The Renaissance in GPCR Research and Drug Discovery
Receptor Function, Receptor Structure, New Techniques, Characterization of Drug Activity, Drug Discovery
- 1st Edition - November 1, 2025
- Imprint: Academic Press
- Editor: Terry P. Kenakin
- Language: English
- Paperback ISBN:9 7 8 - 0 - 4 4 3 - 3 3 4 2 2 - 1
- eBook ISBN:9 7 8 - 0 - 4 4 3 - 3 3 4 2 3 - 8
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
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Request a sales quoteThe 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.
- 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
Pharmacology researchers in academic and corporate setting.
Introduction: GPCRs: Past, Present and Future
I. The Evolution of GPCRs as Drug Targets for Therapy
1. GPCRs: From Low Hanging Fruit to Uncharted Territory
2. Orphan GPCRs: New Horizons for GPCR Therapeutics
II. GPCR Mechanisms for Novel Function
3. GPCR Biased Signaling
4. GPCRs as Nature’s Prototype Allosteric Machine
5. GPCRs as Pleiotropic Ligands with Pluridimensional Efficacy
6. Arrestins: Versatile GPCR Partners
III. New Technologies to Investigate GPCR Function
7. The impact of GPCR Structure on New Drug Discovery
8. Conformational Biosensors / TRUPATH
9. The Impact of Computational Chemistry in GPCR Drug Discovery
10. Label Free GPCR Cellular Technologies
11. New GPCR Assays
12. Molecular Dynamics through Cross-linking Mass Spectrometry
13. New Modalities for Drugging GPCRs
14. Artificial Intelligence in Design of GPCR Drugs
15. New Methods to ‘Drug’ GPCRs
16. Impact of Conformational Dynamics on GPCR Drug Discovery
IV. New Therapeutic Modalities for GPCRs
17. GPCR Polypharmacology
18. GPCR Mutation and Human Disease
19. GPCR Phenotypic Signaling in Human Stem Cells
V. GPCR Ligands
20. Biologics and GPCRs
21. Repurposing GPCR Drugs
22. Intracellular GPCR Signaling
23. Antibodies as Drugs for GPCRs
I. The Evolution of GPCRs as Drug Targets for Therapy
1. GPCRs: From Low Hanging Fruit to Uncharted Territory
2. Orphan GPCRs: New Horizons for GPCR Therapeutics
II. GPCR Mechanisms for Novel Function
3. GPCR Biased Signaling
4. GPCRs as Nature’s Prototype Allosteric Machine
5. GPCRs as Pleiotropic Ligands with Pluridimensional Efficacy
6. Arrestins: Versatile GPCR Partners
III. New Technologies to Investigate GPCR Function
7. The impact of GPCR Structure on New Drug Discovery
8. Conformational Biosensors / TRUPATH
9. The Impact of Computational Chemistry in GPCR Drug Discovery
10. Label Free GPCR Cellular Technologies
11. New GPCR Assays
12. Molecular Dynamics through Cross-linking Mass Spectrometry
13. New Modalities for Drugging GPCRs
14. Artificial Intelligence in Design of GPCR Drugs
15. New Methods to ‘Drug’ GPCRs
16. Impact of Conformational Dynamics on GPCR Drug Discovery
IV. New Therapeutic Modalities for GPCRs
17. GPCR Polypharmacology
18. GPCR Mutation and Human Disease
19. GPCR Phenotypic Signaling in Human Stem Cells
V. GPCR Ligands
20. Biologics and GPCRs
21. Repurposing GPCR Drugs
22. Intracellular GPCR Signaling
23. Antibodies as Drugs for GPCRs
- Edition: 1
- Published: November 1, 2025
- No. of pages (Paperback): 400
- No. of pages (eBook): 400
- Imprint: Academic Press
- Language: English
- Paperback ISBN: 9780443334221
- eBook ISBN: 9780443334238
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