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TRP Channels as Therapeutic Targets
Advances in Basic Science and Clinical Use
- 2nd Edition - August 22, 2024
- Editor: Arpad Szallasi
- Language: English
- Hardback ISBN:9 7 8 - 0 - 4 4 3 - 1 8 6 5 3 - 0
- eBook ISBN:9 7 8 - 0 - 4 4 3 - 1 8 6 5 4 - 7
TRP Channels as Therapeutic Targets: From Basic Science to Clinical Use, Second Edition is a comprehensive reference on the roles of TRP Channels in health and disease states. C… Read more
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Request a sales quoteTRP Channels as Therapeutic Targets: From Basic Science to Clinical Use, Second Edition is a comprehensive reference on the roles of TRP Channels in health and disease states. Chapters are completely updated, withe new topics on TRP channels biology, the crystalline structure of TRP channels, targeting TRP channels for pain relief, the relationship with migraine, emerging pain targets, a comprehensive view of the role of TRP channels in respiratory diseases and COVID complications, anxiety relief, renal disease, arthritis, and therapeutic opportunities for thermal regulation. This is a great reference for broad segments of the scientific and medical community. Researchers working on TRP channel drug discovery will benefit from the overview of applications to conditions in specific organ systems. Clinicians interested in new drugs in the pipeline will also find this book helpful for biologic principles of action.
- Presents the perspectives of several life science research specialties on the topic
- Provides a comprehensive picture of the TRP field, from TRP channel dysfunction through TRP drug discovery and development to clinical trials and everyday medical practice
- Represents an updated and complete reference
Research and development scientists in the pharmaceutical industry. Clinicians interested in new drugs in the pipeline
- Cover image
- Title page
- Table of Contents
- Copyright
- Contributors
- Preface
- Chapter 1. Opening remarks: What makes TRP channels attractive therapeutic targets?
- Introduction
- Group I channels
- Group II channels
- THE physiological roles of TRP channels
- Chapter 2. Biology of TRP channels
- Introduction
- Families of TRP channels
- Physiological importance of TRP channels
- TRP channels in the physiology of different cell systems
- Cardiovascular system
- Respiratory system
- Endothelial barrier
- Immune system
- Pancreas
- Reproductive system
- Urinary system
- Gastrointestinal tract, liver, and adipose tissue
- Skeletal muscle and bone system
- Central nervous system
- Conclusion
- Chapter 3. Targeting TRP channels: The emerging role of cryogenic electron microscopy in drug discovery
- Introduction
- Structure-based drug discovery
- TRP channel structural biology
- Cryo-electron microscopy
- TRPV1
- TRPV5
- TRPV3
- TRPM8
- TRPA1
- Future perspectives
- Chapter 4. Thermo-TRPs: Temperature-sensitive TRP channels
- Introduction
- The definition of temperature sensitive channels
- Discovery, functional characterization, and structural studies of thermo-TRPs
- TRPV1
- TRPV2
- TRPV3
- TRPV4
- TRPA1
- TRPM2
- TRPM3
- TRPM4/5
- TRPM8
- TRPC5
- Basic thermodynamics of thermo-TRPs
- Temperature sensor
- Concluding remarks
- Chapter 5. “TRP channelopathies”: TRP channel dysfunction in hereditary diseases
- Overview
- The mechanisms and the effects of TRP dysregulation in hereditary diseases
- Hereditary diseases that are caused by TRP dysfunction
- Perspectives
- Chapter 6. Current understanding of TRP channels and their genomics: Implications in health research
- Summary
- TRP channels: General introduction
- Classification and functions of TRP channels
- Localization of TRP channels in cells and in subcellular organelles
- TRP channels as regulators of development and gene expressions
- Copy number variations of TRP channels
- Alternate splicing of TRP genes
- Cross talk between TRP channels and miRNA
- Different variants of TRP channels
- Pathogenic mutations of TRP channels (genetic mutations)
- Penetration of TRP variants: No-phenotype to embryonic lethality
- Nonconventional translation initiation of TRP channels
- TRP variants as risk factors
- Conclusion and future outlook
- Chapter 7. TRP channel drug discovery strategies
- Introduction
- Overview of TRP channels
- Drug discovery strategies
- Conclusion
- Chapter 8. High-dose capsaicin patch for pain relief: Clinical experience
- Background
- Efficacy of high-dose capsaicin in clinical practice: Clinical and observational trial data
- Tolerability and adverse effects
- Comparison with oral therapies
- Cost and access
- Practical considerations
- Summary and conclusions
- Chapter 9. Therapeutic uses of injectable capsaicin for pain
- Introduction
- Therapeutic uses of capsaicin
- Potential mechanisms of analgesia
- Conclusion
- Chapter 10. Resiniferatoxin for permanent pain relief in cancer patients
- Introduction: TRPV1 agonists and the treatment of pain
- Periganglionic administration
- Intrathecal administration
- Epidural administration
- Conclusions
- Chapter 11. TRPV1 antagonists: Future drug discovery directions
- Introduction
- Clinical overview of TRPV1 antagonists
- Issues to be addressed for clinical TRPV1 antagonists
- Strategies for developing TRPV1 antagonists as drug candidates
- Perspective
- Chapter 12. TRPA1 antagonists for pain relief
- Introduction
- TRPA1 in thermal and chemical sensation
- TRPA1 in mechanical nociception and primary hyperalgesia
- TRPA1 in secondary (central) mechanical hyperalgesia
- TRPA1 in pathophysiological pain models
- Peripheral traumatic neuropathy
- Peripheral diabetic neuropathy
- Chemotherapy-induced neuropathy
- Osteoarthritis
- Sleep deprivation–induced pain hypersensitivity
- Bacterial infection–induced pain and inflammation
- Bladder pain syndrome
- TRPA1 and human pain
- TRPA1 antagonist hit finding and lead optimization
- TRPA1 antagonists
- TRPA1 antagonist phase 1 studies
- TRPA1 antagonist phase 2 studies
- TRPA1 antagonist phase 3 studies
- TRPA1 agonists for pain relief?
