Table of contents
Chapter 1 | In Tribute to John C. Martin
Joanne J. Bronson |
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Chapter 2 | Continually Humbling, Endlessly Fascinating, and Unfailingly Rewarding: Practical Lessons from a Lifelong Quest to Discover Breakthrough Medicines
Mark A. Murcko |
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Chapter 3 | Positron Emission Tomography Neuroimaging in Drug Discovery and Development
Erin L. Cole, Lindsey R. Drake |
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Chapter 4 | Recent Advances in the Development of Small-Molecule Apelin Receptor Agonists for Cardiovascular and Metabolic Diseases
Sanju Narayanan, Rajendra Uprety, Rangan Maitra, Scott Runyon |
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Chapter 5 | Recent Progress in Factor XI/XIa Inhibitor Discovery
Wu Yang, James R. Corte, Joseph M. Luettgen |
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Chapter 6 | Emerging Small-Molecule Therapeutics for Dilated Cardiomyopathy
Zhi-Liang Wei, Danielle L. Aubele |
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Chapter 7 | Negative Modulators of the cGAS-STING Pathway
Kelly A. Pike, Ramsay Beveridge, Patrick Cyr, Alex Skeldon, Li Wang, Jason D. Burch |
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Chapter 8 | RIPK2—From “Off-Target” to Clinical Candidate and Beyond
Karin Worm, Jill Henault |
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Chapter 9 | Small-Molecule Protein-Protein Interaction Modulators (PPIm) of the IL-17 and IL-17R Complexes
Mark David Andrews, Marcel John de Groot, Kevin Neil Dack |
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Chapter 10 | Arginase Inhibitors for Immuno-Oncology
Min Lu, Rachel L. Palte, Scott N. Mlynarski, Jason D. Shields |
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Chapter 11 | The Preclinical Journey of MET Inhibitors
Oliver Schadt, Guangxiu Dai |
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Chapter 12 | Recent Advances in Targeting the Androgen Receptor with PROTACs
Weiguo Xiang, Xin Han, Lijie Zhao, Shaomeng Wang |
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Chapter 13 | Small-Molecule Inhibitors of Herpes Simplex Virus: Standard of Care, State-of-the-Art, Future Directions
Thomas P. Stratton, Alexandre Mercier, Emma Abernathy, Jason Hudlicky |
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Chapter 14 | Medicinal Chemistry Endeavors for The Discovery of Novel Tuberculosis Drugs
Lutete Peguy Khonde, Paul Jackson |
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Chapter 15 | Deubiquitinases and Their Inhibitors: Challenges and Recent Advances
Peter R. Hewitt, Oliver Barker, Matthew D. Helm, Xavier Jacq, Colin R. O’Dowd, Natalie Page, J. S. Shane Rountree, Timothy Harrison |
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Chapter 16 | Leveraging Small Molecules to Modulate the Microbiome to Treat Human Diseases
Anmol Gulati, Xin Guo |
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Chapter 17 | Cellular Target Engagement Assays for Small-Molecule Drug Discovery
Anton Delwig, Noriko Ishisoko, Robert A. Blake |
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Chapter 18 | Accelerating Drug Discovery by High-Throughput Experimentation
Jose Raul Montero Bastidas, Abdellatif El Marrouni, Maria Irina Chiriac, Thomas Struble, Dipannita Kalyani |
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Chapter 19 | Hydrogen/Deuterium Exchange-Mass Spectrometry in Medicinal Chemistry
Jeffrey A. Dodge, Michael J. Chalmers, Howard Broughton, Alfonso Espada |
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Chapter 20 | Cryo-EM and SLC Transporters
Joshua A. Lees, Seungil Han |
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Chapter 21 | Case History: Nurtec® ODT (Rimegepant) for the Acute and Preventive Treatment of Migraine
Gene M. Dubowchik, Robert Croop, Charles M. Conway |
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Chapter 22 | Veklury® (Remdesivir), A Nucleotide Prodrug Approved for the Treatment of COVID-19
Richard L. Mackman, Tomas Cihlar |
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Chapter 23 | New Chemical Entities Entering Phase III Trials in 2021
Matthew L. Condakes, Anna E. Hurtley, David W. Lin, Rhiannon Thomas-Tran, Juan del Pozo |
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Chapter 24 | To Market, to Market—2020: Small Molecules
Erika Araujo, Ian M. Bell, Alexander Burckle, Dennis C. Koester, James R. Manning, Richard D. Caldwell, Georgette Castanedo, Samantha A. Green, Mingshuo Zeng, Laurent Debien, T. G. Murali Dhar, Natalie Holmberg-Douglas, Eric R. Welin, J. Robert Merritt, Kevin M. Peese, Denise C. Grünenfelder, Julian C. Lo |
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Chapter 25 | To Market, to Market—2021: Macromolecular Therapeutics
Nicholas J. Agard, Peter S. Dragovich, Ryan L. Kelly, Shion A. Lim, Allison M. Beal, Ian Moench, Si-Jie Chen, Anna M. Gram, Pei-Pei Kung, |