sandrine Faivre, Eric Raymond -- Antipsychotics / Claus Riemer -- Triple-Uptake Inhibitors (Broad-Spectrum Antidepressants) / Phil Skolnick -- Therapeutic Potential of Small Molecules Modulating the Cyclooxygenase65-Lipoxygenase Pathway / Wolfgang Albrecht, Stefan Laufer -- Drug Research Leading to Imatinib and beyond to Nilotinib / Paul W Manley, Jorg Zimmermann -- Towards Antimalarial Hybrid Drugs / Bernard Meunier -- Multitargeted Drugs for Treatment of Alzheimer's Disease / Andrea Cavalli, Maria Laura Bolognesi -- Carbonic Anhydrases: Off Targets, Add-On Activities, or Emerging Novel Targets? / Claudiu T Supuran -- Index
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"An essential outline of the main facets of polypharmacology in drug discovery research. Extending drug discovery opportunities beyond the "one drug, one target" philosophy, a polypharmacological approach to the treatment of complex diseases is emerging as a hot topic in both industry and academic research. Polypharmacology in Drug Discovery presents an overview of the various facets of polypharmacology and how it can be applied as an innovative concept for developing medicines for treating bacterial infections, epilepsy, cancer, psychiatric disorders, and more."--
"Covers the two-sided nature of polypharmacology--its contribution to adverse drug reactions and its benefit in certain therapeutic drug classes. Addresses the important topic of polypharmacology in drug discovery, a subject that has not been thoroughly covered outside of scattered journal articles. Overviews state-of-the-art approaches and developments to help readers understand concepts and issues related to polypharmacology."--