The Renaissance in GPCR Research and Drug Discovery
Receptor Function, Receptor Structure, New Techniques, and Characterization of Drug Activity
- 1st Edition - November 1, 2026
- Latest edition
- Editor: Terry P. Kenakin
- Language: English
The Renaissance in GPCR Research and Drug Discovery: Receptor Function, Receptor Structure, New Techniques, Characterization of Drug Activity, Drug Discovery is a compre… Read more
Description
Description
The Renaissance in GPCR Research and Drug Discovery: Receptor Function, Receptor Structure, New Techniques, Characterization of Drug Activity, Drug Discovery is a comprehensive reference for pharmacology researchers. It focuses on utilizing novel aspects of GPCR function for therapeutic advantage and applying new chemical types to modify GPCR behavior. Recent advancements have revitalized GPCR discovery, opening unexplored avenues for new drug development. The book's content is meticulously divided into five distinct parts, covering evolutionary perspectives, novel functions, investigative technologies, therapeutic modalities, and a broad range of GPCR ligands.
Beyond these key topics, the book delves into the evolution of GPCRs as drug targets, the mechanisms behind their novel functions, and the latest technologies driving research and discovery. It also highlights new and recently approved therapeutic modalities and provides a broad coverage of GPCR ligands. Edited and authored by leading researchers, this book serves as an essential reference for drug discovery researchers and medicinal chemists, as well as AI researchers exploring this drug discovery space.
Beyond these key topics, the book delves into the evolution of GPCRs as drug targets, the mechanisms behind their novel functions, and the latest technologies driving research and discovery. It also highlights new and recently approved therapeutic modalities and provides a broad coverage of GPCR ligands. Edited and authored by leading researchers, this book serves as an essential reference for drug discovery researchers and medicinal chemists, as well as AI researchers exploring this drug discovery space.
Key features
Key features
- Covers the advances in the understanding of protein allostery and biased signaling that have revolutionized GPCR research in the past few years
- Introduces the new techniques providing tremendous advantages in the drug discovery field
- Edited and authored by the leading worldwide researchers in this area
Readership
Readership
Pharmacology researchers in academic and corporate setting
Table of contents
Table of contents
1. Introduction: GPCRs: Past, Present and Future
I. The Evolution of GPCRs as Drug Targets for Therapy
2. GPCRs: From Low Hanging Fruit to Uncharted Territory
3. Orphan GPCRs: New Horizons for GPCR Therapeutics
II. GPCR Mechanisms for Novel Function
4. GPCR Biased Signaling
5. Mechanisms of GPCR Bias and GPCR ‘Decoy Receptors’
6. GPCRs as Nature’s Prototype Allosteric Machine
7. Biasing GPCRs with ligands: expectations and limitations
III. New Technologies to Investigate GPCR Function
8. The Structural Biology Revolution in GPCR Pharmacology
9. Conformational Biosensors / TRUPATH
10. Impact of Conformational Dynamics on GPCR Drug Discovery
11. The kinetics of GPCR signaling and drug action
IV. New Therapeutic Modalities for GPCRs
12. GPCR Mutation and Human Disease
13. GPCR Phenotypic Signaling in Human Stem Cells
V. GPCR Ligands
14. Intracellular GPCR Signaling
15. Antibodies as Drugs for GPCRs
I. The Evolution of GPCRs as Drug Targets for Therapy
2. GPCRs: From Low Hanging Fruit to Uncharted Territory
3. Orphan GPCRs: New Horizons for GPCR Therapeutics
II. GPCR Mechanisms for Novel Function
4. GPCR Biased Signaling
5. Mechanisms of GPCR Bias and GPCR ‘Decoy Receptors’
6. GPCRs as Nature’s Prototype Allosteric Machine
7. Biasing GPCRs with ligands: expectations and limitations
III. New Technologies to Investigate GPCR Function
8. The Structural Biology Revolution in GPCR Pharmacology
9. Conformational Biosensors / TRUPATH
10. Impact of Conformational Dynamics on GPCR Drug Discovery
11. The kinetics of GPCR signaling and drug action
IV. New Therapeutic Modalities for GPCRs
12. GPCR Mutation and Human Disease
13. GPCR Phenotypic Signaling in Human Stem Cells
V. GPCR Ligands
14. Intracellular GPCR Signaling
15. Antibodies as Drugs for GPCRs
Product details
Product details
- Edition: 1
- Latest edition
- Published: November 1, 2026
- Language: English
About the editor
About the editor
TK
Terry P. Kenakin
Dr. Terry Kenakin is Professor of Pharmacology at the University of North Carolina School of Medicine. Prior to this, he spent 7 years in drug discovery at Burroughs-Wellcome. He then moved to GlaxoSmithKline for 25 years. Dr. Kenakin has written 11 books on Pharmacology, is the Editor in Chief of the Journal of Receptors and Signal Transduction, is on numerous Editorial Boards. He is the Editor-in-Chief of Comprehensive Pharmacology (Elsevier, 2022). He is the recipient of the 2008 Poulsson Medal for Pharmacology awarded by the Norwegian Society of Pharmacology for achievements in basic and clinical pharmacology and toxicology. He has also been awarded the 2011 Ariens Award from the Dutch Pharmacological Society and the 2014 Gaddum Memorial Award from the British Pharmacological Society, and the 2020 Goodman and Gilman Award in Receptor Pharmacology from ASPET.
Affiliations and expertise
Professor, Pharmacology, University of North Carolina, USA