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TRP Channels as Therapeutic Targets
From Basic Science to Clinical Use
1st Edition - March 14, 2015
Editor: Arpad Szallasi
Language: English
Hardback ISBN:9780124200241
9 7 8 - 0 - 1 2 - 4 2 0 0 2 4 - 1
eBook ISBN:9780124200791
9 7 8 - 0 - 1 2 - 4 2 0 0 7 9 - 1
TRP Channels as Therapeutic Targets: From Basic Science to Clinical Use is authored by experts across academia and industry, providing readers with a complete picture of the thera…Read more
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TRP Channels as Therapeutic Targets: From Basic Science to Clinical Use is authored by experts across academia and industry, providing readers with a complete picture of the therapeutic potential and challenges associated with using TRP channels as drug targets.
This book offers a unique clinical approach by covering compounds that target TRP channels in pre-clinical and clinical phases, also offering a discussion of TRP channels as biomarkers.
An entire section is devoted to the novel and innovative uses of these channels across a variety of diseases, offering strategies that can be used to overcome the adverse effects of first generation TRPV1 antagonists.
Intended for all researchers and clinicians working toward the development of successful drugs targeting TRP channels, this book is an essential resource chocked full of the latest clinical data and findings.
Contains comprehensive coverage of TRP channels as therapeutic targets, from emerging clinical indications to completed clinical trials
Discusses TRP channels as validated targets, ranging from obesity and diabetes through cancer and respiratory disorders, kidney diseases, hypertension, neurodegenerative disorders, and more
Provides critical analysis of the complications and side effects that have surfaced during clinical trials, offering evidence-based suggestions for overcoming them
New and established researchers from academia and industry involved in target validation, compound discovery and drug development programs aimed at TRP channels; clinical investigators/clinicians who need to become familiar with the latest clinical trials with drugs targeting TRP channels
Preface
Chapter 1: An Introduction to Transient Receptor Potential Ion Channels and Their Roles in Disease
Abstract
Discovery and General Properties of TRP Channels
TRP Channels in Normal Physiology
TRP Channels and Disease
Therapeutic Strategies Based on TRP Channel Modulation
Acknowledgment
Chapter 2: Transient Receptor Potential Dysfunctions in Hereditary Diseases: TRP Channelopathies and Beyond
Abstract
Acknowledgments
Introduction
TRPC Channelopathies
TRPV Channelopathies
TRPM Channelopathies
TRPA Channelopathies
TRPML Channelopathies
TRPP Channelopathies
Conclusions
Chapter 3: The Role of TRPV1 in Acquired Diseases: Therapeutic Potential of TRPV1 Modulators
Abstract
Acknowledgment
Introduction
TRPV1 and Pain
TRPV1 and Gastrointestinal System-Related Disease
TRPV1 and Urinary System-Related Diseases
TRPV1 and Central Nervous System-Related Diseases
TRPV1 and Respiratory System-Related Diseases
TRPV1 and Cancer
TRPV1 and Cardiovascular System-Related Diseases
TRPV1 and Metabolic Diseases
TRPV1 and Other Disease Conditions
Conclusions
Chapter 4: TRP Gene Polymorphism and Disease Risk
Abstract
TRP Gene Polymorphism
TRPA1
The TRPC Subfamily
The TRPM Subfamily
The TRPML Subfamily
The TRPV Subfamily
Disease Risk, Clinical Diagnosis, and Personalized Medicine
Chapter 5: Use of Topical Capsaicin for Pain Relief
Abstract
Introduction
Pharmacodynamics
Pharmacokinetics
Efficacy and Therapeutic Uses
Safety and Tolerability
Delivery of Treatment with Capsaicin 8% Patch—Practical Aspects
Application Procedure for the Capsaicin 8% Patch
Postprocedural Instructions for Patients
Chapter 6: TRPV1 Agonist Cytotoxicity for Chronic Pain Relief: From Mechanistic Understanding to Clinical Application
Abstract
Introduction
Mechanisms of TRPV1 Agonist Therapeutic Action
Four Main Determinants of TRPV1 Agonist Actions
Selectivity of RTX at the Cellular Level
RTX Produces a Prolonged Channel Open Time
TRPV1 Is Selectively Expressed in Subpopulations of DRG Neurons
RTX Is Administered Locally
Companion Dog and Human Studies
Companion (Pet) Dog Models of Chronic Pain
TRPV1 Agonists in the Companion Dog Model of Bone Cancer
TRPV1 Agonists in the Companion Dog Model of Osteoarthritis
Human Studies
Chapter 7: Intravesical Capsaicin and Resiniferatoxin for Bladder Disorders
Abstract
Capsaicin and Resiniferatoxin Targets and Effects in the Urinary Bladder
The Rationale for Using Vanilloids to Overcome Lower Urinary Tract Symptoms
Intravesical Application of Vanilloids
Is There a Future for Intravesical Instillation of Vanilloids in the Urinary Bladder?
