
2022 Medicinal Chemistry Reviews
Editor(s):
Volume 57
Publication Date (Web):December 21, 2022
1 Genentech, South San Francisco, California, U.S.A.
2 Bristol Myers Squibb, Cambridge, Massachusetts, U.S.A.
ISBN13: 9781734427455
eISBN: 9781734427455
DOI: 10.1021/mc-2022-vol57
Joanne J. Bronson and Joachim Rudolph, Editors-In-Chief, the ACS Division of Medicinal Chemistry, and the American Chemical Society are pleased to announce the publication of 2022 Medicinal Chemistry Reviews, Volume 57 in the series. Become a member of the ACS Division of Medicinal Chemistry now to access the electronic version of Medicinal Chemistry Reviews at no cost in the Resources section. As of 2022, ACS eBooks collections now include Medicinal Chemistry Reviews, an outstanding annual volume produced by the ACS Division of Medicinal Chemistry, providing timely and critical reviews of important topics in medicinal chemistry. Prior year volumes can be obtained from the ACS Division of Medicinal Chemistry.
Table of Contents, Contributor List, Preface
i-xixDOI: 10.1021/mc-2022-vol57.frnt
IN TRIBUTE TO JOHN C. MARTIN
Joanne J. Bronson
Chapter
1, 1-24DOI: 10.1021/mc-2022-vol57.ch01
CONTINUALLY HUMBLING, ENDLESSLY FASCINATING, AND UNFAILINGLY REWARDING: PRACTICAL LESSONS FROM A LIFELONG QUEST TO DISCOVER BREAKTHROUGH MEDICINES
Mark A. Murcko
Chapter
2, 27-57DOI: 10.1021/mc-2022-vol57.ch02
POSITRON EMISSION TOMOGRAPHY NEUROIMAGING IN DRUG DISCOVERY AND DEVELOPMENT
Erin L. Cole - and
Lindsey R. Drake
Chapter
3, 61-90DOI: 10.1021/mc-2022-vol57.ch03
RECENT ADVANCES IN THE DEVELOPMENT OF SMALL-MOLECULE APELIN RECEPTOR AGONISTS FOR CARDIOVASCULAR AND METABOLIC DISEASES
Sanju Narayanan - ,
Rajendra Uprety - ,
Rangan Maitra - , and
Scott Runyon
Chapter
4, 95-115DOI: 10.1021/mc-2022-vol57.ch04
RECENT PROGRESS IN FACTOR XI/XIA INHIBITOR DISCOVERY
Wu Yang - ,
James R. Corte - , and
Joseph M. Luettgen
Chapter
5, 117-141DOI: 10.1021/mc-2022-vol57.ch05
EMERGING SMALL-MOLECULE THERAPEUTICS FOR DILATED CARDIOMYOPATHY
Zhi-Liang Wei - and
Danielle L. Aubele
Chapter
6, 143-163DOI: 10.1021/mc-2022-vol57.ch06
NEGATIVE MODULATORS OF THE CGAS-STING PATHWAY
Kelly A. Pike - ,
Ramsay Beveridge - ,
Patrick Cyr - ,
Alex Skeldon - ,
Li Wang - , and
Jason D. Burch
Chapter
7, 167-196DOI: 10.1021/mc-2022-vol57.ch07
RIPK2—FROM “OFF-TARGET” TO CLINICAL CANDIDATE AND BEYOND
Karin Worm - and
Jill Henault
Chapter
8, 199-219DOI: 10.1021/mc-2022-vol57.ch08
SMALL-MOLECULE PROTEIN-PROTEIN INTERACTION MODULATORS (PPIm) OF THE IL-17 AND IL-17R COMPLEXES
Mark David Andrews - ,
Marcel John de Groot - , and
Kevin Neil Dack
Chapter
9, 221-238DOI: 10.1021/mc-2022-vol57.ch09
ARGINASE INHIBITORS FOR IMMUNO-ONCOLOGY
Min Lu - ,
