Pharmacology and Therapeutics of Constitutively Active Receptors

Pharmacology and Therapeutics of Constitutively Active Receptors

1st Edition - June 11, 2014

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  • Editor: Ya-Xiong Tao
  • Hardcover ISBN: 9780124171978
  • eBook ISBN: 9780124172067

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Description

Volume 70 of Advances in Pharmacology presents the pharmacology and therapeutics of constitutively active receptors. With a variety of chapters and the best authors in the field, the volume is an essential resource for pharmacologists, immunologists, and biochemists alike. Advances in Pharmacology provides a rich collection of reviews on timely topics. The series places emphasis on the molecular bases of drug action, both applied and experimental.

Key Features

  • Contributions from the best authors in the field
  • An essential resource for pharmacologists, immunologists, and biochemists

Readership

Pharmacologists, immunologists, and biochemists

Table of Contents

    • Preface
    • Chapter One: Constitutively Active Rhodopsin and Retinal Disease
      • Abstract
      • 1 Introduction
      • 2 Rhodopsin Activity
      • 3 Constitutive Activity in Rhodopsin that Causes Disease
      • 4 How Constitutive Activity Can Cause Different Phenotypes
      • 5 Conclusion
      • Conflict of Interest
      • Acknowledgments
    • Chapter Two: Constitutive Activity in Gonadotropin Receptors
      • Abstract
      • 1 Introduction
      • 2 Naturally Occurring CAMs of the Gonadotropin Receptors
      • 3 Experimental Models of Gonadotropin Receptor CAMs
      • 4 Molecular Basis of Constitutive Activity in Gonadotropin Receptors
      • 5 Design of New Molecules for Controlling the Activity of Constitutively Active Gonadotropin Receptors
      • 6 Conclusion
      • Conflict of Interest
      • Acknowledgments
    • Chapter Three: Constitutive Activities in the Thyrotropin Receptor: Regulation and Significance
      • Abstract
      • 1 Introduction
      • 2 Constitutive Activity in the Thyrotropin Receptor
      • 3 Conclusion
      • Conflict of Interest
      • Acknowledgments
    • Chapter Four: Constitutive Activity in Cannabinoid Receptors
      • Abstract
      • 1 Introduction
      • 2 Challenges in Proving Constitutive Receptor Activity
      • 3 Supporting Evidence for Constitutive Activity in Cannabinoid Receptors
      • 4 Conclusion
      • Conflict of Interest
    • Chapter Five: Constitutive Activity in Melanocortin-4 Receptor: Biased Signaling of Inverse Agonists
      • Abstract
      • 1 Introduction
      • 2 Constitutive Activity of MC4R in the Gs-cAMP Pathway
      • 3 Constitutive Activity of MC4R in the ERK1/2 Pathway
      • 4 In Vivo Relevance of the Constitutive Activity of the MC4R
      • 5 Therapeutic Relevance of Inverse Agonism
      • 6 Conclusion
      • Conflict of Interest
      • Acknowledgments
    • Chapter Six: Constitutive Activity in the Angiotensin II Type 1 Receptor: Discovery and Applications
      • Abstract
      • 1 Introduction
      • 2 Discovering Constitutive Activity of AT1 Receptor
      • 3 Mechanism of Constitutive Activation in AT1 Receptor
      • 4 Inverse Agonists and Partial Agonists of AT1 Receptor
      • 5 Constitutive Activity of AT1 Receptor In Vivo
      • 6 Constitutive Activation of AT1 Receptor and Pathophysiology
      • 7 CAM AT1 Receptors as Research Tools
      • 8 Conclusion
      • Conflict of Interest
      • Acknowledgments
    • Chapter Seven: Constitutive Activities and Inverse Agonism in Dopamine Receptors
      • Abstract
      • 1 Introduction
      • 2 Molecular Basis for the Constitutive Activities of D1-Class Receptors
      • 3 Molecular Basis for the Constitutive Activities of D2-Class Receptors
