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36 reviewsAn 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. Filled with a collection of instructive case studies that reinforce the material and illuminate the subject, this practical guide:
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
Fosters interdisciplinary drug discovery research by embracing computational, synthetic, in vitro and in vivo pharmacological and clinical aspects of polypharmacology
A clear road map for helping readers successfully navigate around the problems involved with promiscuous ligands and targets, Polypharmacology in Drug Discovery provides real examples, in-depth explanations and discussions, and detailed reviews and opinions to spark inspiration for new drug discovery projects.Content:
Chapter 1 The Relevance of Off?Target Polypharmacology (pages 7–14): Bruce D. Car
Chapter 2 Screening for Safety?Relevant Off?Target Activities (pages 15–46): Laszlo Urban, Steven Whitebread, Jacques Hamon, Dmitri Mikhailov and Kamal Azzaoui
Chapter 3 Pharmacological Promiscuity and Molecular Properties (pages 47–62): Jens?Uwe Peters
Chapter 4 Kinases as Antitargets in Genotoxicity (pages 63–81): Stephan Kirchner
Chapter 5 Activity at Cardiovascular Ion Channels: A Key Issue for Drug Discovery (pages 83–109): Ian M. Bell, Mark T. Bilodeau and Armando A. Lagrutta
Chapter 6 Prediction of Side Effects Based on Fingerprint Profiling and Data Mining (pages 111–132): Jacques Migeon
Chapter 7 Polypharmacological Drugs: “Magic Shotguns” for Psychiatric Diseases (pages 133–148): Wesley K. Kroeze and Bryan L. Roth
Chapter 8 Polypharmacological Kinase Inhibitors: New Hopes for Cancer Therapy (pages 149–165): Annalisa Petrelli
Chapter 9 Polypharmacology as an Emerging Trend in Antibacterial Discovery (pages 167–202): Lynn L. Silver
Chapter 10 A “Magic Shotgun” Perspective on Anticonvulsant Mechanisms (pages 203–225): Matt T. Bianchi and Kathy Chuang
Chapter 11 Selective Optimization of Side Activities (SOSA): A Promising way for Drug Discovery (pages 227–243): Thierry Langer and Camille?Georges Wermuth
Chapter 12 Selective Multitargeted Drugs (pages 245–262): Richard Morphy
Chapter 13 Computational Multitarget Drug Discovery (pages 263–301): Jeremy A. Horst, Adrian Laurenzi, Brady Bernard and Ram Samudrala
Chapter 14 Behavior?Based Screening as an Approach to Polypharmacological Ligands (pages 303–313): Dani Brunner, Vadim Alexandrov, Barbara Caldarone, Taleen Hanania, David Lowe, Jeff Schneider and Jayaraman Chandrasekhar
Chapter 15 Multicomponent Therapeutics (pages 315–321): Alexis A. Borisy, Grant R. Zimmermann and Joseph Lehar
Chapter 16 Discovery of Sunitinib as a Multitarget Treatment of Cancer (pages 323–342): Catherine Delbaldo, Camelia Colichi, Marie?Paule Sablin, Chantal Dreyer, Bertrand Billemont, Sandrine Faivre and Eric Raymond
Chapter 17 Antipsychotics (pages 343–362): Claus Riemer
Chapter 18 Triple?Uptake Inhibitors (Broad?Spectrum Antidepressants) (pages 363–382): Phil Skolnick
Chapter 19 Therapeutic Potential of Small Molecules Modulating the Cyclooxygenase–5?Lipoxygenase Pathway (pages 383–408): Wolfgang Albrecht and Stefan Laufer
Chapter 20 Drug Research Leading to Imatinib and beyond to Nilotinib (pages 409–421): Paul W. Manley and Jurg Zimmermann
Chapter 21 Towards Antimalarial Hybrid Drugs (pages 423–439): Bernard Meunier
Chapter 22 Multitargeted Drugs for Treatment of Alzheimer's Disease (pages 441–458): Andrea Cavalli and Maria Laura Bolognesi
Chapter 23 Carbonic Anhydrases: Off Targets, Add?On Activities, or Emerging Novel Targets? (pages 459–491): Claudiu T. Supuran