Rachel L. Palte - ,
Scott N. Mlynarski - , and
Jason D. Shields
Chapter
10, 243-265DOI: 10.1021/mc-2022-vol57.ch10
THE PRECLINICAL JOURNEY OF MET INHIBITORS
Oliver Schadt - and
Guangxiu Dai
Chapter
11, 267-292DOI: 10.1021/mc-2022-vol57.ch11
RECENT ADVANCES IN TARGETING THE ANDROGEN RECEPTOR WITH PROTACS
Weiguo Xiang - ,
Xin Han - ,
Lijie Zhao - , and
Shaomeng Wang
Chapter
12, 295-317DOI: 10.1021/mc-2022-vol57.ch12
SMALL-MOLECULE INHIBITORS OF HERPES SIMPLEX VIRUS: STANDARD OF CARE, STATE-OF-THE-ART, FUTURE DIRECTIONS
Thomas P. Stratton - ,
Alexandre Mercier - ,
Emma Abernathy - , and
Jason Hudlicky
Chapter
13, 321-334DOI: 10.1021/mc-2022-vol57.ch13
MEDICINAL CHEMISTRY ENDEAVORS FOR THE DISCOVERY OF NOVEL TUBERCULOSIS DRUGS
Lutete Peguy Khonde - and
Paul Jackson
Chapter
14, 337-358DOI: 10.1021/mc-2022-vol57.ch14
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 - , and
Timothy Harrison
Chapter
15, 363-387DOI: 10.1021/mc-2022-vol57.ch15
LEVERAGING SMALL MOLECULES TO MODULATE THE MICROBIOME TO TREAT HUMAN DISEASES
Anmol Gulati - and
Xin Guo
Chapter
16, 389-414DOI: 10.1021/mc-2022-vol57.ch16
CELLULAR TARGET ENGAGEMENT ASSAYS FOR SMALL-MOLECULE DRUG DISCOVERY
Anton Delwig - ,
Noriko Ishisoko - , and
Robert A. Blake
Chapter
17, 419-440DOI: 10.1021/mc-2022-vol57.ch17
ACCELERATING DRUG DISCOVERY BY HIGH-THROUGHPUT EXPERIMENTATION
Jose Raul Montero Bastidas - ,
Abdellatif El Marrouni - ,
Maria Irina Chiriac - ,
Thomas Struble - , and
Dipannita Kalyani
Chapter
18, 443-463DOI: 10.1021/mc-2022-vol57.ch18
HYDROGEN/DEUTERIUM EXCHANGE-MASS SPECTROMETRY IN MEDICINAL CHEMISTRY
Jeffrey A. Dodge - ,
Michael J. Chalmers - ,
Howard Broughton - , and
Alfonso Espada
Chapter
19, 465-487DOI: 10.1021/mc-2022-vol57.ch19
CRYO-EM AND SLC TRANSPORTERS
Joshua A. Lees - and
Seungil Han
Chapter
20, 489-512DOI: 10.1021/mc-2022-vol57.ch20
CASE HISTORY: NURTEC® ODT (RIMEGEPANT) FOR THE ACUTE AND PREVENTIVE TREATMENT OF MIGRAINE
Gene M. Dubowchik - ,
Robert Croop - , and
Charles M. Conway
Chapter
21, 517-542DOI: 10.1021/mc-2022-vol57.ch21
VEKLURY® (REMDESIVIR), A NUCLEOTIDE PRODRUG APPROVED FOR THE TREATMENT OF COVID-19
Richard L. Mackman* - and
Tomas Cihlar
Chapter
22, 545-569DOI: 10.1021/mc-2022-vol57.ch22
NEW CHEMICAL ENTITIES ENTERING PHASE III TRIALS IN 2021
Matthew L. Condakes - ,
Anna E. Hurtley - ,
David W. Lin - ,
Rhiannon Thomas-Tran - , and
Juan del Pozo
Chapter
23, 571-484DOI: 10.1021/mc-2022-vol57.ch23
TO MARKET, TO MARKET–2021: 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 - , and
Julian C. Lo
Chapter
24, 587-731DOI: 10.1021/mc-2022-vol57.ch24
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 - , and
Pei-Pei Kung
Chapter
25, 733-805DOI: 10.1021/mc-2022-vol57.ch25