Chapter 8: Clinical and Preclinical Experience with TRPV1 Antagonists as Potential Analgesic Agents
General Properties of the TRPA1 Channel in Pain Transduction and Amplification
TRPA1 in Pathophysiological Pain Models
Biomarkers
Conclusions
Chapter 10: TRPA1 Antagonists as Potential Therapeutics for Respiratory Diseases
Abstract
TRPA1 as a Reactive, Noxious Irritant Sensor
Presence and Function of TRPA1 in the Mammalian Respiratory Tract
Exogenous Agonists that Cause TRPA1 Activation in the Airways
Non-Aldehyde TRPA1 Agonists Found in Cigarette Smoke
Other Hazardous Air Pollutants that Activate TRPA1
Endogenous Molecules that Signal Through TRPA1 in Mammals
Nonneuronal TRPA1 Expression and Function
In Vivo Preclinical Pharmacology of TRPA1 Blockers
TRPA1 Antagonists Claimed in the Patent Literature
Conclusions
Chapter 11: Is TRPV3 a Drug Target?—A Decade of Learning
Abstract
Introduction
TRPV3 Tissue Expression
TRPV3 Activation
Functional Role of TRPV3 Channel: Evidence from Genetic Studies
TRPV3 and Human Diseases
Safety of TRPV3 Antagonists
Pharma Efforts in Discovering TRPV3 Antagonists in Treatment of Human Diseases
Chapter 12: Small Molecule Agonists and Antagonists of TRPV4
Abstract
Introduction
TRPV4 Agonists
TRPV4 Antagonists
Conclusions
Chapter 13: Potential Therapeutic Applications for TRPV4 Antagonists in Lung Disease
Abstract
Introduction
TRPV4 Localization in Lungs
Acute Lung Injury via Direct Channel Activation
Ventilator-Induced Lung Injury (VILI)
High Vascular Pressure-Induced Lung Injury
Heart Failure and Pulmonary Edema
Pulmonary Arterial Hypertension
Airway Disease and Cough
Chapter 14: TRPM8 as a Target for Analgesia
Abstract
TRPM8 Structure
Localization of TRPM8 in the Nervous System
In Vitro Studies on the Physiological Role of TRPM8 in Sensing Cool/Cold Temperatures
In Vivo Studies on the Physiological Role of TRPM8 in Sensing Cool/Cold Temperatures
Setting of Thermal Sensitivity in TRPM8-Expressing Sensory Neurons
The Impact of Pain States on TRPM8 Function
TRPM8-Mediated Analgesia
TRPM8 in Thermoregulation
Pharmacology of TRPM8 Antagonists and Agonists
Modulation of TRPM8 Function by Cellular Signaling
CNS Processes Activated by TRPM8-Positive Afferents
Conclusions
Chapter 15: Connecting TRP Channels and Cerebrovascular Diseases
Abstract
Overview: TRP Channels: Types, Distribution, and Function
TRP Channels in Diseases
TRP Channels in Smooth Muscle Cells
TRP Channels and Endothelial Function
TRP Channels and Hypertension
TRP Channels and Stroke
Future Directions
Chapter 16: Activating, Inhibiting, and Highjacking TRP Channels for Relief from Itch
Abstract
Introduction
Which Sensory Neurons Signal Itch?
