Pharmacochemistry Library, Volume 19: Small Peptides: Chemistry, Biology, and Clinical Studies focuses on the processes, reactions, properties, and characteristics of peptides, including analogues and proteases. The publication first takes a look at angiotensin II and bombesin/gastrin-releasing peptide. Topics include conformationally restricted analogues of bombesin, non-peptide antagonists of angiotensin II, receptor subtypes of angiotensin II, and bombesin/GRP antagonists and cancer. The text then elaborates on bradykinin, cholecystokinin, and enkephalin analogues. The manuscript examines luteinizing hormone releasing hormone and somatostatin. Topics include enzymic degradation of somatostatin and analogues, clinical applications of somatostatin analogues, and pharmacological and clinical studies with LHRH agonists and antagonists. The formulation of peptides and inhibitors of aspartyl proteases are also mentioned. The book is a valuable source of information for chemists, biologists, and readers interested in small peptides.

Table of Contents



Chapter 1 Angiotensin II

1. Introduction

2. Receptor Subtypes of Angiotensin II

3. Agonist Analogues of Angiotensin II

4. Peptide Antagonists of Angiotensin II

4.1. Modifications of the C-Terminal Phe Residue

4.2. Replacement of the Tyr4 Residue

4.3. N- or C-Terminal Deletions

4.4. Interchanging the Tyr4 and Phe8 Residues

5. Non-Peptide Antagonists of Angiotensin II

5.1. Modifications of the Early Imidazole Leads

5.2. Imidazole-5-Acrylic Acid Derivatives as Antagonists of Angiotensin II

5.3. Imidazo[4,5-b]pyhdine Derivatives as Antagonists of Angiotensin II

5.4. 2-Alkyl Benzimidazole Derivatives as Antagonists of Angiotensin II

5.5. 2-Alkyl-4-(Biphenyl)Methoxyquinoline and 2,6-Dialkyl-4-(Biphenyl)Methoxy Pyridine Derivatives as Antagonists of Angiotensin II

5.6. Naphthalene, Tetrahydronaphthalene, Bromoindole and Bromobenzofuran Derivatives as Antagonists of Angiotensin II

5.7. Angiotensin Antagonists Containing an Aminomethylene Bridge

6. Non-Peptide Antagonists of Angiotensin II Acting at the AT2 Receptor

7. Summary

8. References

Chapter 2 Bombesin/Gastrin-Releasing Peptide

1. Introduction

2. Antagonists of Bombesin/GRP

2.1 Deletion of the C-Terminal Methionine Residue or the Dipeptide Leucylmethionine

2.2 Modification of the Backbone Amide Groups

2.3 Amino Acid Substitutions in Position 12

2.4 Substance P Antagonists as Bombesin Antagonists

3. Conformationally Restricted Analogues of Bombesin

4. Bombesin/GRP Antagonists and Cancer

5. Summary


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© 1993
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