2017 Medicinal Chemistry Reviews

Volume 52
Joanne J. Bronson, Editor-In-Chief

Medicinal Chemistry Reviews is an outstanding 600 page volume providing timely and critical reviews of important topics in medicinal chemistry. It is provided free of charge to MEDI members in electronic format. Members can also order a print copy, for the cost of printing, shipping and handling (US, $30; International, $50).   

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Table of Contents:

Chapter 1

Discovery of TAK-063, a PDE10A Inhibitor with Balanced Activation of Direct and Indirect Pathways

Haruhide Kimura and Takahiko Taniguchi

Chapter 2

PDE1 Inhibition:  Potential for the Treatment of Cognitive Impairment

Brian Dyck, Marco Peters, and J. Guy Breitenbucher

Chapter 3

Discovery of the ALK/ROS1 Inhibitor, Lorlatinib (PF-06463922)

Paul F. Richardson and Ted W. Johnson

Chapter 4

Advances and Insights from CNS G Protein-Coupled Receptor Crystallography

John A. Christopher, Miles Congreve, Francesca Deflorian, and Fiona H. Marshall

Chapter 5

Recent Advances in BACE1 Biology and Inhibitors in Clinical Development

Jared N. Cumming, Matthew E. Kennedy, and Andrew W. Stamford

Chapter 6

Cardiac Sarcomere Activation and its Therapeutic Application in Heart Failure

Antonio Romero and Bradley P. Morgan

Chapter 7

Development of Sodium-Dependent Phosphate Co-Transporter 2b Inhibitors for Treatment of Hyperphosphatemia

Yanping Xu and Dariusz Wodka

Chapter 8

Glucokinase Activators for the Treatment of Diabetes

Paul Dransfield

Chapter 9

Recent Advances in the Discovery of CSFqR Inhibitors for Autoimmune Diseases

Dawn M. George, Michael Hoemann, and Jacqueline Loud

Chapter 10

Diverse Drugs with Gastrointestinal-Restricted Delivery

Thomas D. Aicher, Clarke B. Taylor, and Peter L. Toogood

Chapter 11

ROR-gamma-T Modulators for Th17-Driven Diseases:  Progress Into the Clinic

Colin M. Tice, Yuri Bukhtiyarov, Ya-Jun Zheng, Deepak Lala, and Suresh B. Singh

Chapter 12

Small Molecules for Cancer Immunotherapy

Timothy P. Heffon and Bryan K. Chen

Chapter 13

Beyond PARP:  Inhibitors of DNA Repair Processes as Potential Therapeutic Agents for Cancer

Allan Michael Jordan and Kate Mary Smith

Chapter 14

Small-Molecule Antagonists of Mcl-1

Joshua P. Taygerly and Daniel W. Robbins

Chapter 15

Novel Bacterial Type II Topoisomerase Inhibitors

Mark Joseph Mitton-Fry

Chapter 16

Capsid Assembly Modulators as Novel Antiviral Agents for the Treatment of Hepatitis B

Scott D. Kuduk and Angela M. Lam

Chapter 17

Recent Advances Towards Rational Antibacterial Discovery:  Addressing Permeation and Efflux

Quentin P. Avila, Helen I. Zgurskaya, and Adam S. Duerfeldt

Chapter 18

Endogenous Allosteric Modulators of G Protein-Coupled Receptors:  Implications in Drug Design

Dario Doller

Chapter 19

Thinking Small and Dreaming Big:  Medicinal Chemistry Strategies for Designing Optimal Antibody-Drug Conjugates (ADCs)

L. Nathan Tumey

Chapter 20

SILAC Proteomics in Drug Discovery

Thomas M. Graczyk, James P. Finn, and Ravi R. Iyer

Chapter 21

Aldehyde Oxidase Metabolism in Drug Discovery

Aaron C. Burns

Chapter 22

Repositioning Strategies that Target Remyelination for the Treatment of Multiple Sclerosis

Stefania Risso, Robert L. Hudkins, Peter H. Hutson, and Dmitri Leonoudakis

Chapter 23

Structure-Activity Relationship (SAR) Studies of Transient Receptor Potential (TRP) Channel Modulators

Christina M. LeGay and Darren J. Derksen

Chapter 24

Drug-Induced Liver Injury (DILI) Arising from Inhibition of Bile Acid Transport Proteins

Michael D. Aleo, Deepak Dalvie, and Amit S. Kalgutkar

Chapter 25

Case History:  Zurampic® (Lesinurad):  A Selective Uric Acid Reabsorption Inhibitor for the Treatment of Hyperuricemia in Gout Patients

Jean-Luc Girardet and Barry D. Quart

Chapter 26

Case History:  Epidaza® (Chidamide):  A Novel Oral Histone Deacetylase Inhibitor with Subtype Selectivity for Cancer Treatment

Xian P. Lu, Zhi B. Li, Zhi Q. Ning, De S. Pan, Song Shan, Xia Guo, Hai X. Cao, Jin D. Yu, and Qian J. Yang

Chapter 27

New Chemical Entities Entering Phase III Trials in 2016

Amy S. Lee, Adam J. Schrier, Salman Jabri, Nathan E. Wright, and Gregory T. Notte

Chapter 28

To Market, To Market--2016

Catherine A. Bolger, T.G. Murali Dhar, Achal Pashine, Peter S. Dragovich, William Mallet, J. Robert Merritt, and Kevin M. Peese

ACS Division of Medicinal Chemistry

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