Handbook of Experimental Pharmacology

Sigma Proteins: Evolution of the Concept of Sigma Receptors

Editors: Kim, Felix J, Pasternak, Gavril (Eds.)

  • Provides an updated perspective on this rapidly evolving field undergoing changes in fundamental concepts of key importance to the discipline of pharmacology 
  • Emphasis is laid on the roles of sigma proteins in pathophysiology and on emergent therapeutic initiatives  
  • New investigators combined with more experienced investigators - as represented by the editors
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eBook $329.00
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Hardcover $419.00
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  • ISBN 978-3-319-65851-3
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About this book

Two sigma receptor subtypes have been proposed, sigma1 and 2. Much of our understanding of this system is based on biochemical and pharmacological characterization of the cloned sigma1 receptor subtype (Sigma1). It has become clear that sigma receptors are not canonical receptors. Sigma1 is highly conserved among mammalian species, however, it does not share significant homology with any other mammalian protein. Although a range of structurally diverse small molecules bind Sigma1 with high affinity, and it has been associated with a broad range of signaling systems, Sigma1 itself has no known signaling or enzymatic activity. The evolution of this field over nearly four decades has more recently led to a fundamental shift in the concept of “sigma receptors” to what may more accurately and generally be called sigma proteins. Largely based on traditional pharmacologic approaches, the Sigma1 protein has been associated with a broad range of signaling systems, including G-protein coupled receptors, NMDA receptors, and ion channels. Sigma proteins have been linked to a range of physiological processes, including intracellular calcium signaling, neuroprotection, learning, memory, and cognition. Emerging genetic, clinical, and mechanism focused molecular pharmacology data demonstrate the involvement of proteins in a range of pathophysiologies and disorders including neurodegenerative disease, pain, addiction, psychomotor stimulant abuse, and cancer. However, an understanding of the physiological role of sigma proteins has remained elusive. Emerging data associate Sigma1 with chaperone-like activities or molecular scaffold functions. This book aims to provide an updated perspective on this rapidly evolving field undergoing changes in fundamental concepts of key importance to the discipline of pharmacology. It focusses on the reported roles of sigma proteins in pathophysiology and on emergent therapeutic initiatives.

About the authors

Felix J Kim PhD, Drexel University, College of Medicine, Pharmacology and Physiology, Philadelphia, USAGavril Pasternak MD Ph., Memorial Sloan-Kettering Cancer Center, Anne Burnett Tandy Chair in Neurology, Molec Pharmacology and Chemistry, New York, USA

Table of contents (12 chapters)

  • Introduction to Sigma Proteins: Evolution of the Concept of Sigma Receptors

    Kim, Felix J.

    Pages 1-11

  • Structural Insights into Sigma1 Function

    Kruse, Andrew

    Pages 13-25

  • 3D Homology Model of Sigma1 Receptor

    Laurini, Erik (et al.)

    Pages 27-50

  • Medicinal Chemistry of σ1 Receptor Ligands: Pharmacophore Models, Synthesis, Structure Affinity Relationships, and Pharmacological Applications

    Weber, Frauke (et al.)

    Pages 51-79

  • Sigma-1 (σ1) Receptor in Memory and Neurodegenerative Diseases

    Maurice, Tangui (et al.)

    Pages 81-108

Buy this book

eBook $329.00
price for USA (gross)
  • ISBN 978-3-319-65853-7
  • Digitally watermarked, DRM-free
  • Included format: PDF, EPUB
  • ebooks can be used on all reading devices
  • Immediate eBook download after purchase
Hardcover $419.00
price for USA
  • ISBN 978-3-319-65851-3
  • Free shipping for individuals worldwide
  • Usually dispatched within 3 to 5 business days.
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Bibliographic Information

Bibliographic Information
Book Title
Sigma Proteins: Evolution of the Concept of Sigma Receptors
Editors
  • Felix J Kim
  • Gavril Pasternak
Series Title
Handbook of Experimental Pharmacology
Series Volume
244
Copyright
2017
Publisher
Springer International Publishing
Copyright Holder
Springer International Publishing AG
eBook ISBN
978-3-319-65853-7
DOI
10.1007/978-3-319-65853-7
Hardcover ISBN
978-3-319-65851-3
Series ISSN
0171-2004
Edition Number
1
Number of Pages
VIII, 330
Number of Illustrations and Tables
32 b/w illustrations, 32 illustrations in colour
Topics