This book offers a detailed exploration of G-protein-coupled receptors (GPCRs), key membrane proteins that mediate cellular responses to diverse signals. It covers GPCR activation, regulation, structural advances, technological innovations, and drug discovery, emphasizing their crucial roles in physiology and therapy. By integrating molecular insights with clinical applications, the book bridges basic science and translational research in GPCR biology.
GPCRs function as vital cellular communication hubs by activating guanine nucleotide-binding proteins (G proteins) to transduce extracellular signals into intricate intracellular pathways. These signaling cascades regulate processes such as cell growth, gene expression, and intercellular communication, crucial for maintaining cellular homeostasis. Disruptions in GPCR signaling are linked to diverse pathologies, making them prime targets for therapeutic intervention.
The book begins with GPCR structure and activation mechanisms, followed by signaling networks and receptor regulation. It then covers breakthroughs in structural biology and cutting-edge research technologies. Drug discovery strategies, including allosterism and biased signaling, are explored next. Systems biology and molecular pathologies provide deeper insights into GPCR functions and diseases. The final chapters focus on cellular toxicity, preclinical to clinical drug development, and future research challenges.
This resource is designed for researchers and scientists in molecular pharmacology, cell biology, and drug discovery, as well as graduate and postgraduate students. Pharmaceutical industry professionals, educators, trainees, and healthcare professionals engaged in GPCR-targeted therapies will also find this book an essential guide to the latest advances and clinical applications.
Table of Contents:
Chapter 1. Introduction to G protein-coupled receptors (GPCRs): Structure and Function.- Chapter 2. Ligand-induced Allosteric Changes: Mechanisms of GPCR Activation.- Chapter 3. Unravelling the Complexity: GPCR Signaling Networks.- Chapter 4. Targeting Desensitized GPCRs: Therapeutic Opportunities and Challenges.- Chapter 5. Breaking Barriers: Latest Frontiers in GPCR Structural Analysis.- Chapter 6. Strategies for GPCR-directed Disease Management.- Chapter 7. Revolutionizing GPCR Studies: Cutting-edge Technologies.- Chapter 8. Translating GPCR Movements into Therapeutic Innovations.- Chapter 9. Advanced Concepts in GPCR Allosterism and Biased Signaling.- Chapter 10. Exploring GPCR Functions through Systems Biology.- Chapter 11. Strategic Pathways for Future GPCR Research and Development.- Chapter 12. Molecular Mechanisms Underlying GPCR-Associated Pathologies.- Chapter 13. Ligand-based and structure-based drug design for GPCRs.- Chapter 14. Exploring GPCR-Mediated Cellular Toxicity: Mechanisms and Implications.- Chapter 15. GPCR Drug Development from Preclinical Insights to Clinical Applications.
About the Author :
Dr. Prashant Tiwari is a distinguished academician and researcher in pharmaceutical sciences with over 15 years of teaching and research experience across reputed institutions in India. He is currently serving as an Associate Professor at Dayananda Sagar University, Bengaluru, Karnataka. His inventive research is reflected in multiple national and international patents. These include microencapsulation of Celecoxib to improve solubility for Alzheimer’s therapy, AI‑driven strategies for cancer drug analysis, a smart IV fluid controller with advanced locking mechanisms. He has been awarded grants from the Department of Biotechnology, Government of India, along with seed project funding from DSU. He has authored and edited more than 30 scholarly books and chapters with leading publishers and Nirali Prakashan Notable works include The 3R’s Approach in Preclinical Pharmacology (2025), Enzymatic Targets for Drug Discovery Against Alzheimer’s Disease (2024) and Brain Tumor Drug Development (2024). He has organized national conferences, delivered lectures and chaired sessions internationally. His achievements have earned prestigious honors, including the SPSR Excellence Award (2025), Dr. P.D. Patil National Award (2022), Young Scientist Award (2023), IPES Fellowship (2021), and the ICMR Senior Research Fellowship (2016–2019). His pursues research in neurodegenerative diseases, drug interactions, pharmacokinetics/pharmacodynamics and metabolic disorders.
Dr. K. Sunil Kumar is an Associate Professor at the College of Pharmaceutical Sciences, Dayananda Sagar University, Bengaluru, with over 16 years of teaching and research experience. He earned his PhD in Pharmaceutical Sciences from JNTU Hyderabad and has established himself as a dedicated academician in pharmacology. His research spans neuropharmacology, metabolic disorders, organ‑protective activities and drug interactions, reflecting a multidisciplinary approach. He has authored 65 research and review articles in reputed journals, five books and four book chapters, alongside six patents showcasing his innovative contributions to drug development. An active member of the Association of Pharmaceutical Teachers of India, he engages deeply with the academic community. His recent work highlights clinically relevant drug interactions, including Alprazolam with Pomegranate, Carbamazepine with Losartan and Naproxen with St. John’s Wort, as well as the antiparkinsonian potential of traditional formulations like Zinda Tilismath, inspiring students and researchers alike.
Dr. Pratap Kumar Sahu is actively engaged in advanced research in neuropharmacology, with a particular focus on Alzheimer’s disease and related cognitive disorders at the School of Pharmaceutical Sciences, Siksha O Anusandhan University. His recent work centers on the interplay between diabetes mellitus and neurodegeneration, exploring how metabolic dysfunction contributes to cognitive decline. He extensively investigates the repurposing of antidiabetic agents and evaluates their neuroprotective mechanisms using well‐established experimental models of AD and diabetes-induced cognitive impairment. A major component of his research involves nanotechnology-enabled drug delivery systems, including solid lipid nanoparticles, metal-based nanoformulations (AuNPs, SeNPs) and lipid nanocarriers designed to improve brain bioavailability and therapeutic efficacy of neuroprotective drugs. His publications highlight innovative approaches to enhance cognitive outcomes through nanoformulated antidiabetic compounds, paving the way for translational applications in neurodegenerative disease management. He also plays a major role in sponsored research, serving as Co-Principal Investigator in projects funded by LSRB-DRDO, ICMR and DBT BUILDER, and as Principal Investigator on an ICMR-funded project. He is a recipient of the UGC-GATE Scholarship (1999–2001), reflecting his longstanding academic excellence and deep commitment to research.