- Conclusions
- Chapter 13. TRPM3: An emerging pain target (and more)
- Introduction
- TRPM3 basics II—Pharmacology
- TRPM3 in the somatosensory system
- Chapter 14. TRP channels and migraine
- Migraine mediators
- Neurogenic inflammation and CGRP
- CGRP and migraine
- TRP channels in PSNs
- TRPV1 and migraine
- TRPA1 and migraine
- Other TRP channels and migraine
- Conclusions
- Chapter 15. TRP channels in the GU tract
- Introduction
- TRP channels in bladder afferents
- TRP channels in nonneuronal cells in the urinary bladder
- TRP role in bladder function
- TRP role during micturition dysfunction
- Interactions between different TRPs and between TRP and non-TRP receptors
- TRP channels in the kidney, ureters, and urethra
- TRP channels in the male genital tract
- TRP channels in the female genital tract
- TRP channels and cancer
- Chapter 16. TRP channels in respiratory disorders
- Introduction
- Respiratory disorders
- The role of TRP channels in respiratory disorders
- Summary
- Chapter 17. TRP channels: Emerging targets in COVID-19 and its complications
- Introduction
- SARS-CoV-2 and COVID-19
- TRP channels
- Inflammation and cytokine storm in COVID-19
- Pain in COVID-19
- Respiratory complications in COVID-19
- Fever in COVID-19
- Neurological complications in COVID-19
- Cardiovascular complications in COVID-19
- GI complications in COVID-19
- Other complications in COVID-19
- Post-COVID-19 (long-COVID-19) symptoms
- TRP channels as emerging therapeutic targets
- Abbreviations
- Chapter 18. TRP channels in cardiovascular disease
- Calcium signaling in the cardiovascular system
- TRP channels and cardiovascular disease
- TRP channels in cardiac hypertrophy
- Role of TRP channels in cardiac hypertrophy signaling pathways
- Pharmacological developments targeting TRP channels in cardiac hypertrophy
- TRP channels and cardiac arrhythmias
- TRPM4 and cardiac conduction disease
- TRP channels and atrial fibrillation and fibrosis
- TRP channels in pulmonary hypertension
- Chapter 19. TRP channels in cerebral vascular disorders
- Introduction
- The cerebral circulation
- TRP channels in cerebral vascular physiology
- TRP channels in stroke
- Alzheimer's disease and related dementias
- Conclusion and perspectives
- Chapter 20. TRPV1 in blood pressure regulation: A new therapeutic target in hypertension?
- Historical background—General remarks
- Structure and regulation of TRPV1
- TRPV1-mediated vascular functions
- Pharmacology of the vascular TRPV1
- Physiological ligand and regulators of TRPV1 in the vasculature
- Future perspectives
- Chapter 21. Activating, inhibiting, and hijacking TRP channels for relief from itch
- Introduction
- Which sensory neurons signal itch?