Activating TRP Channels to Block Itch
Inhibiting TRP Channels to Block Itch
Highjacking TRP Channels to Deliver Relief from Itch
An Unexpected Role for TprV3: Mutations in TRPV3 Result in Itchy Lesions Found in Olmsted Syndrome
Conclusions
Chapter 17: Role of TRP Channels in Skin Diseases
Abstract
Introduction
TRPV Subfamily
TRPA1
The TRPC (Canonical) Family
TRPMs
TRPML3
Summary
Chapter 18: Transient Receptor Potential Channels in Hypertension and Metabolic Syndrome
Abstract
TRP Channels in Hypertension
TRP Channels in Metabolic Syndrome
Perspective
Chapter 19: Transient Receptor Potential (TRP) Cation Channels in Diabetes
Abstract
Acknowledgments
TRP’s in Pancreatic ß Cells
TRPV1-Expressing Sensory Neurons in β Cell Function and Diabetes Mellitus
TRP Channels in Diabetes-Associated Complications
TRP Channels as Drug Target in T1DM and T2DM
Conclusions
Chapter 20: TRP Channels in Cardiovascular Disease
Abstract
Acknowledgment
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
TRPM7 Channels and Atrial Fibrillation
TRPC Channels in Pulmonary Hypertension
Chapter 21: Targeting of Transient Receptor Potential Channels in Digestive Disease
Abstract
Acknowledgments
Overview
Expression of TRP Channels in the Gut and Their Role in GI Motility and Secretion
TRP Channels as Targets for Prokinetic Drugs
Roles of TRP Channels in the Development of IBD
TRP Channel Sensitization in IBS- and IBD-Related Pain
Summary
Chapter 22: TRP Channels in Cancer
Abstract
Introduction
The Role of TRP Channels in Cancer
Clinical Implications and Concluding Remarks
Chapter 23: Are Brain TRPs Viable Targets for Curing Neurodegenerative Disorders and Improving Mental Health?
Abstract
The Role of TRP Channels in Building the Brain and Regulating its Functions: Introducing the Players
TRP Channel Dysfunction in Epilepsy
Cerebellar Ataxia as a “TRP Channelopathy”
TRP Channels in Neuroprotection and Their Dysfunction in Neurodegenerative Disorders
TRP Channels in Psychiatric Disorders and Mental Retardation
The “Addictive” TRP Channels
TRP Channels in Stroke and Traumatic Brain Injury
Conclusions
Chapter 24: Mucolipidosis Type IV: Part I
Abstract
Introduction
Clinical Presentation
Cellular Abnormalities in MLIV Patients
MCOLN1 and Mucolipin-1
Mutations in the MCOLN1 gene
The Mucolipin Channel and its Interacting Partners
Animal Models for MLIV
Summary and Future Goals
Chapter 25: TRPML1-Dependent Processes as Therapeutic Targets
Abstract
Acknowledgments
Introduction
TRPML1 Features and Properties
TRPML1-Dependent Processes, Shown and Discussed
TRPML1-Dependent Processes Inferred from its Functional Context
Conclusions
Chapter 26: TRPs in Respiratory Disorders: Opportunities Beyond TRPA1
Abstract
Introduction
Overview of TRP Channels and Their Expression and Function in the Respiratory System
Summary and Perspectives
Chapter 27: Conclusions
Index
No. of pages: 536
Language: English
Edition: 1
Published: March 14, 2015
Imprint: Academic Press
Hardback ISBN: 9780124200241
eBook ISBN: 9780124200791
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, Hungary
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