Small Peptides

Chemistry, Biology and Clinical Studies


  • A. Dutta, Zeneca Pharmaceuticals, Macclesfield, UK

Series Editor:

  • H. Timmerman

This book covers many of the aspects of peptide research. In chapters dealing with individual peptides, effort has been concentrated on highlighting the approaches that have led to the receptor classification and the discovery of potent agonist and antagonist analogues. Other aspects, e.g. detailed pharmacology and clinical data, are covered in those cases where the peptide products are either approaching the market or are already being sold as drugs (LHRH and Somatostatin). The chapter on peptide formulations is designed to highlight various approaches which may be useful in the delivery of peptides.

In each section, a number of references to reviews has been included so that readers more interested in a particular aspect can easily obtain that information. The book will be of great interest to pharmacologists, pharmacists and medicinal chemists.

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Book information

  • Published: September 1993
  • Imprint: ELSEVIER
  • ISBN: 978-0-444-88655-2

Table of Contents

1. Angiotensin II. Introduction. Receptor subtypes of angiotensin II. Agonist analogues of angiotensin II. Peptide antagonists of angiotensin II. Non-peptide antagonists of angiotensin II. Non-peptide antagonists of angiotensin II acting at the AT2 receptors. 2. Bombesin/gastrin-releasing peptide. Introduction. Antagonists of bombesin/GRP. Conformationally restricted analogues of bombesin. Bombesin/GRP antagonists and cancer. 3. Bradykinin analogues. Introduction. Receptor subtypes of bradykinin. Agonist analogues of bradykinin. Antagonists of bradykinin. Biological profile of hoe 140 and related antagonists. Side effects associated with bradykinin antagonists. 4. Cholecystokinin analogues. Introduction. Distribution and biological functions of cholecystokinin. Cholecystokinin receptor subtypes and receptor-selective ligands. Peptide antagonists of cholecystokinin and gastrin. Non-peptide antagonists of CCK and gastrin. 5. Enkephalin analogues. Introduction. Enzymic inactivation of enkephalins. Early structure activity relationship studies. Agonist analogues displaying analgesic activity. Receptor selective agonist analogues of enkephalins. Antagonists of enkephalins. 6. Luteinising hormone releasing hormone. Introduction. Enzymic degradation of LHRH. SAR of LHRH agonists. SAR of LHRH antagonists. LHRH antagonists and histamine release. Hexapeptide derivatives as LHRH antagonists. Ketaconazole derivatives as LHRH antagonists. Formulations of LHRH and analogues. Pharmacological and clinical studies with LHRH agonists and antagonists. 7. Somatostatin. Introduction. Enzymic degradation of somatostatin and analogues. Agonist analogues of somatostatin. SAR studies. Clinical applications of somatostatin analogues. 8. Tachykinins. Substance P, Neurokinin A and Neurokinin B. Introduction. Receptor subtypes of tachykinins. SAR of the mammalian tachykinins. Antagonists of substance P. Antagonists of neurokinin A and neurokinin B. Non-peptide antagonists of the tachykinins. Biological studies using SP analogues. 9. Inhibitors of Aspartyl Proteases. 1. Renin. Introduction. Inhibitors of renin. 10. Inhibitors of Aspartyl Proteases. 2. HIV Protease. Introduction. Nature of the enzyme. Chemical approaches used in the design of inhibitors. Non-peptide inhibitors of HIV protease. 11. Metallopeptidase (ACE, Enkephalinase and Atriopeptidase) Inhibitors. Introduction. Inhibitors of angiotensin converting enzyme. Inhibitors of enkephalin degrading dipeptidylcarboxypeptidase (enkephalinase). Inhibitors of atriopeptidase. 12. Formulation of Peptides. Introduction. Polymeric controlled drug delivery systems (depot formulations). Improvements in the oral delivery of peptides. Intranasal administration of peptides. Transdermal iontophoretic delivery of peptides. Administration of peptides by ocular, vaginal and rectal routes.

Each chapter concludes with a Summary and Reference section.