- Activating TRP channels to block itch
- Inhibiting TRP channels to block itch
- Hijacking TRP channels to deliver relief from itch
- An unexpected role for TprV3: Mutations in TrpV3 result in itchy lesions found in Olmsted syndrome
- Chapter 22. TRP channels in dermatology
- Introduction
- TRP channels in the skin
- TRP channels in dermatological conditions
- Concluding remarks: Therapeutic targeting, future directions
- Chapter 23. Transient Receptor Potential (TRP) channels in cancer: Implications for drug discovery and development
- Background and general aspects
- The TRPC channel family
- TRPC1
- TRPC6
- The TRPM channel family
- TRPM1
- TRPM2
- TRPM4
- TRPM7
- TRPM8
- The TRPV channel family
- TRPV1
- TRPA1
- Summary
- Chapter 24. TRP channel expression in the tumor microenvironment: Implications for tumor progression and metastasis
- Cancer microenvironment; sensors of metabolic changes
- Cancer-associated fibroblasts (CAFs) and TRP channels
- Cancer-associated stellate cells and TRP channels
- Angiogenesis and TRP channels
- Tumor-infiltrating immune cells and TRP channels
- TRP channels and macrophages
- TRP channels and dendritic cells
- T lymphocytes and TRP channels
- Cancer infiltrating nerve fibers and TRP channels
- Schwann cells, cancer microenvironment and TRP channels
- Conclusions
- Chapter 25. TRP channels as potential target molecules for pharmacotherapy of neurological diseases
- Stroke
- TRPM2
- TRPM3
- TRPM4
- TRPM7
- TRPM8
- TRPV1
- TRPV2
- TRPV4
- TRPC1
- TRPC3
- TRPC4
- TRPC5
- TRPC6
- Migraine
- TRPA1
- TRPV1
- TRPV4
- TRPM8
- TRPC4
- Epilepsy
- TRPA1
- TRPC
- TRPC1, TRPC4, 5
- TRPC3, 6, 7
- TRPV1
- TRPV4
- TRPM2
- TRPM3
- TRPM4, 6, 7
- TRPM8
- TRPP
- Alzheimer's disease
- TRPA1
- TRPV
- TRPC
- TRPM
- Parkinson's disease
- TRPC1
- TRPC3
- TRPM2
- TRPM7
- TRPM8
- TRPML1
- TRPV1
- Multiple sclerosis
- TRPA1
- TRPV1
- TRPV6
- TRPM2
- TRPM8
- TRPP1, 3
- TRP channels and MS
- Conclusions
- Funding
- Chapter 26. Targeting TRP channels for anxiety relief and improving mental health
- The role of canonical TRP channels in building the brain and regulating its functions
- Redox sensitive TRP channels in the brain
- TRP channels in psychiatric disorders and mental retardation
- The “addictive” TRP channels
- Conclusions
- Chapter 27. Potential of agents that modulate transient receptor potential (TRP) channels as therapies in arthritis
- Introduction
- Discovery of the TRPV1 channel
- Discovery of capsaicin
- The TRPV1 channel
- Use of capsaicin analogs
- The ultrapotent capsaicin agonist resiniferatoxin (RTX)
- TRPV1 receptor antagonists
- Discovery of the TRPA1 receptor and link to neurogenic inflammation
- Other TRP ligands
- Chapter 28. TRP channels as molecular targets to relieve endocrine-related diseases
- Development and classification of TRP channels
- TRP channels in the pancreas
- TRP channels in the salivary gland
- TRP channels in the adrenal gland
- TRP channels in the mammary gland
- TRP channels in the gallbladder
- TRP channels in the sweat glands
- TRP channels in the lacrimal gland
- Conclusion and discussion
- Abbreviations
- Chapter 29. Transient receptor potential (TRP) channels in metabolic syndrome
- Introduction
- TRP channels
- Functional characteristics of TRP channels in various aspects of MS and T2DM
- Conclusion
- Chapter 30. TRP channels in renal disease. Lessons from Polycystin-2 (TRPP2)
- Transient receptor potential (TRP) superfamily
- TRP channels and renal function
- Lessons from Polycystin-2 in renal function and disease
- TRP channels and Ca2+ oscillations in renal cells
- Perspective
- Chapter 31. TRP channels and thermoregulation; therapeutic opportunities
- Introduction
- Thermosensing by peripheral sensory neurons
- Thermoregulation by thermal input to peripheral sensory neurons
- Thermosensing at the hypothalamic thermoregulatory center
- TRP channels regulate effector functions for thermoregulation
- Body temperature change in mice with TRP channel KO
- Perspectives
- Chapter 32. Concluding remarks: Past, present, future
- Background
- A new dawn
- TRP channels and sensory transduction
- TRP channel structures
- TRP channels and therapeutics
- Index
- No. of pages: 608
- Language: English
- Edition: 2
- Published: August 22, 2024
- Imprint: Academic Press
- Hardback ISBN: 9780443186530
- eBook ISBN: 9780443186547
AS
Arpad Szallasi
Arpad Szallasi is a leading expert on the roles of TRP channels in health and disease. He was the first to provide a biochemical proof for the existence of the vanilloid (capsaicin) receptor, now known as TRPV1. Currently, he holds an Associate Professor position at the 1st Department of Pathology and Experimental Cancer Research, Semmelweis University, Budapest, Hungary.
His research focuses on targeting of TRP channels for therapeutic purposes, with special emphasis on pain and inflammation.
Arpad Szallasi obtained his MD degree Summa cum Laude from the Medical University School of Debrecen, Hungary (1984). He received his PhD degree in Pharmacology from the Karolinska Institute, Stockholm, Sweden (1995).
Arpad Szallasi held several research positions both in academia (Karolinska Institute, Washington University, St. Louis, MO) and industry (Menarini Ricerche Sud, Pomezia, Italy) before pursuing a carrier in diagnostic pathology.
Arpad Szallasi is a past President for the New Jersey Association of Blood Bank Professional and a former medical advisor to the American Red Cross.
Affiliations and expertise
Associate Professor position at the 1st Department of Pathology and Experimental Cancer Research, Semmelweis University, Budapest, HungaryRead TRP Channels as Therapeutic Targets on ScienceDirect