Reviews: 2022 Medicinal Chemistry Reviews

Ref. n°: REV2022

Table of contents

Chapter 1In Tribute to John C. Martin
Joanne J. Bronson
Chapter 2Continually Humbling, Endlessly Fascinating, and Unfailingly Rewarding: Practical Lessons from a Lifelong Quest to Discover Breakthrough Medicines
Mark A. Murcko
Chapter 3Positron Emission Tomography Neuroimaging in Drug Discovery and Development
Erin L. Cole, Lindsey R. Drake
Chapter 4Recent Advances in the Development of Small-Molecule Apelin Receptor Agonists for Cardiovascular and Metabolic Diseases
Sanju Narayanan, Rajendra Uprety, Rangan Maitra, Scott Runyon
Chapter 5Recent Progress in Factor XI/XIa Inhibitor Discovery
Wu Yang, James R. Corte, Joseph M. Luettgen
Chapter 6Emerging Small-Molecule Therapeutics for Dilated Cardiomyopathy
Zhi-Liang Wei, Danielle L. Aubele
Chapter 7Negative Modulators of the cGAS-STING Pathway
Kelly A. Pike, Ramsay Beveridge, Patrick Cyr, Alex Skeldon, Li Wang, Jason D. Burch
Chapter 8RIPK2—From “Off-Target” to Clinical Candidate and Beyond
Karin Worm, Jill Henault
Chapter 9Small-Molecule Protein-Protein Interaction Modulators (PPIm) of the IL-17 and IL-17R Complexes
Mark David Andrews, Marcel John de Groot, Kevin Neil Dack
Chapter 10Arginase Inhibitors for Immuno-Oncology
Min Lu, Rachel L. Palte, Scott N. Mlynarski, Jason D. Shields
Chapter 11The Preclinical Journey of MET Inhibitors
Oliver Schadt, Guangxiu Dai
Chapter 12Recent Advances in Targeting the Androgen Receptor with PROTACs
Weiguo Xiang, Xin Han, Lijie Zhao, Shaomeng Wang
Chapter 13Small-Molecule Inhibitors of Herpes Simplex Virus: Standard of Care, State-of-the-Art, Future Directions
Thomas P. Stratton, Alexandre Mercier, Emma Abernathy, Jason Hudlicky
Chapter 14Medicinal Chemistry Endeavors for The Discovery of Novel Tuberculosis Drugs
Lutete Peguy Khonde, Paul Jackson
Chapter 15Deubiquitinases 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
Chapter 16Leveraging Small Molecules to Modulate the Microbiome to Treat Human Diseases
Anmol Gulati, Xin Guo
Chapter 17Cellular Target Engagement Assays for Small-Molecule Drug Discovery
Anton Delwig, Noriko Ishisoko, Robert A. Blake
Chapter 18Accelerating Drug Discovery by High-Throughput Experimentation
Jose Raul Montero Bastidas, Abdellatif El Marrouni, Maria Irina Chiriac, Thomas Struble, Dipannita Kalyani
Chapter 19Hydrogen/Deuterium Exchange-Mass Spectrometry in Medicinal Chemistry
Jeffrey A. Dodge, Michael J. Chalmers, Howard Broughton, Alfonso Espada
Chapter 20Cryo-EM and SLC Transporters
Joshua A. Lees, Seungil Han
Chapter 21Case History: Nurtec® ODT (Rimegepant) for the Acute and Preventive Treatment of Migraine
Gene M. Dubowchik, Robert Croop, Charles M. Conway
Chapter 22Veklury® (Remdesivir), A Nucleotide Prodrug Approved for the Treatment of COVID-19
Richard L. Mackman, Tomas Cihlar
Chapter 23New Chemical Entities Entering Phase III Trials in 2021
Matthew L. Condakes, Anna E. Hurtley, David W. Lin, Rhiannon Thomas-Tran, Juan del Pozo
Chapter 24To 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
Chapter 25To 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,