Cholinergic Ligand Interactions

Author： Triggle D. J.;Moran J. F.;Barnard E. A.

Publisher： Elsevier Science‎

Publication year： 2014

E-ISBN: 9781483276564

P-ISBN(Paperback): 9780127004501

P-ISBN(Hardback): 9780127004501

Subject： Q2 Cytobiology;Q5 Biochemistry;Q6 Biophysics;Q7 Molecular Biology

Language： ENG

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Description

Cholinergic Ligand Interactions presents the papers read at a symposium held at the State University of New York at Buffalo, 25-26 May 1970. The recent purification and crystallization of acetylcholinesterase together with real progress in the purification of receptor components indicated the desirability of organizing a symposium to discuss not only these aspects but also the structural bases for cholinergic ligand interaction with these macromolecules, the conformational changes involved with ligand binding, the quantitation of cholinergic ligand binding sites, and the roles of acetylcholinesterase and its isozymes in muscle disease.
The volume contains nine chapters and begins with a study on possible conformational changes in acetylcholinesterase. This is followed by separate chapters on the subunits of acetylcholinesterase; in vitro studies with the cholinergic receptor of the eel electroplax; identification and isolation of acetylcholine receptors; assay and properties of essential (junctional) cholinesterases of the rat diaphragm; and structural variations in cholinergic ligands. Subsequent chapters deal with ligand interactions at the muscarinic receptors and changes in cholinesterases isozymes during normal and dystrophic muscle development.

Chapter

Front Cover

Cholinergic Ligand Interactions

Table of Contents

CONTRIBUTORS

PREFACE

CHAPTER 1. THE POSSIBILITY OF CONFORMATIONAL CHANGES IN ACETYLCHOLINESTERASE

THE HYDROLYTIC MECHANISM

ACID TRANSFERRING INHIBITORS

INHIBITION OF ACYLATION

DECARBANYLATION

SUBUNIT STRUCTURE

CONCENTRATION OF ACETYLCIIOLINESTERASE AT A CHOLINERGIC JUNCTION

REFERENCES

CHAPTER 2. STUDIES ON THE SUBUNITS OF ACETYLCHOLINESTRASE

NUMBER OF ACTIVE SITES

TITRATION OF AChE WITH DFP

TITRATION OF AChE WITH o-NPC

SEPARATION OF THE POLYPEPTIDE CHAINS

DISCUSSION

ACKNOWLEDGEMENT

REFERENCES

CHAPTER 3. IN VITRO STUDIES WITH THE CHOLINERGIC RECEPTOR OF THE EEL ELECTROPLAX

IN VITRO EXCITATION OF PURIFIED MEMBRANE FRAGMENTS BY CHOLINERGIC AGONISTS

SOLUBILIZATION OF A PROTEIN WHICH PRESENTS IN VITRO CHARACTERISTIC PROPERTIES OF THE PHYSIOLOGICAL RECEPTOR FOR ACETYLCHOLINE

CHAPTER 4. BINDING OF CHOLINEROIC LICANDS TO ELECTPOPLAXES AND BRAIN TISSUES

References

CHAPTER 5. ASSAY AND PROPERTIES OF ESSENTIAL (JUNCTIONAL) CHOLINESTERASES OF THE RAT DIAPHRAGM

RADIOMETRIC ASSAY OF AChE IN INTACT DIAPHRAGM

EVIDENCE FOR MINIMAL DIFFUSIONAL BARRIERS FOR SUBSTRATES

EVIDENCE THAT THE ASSAY GIVES INFORMATION ABOUT ESSENTIAL ENZYME

SOME PROPERTIES OF SURFACE, MEMBRANE BOUND AChE

REFERENCES

CHAPTER 6. STRUCTURAL VARIATIONS IN CHOLINERGIC LIGANDS

CRYSTAL STRUCTURE ANALYSIS

CONFORMATION

ELECTRONIC STRUCTURE

LIGAND-RECEPTOR INTERACTIONS

ACKNOWLEDGEMENTS

REFERENCES

CHAPTER 7. MULTIPLE LIGAND BINDING SITES AT THE CHOLINERGIC RECEPTOR

AGONIST AND ANTAGONIST BINDING SITES AT THE MUSCARINIC RECEPTOR

REFERENCES

CHAPTER 8. ACETYLCHOLINESTERASE ISOZYMES AND THE MATURATION OF NORMAL AND DYSTROPHIC MUSCLE

MATERIALS AND METHODS

ChE ISOZYMES OF NORMAL MUSCLE

ChE ISOZYMES OF DYSTROPHIC MUSCLE

INNERVATION AND REGULATION OF ChE ACTIVITY

INNERVATION AND INHERITED MUSCULAR DYSTROPHY

ChE ACTIVITY OF CULTURED CELLS

ACKNOWLEDGEMENTS

REFERENCES

CHAPTER 9. CHOLINESTERASES AT INDIVIDUAL NEUROMUSCULAR JUNCTIONS

INTRODUCTION

MEASUREMENT OF THE ENZYMES AT THE ENDPLATES

THE TYPES AND PROPORTIONS OF THE VARIOUS ESTERASES

AMOUNTS OF CHOLINESTERASES AT JUNCTIONS

NORMAL AND DYSTROPHIC CHICKEN MUSCLES

REFERENCES

SUBJECT INDEX

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