      • 4 Regulation of Constitutive Activities of D1-Class Receptors
      • 5 Physiological and Pathological Relevance of Constitutive Activity for Dopamine Receptors
      • 6 Conclusion
      • Conflict of Interest
      • Acknowledgments
    • Chapter Eight: Receptor Conformation and Constitutive Activity in CCR5 Chemokine Receptor Function and HIV Infection
      • Abstract
      • 1 Introduction
      • 2 CCR5 Signaling Pathways and Evidence for Constitutive Activity of the Wild-Type CCR5 Chemokine Receptor
      • 3 Role of CCR5 Chemokine Coreceptor Conformation in HIV Entry
      • 4 Therapeutic Potential for CCR5 Chemokine Receptor Antagonists and Inverse Agonists
      • 5 Conclusion
      • Conflict of Interest
    • Chapter Nine: Constitutively Active Chemokine CXC Receptors
      • Abstract
      • 1 Introduction
      • 2 Chemokine CXC Receptors
      • 3 Conclusion
      • Conflict of Interest
    • Chapter Ten: Constitutive Activity of Bitter Taste Receptors (T2Rs)
      • Abstract
      • 1 Introduction
      • 2 Activation Mechanism of T2Rs
      • 3 Constitutive Activity in GPCRs
      • 4 Role of CAMs in Discovery of Bitter Taste Blockers
      • 5 Conclusion
      • Conflict of Interest
      • Acknowledgments
    • Chapter Eleven: Constitutive Activity of the Androgen Receptor
      • Abstract
      • 1 Introduction
      • 2 Basic AR Functions
      • 3 Modes of Constitutive and Hypersensitive Activity of Full-Length AR
      • 4 Discovery of Constitutively Active AR Splice Variants
      • 5 Mode of Action of Constitutive Active AR and AR-V in Gene Regulation
      • 6 Targeting Constitutive Activity of AR in PCa
      • 7 Conclusion
      • Conflict of Interest
      • Acknowledgments
    • Chapter Twelve: Sodium Channels, Cardiac Arrhythmia, and Therapeutic Strategy
      • Abstract
      • 1 Introduction
      • 2 Structure and Physiological Function of Cardiac Na+ Channels
      • 3 Cardiac Diseases Associated With Abnormal Na+ Channels
      • 4 Conclusion
      • Conflict of Interest
    • Chapter Thirteen: Constitutive Activity of the Acetylcholine-Activated Potassium Current IK,ACh in Cardiomyocytes
      • Abstract
      • 1 Introduction
      • 2 Molecular Mechanisms of Constitutively Active IK,ACh
      • 3 Constitutively Active IK,ACh as Potential Therapeutic Target
      • 4 Conclusion
      • Conflict of Interest
      • Acknowledgments
    • Index

Product details

  • No. of pages: 440
  • Language: English
  • Copyright: © Academic Press 2014
  • Published: June 11, 2014
  • Imprint: Academic Press
  • Hardcover ISBN: 9780124171978
  • eBook ISBN: 9780124172067

About the Editor

Ya-Xiong Tao

Dr. Ya-Xiong Tao is currently Professor of Physiology at Auburn University College of Veterinary Medicine in Auburn, Alabama, USA. He has been working on several G protein-coupled receptors, including gonadotropin receptors regulating reproduction, and melanocortin receptors regulating energy and glucose homeostasis. He has published extensively in peer-reviewed biomedical journals and obtained funding for his research from National Institutes of Health, American Diabetes Association and American Heart Association, among others. He has delivered numerous lectures at universities and research institutes in USA, Canada, China, India, and Mexico. He has edited ten volumes, including seven volumes in Progress in Molecular Biology and Translational Science. He teaches several courses, including Physiology, Receptorology, Genomics and Personalized Medicine, and Molecular Endocrinology, for veterinarian, graduate, and undergraduate Honors students.

Affiliations and Expertise

Professor of Physiology, College of Veterinary Medicine, Auburn University, AL, USA

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