Biotinyl analogues of amylin as biologically active probes for amylin/CGRP receptor recognition

Chantry, Andrew; Foot, Elizabeth; Leighton, Brendan; Day, Anthony J.; Willis, Antony C.

doi:10.1016/0014-5793(92)80362-k

Cited by 2 publications

(1 citation statement)

References 16 publications

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“…However, modification of Lys 1 with the addition of a biotin moiety was accommodated when an eight‐atom spanning bridge was included between the Lys‐NH 2 group and the biotin C‐terminus. The resulting analogue retained similar activity to rat amylin (Chantry et al ., ). The activity of any of these analogues at defined amylin receptor subtypes is not known.…”

Section: Structure/function – Detailed Informationmentioning

confidence: 97%

Amylin structure–function relationships and receptor pharmacology: implications for amylin mimetic drug development

Bower

Hay

2016

British J Pharmacology

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Amylin is an important, but poorly understood, 37 amino acid glucoregulatory hormone with great potential to target metabolic diseases. A working example that the amylin system is one worth developing is the FDA-approved drug used in insulin-requiring diabetic patients, pramlintide. However, certain characteristics of pramlintide pharmacokinetics and formulation leave considerable room for further development of amylin-mimetic compounds. Given that amylin-mimetic drug design and development is an active area of research, surprisingly little is known about the structure/function relationships of amylin. This is largely due to the unfavourable aggregative and solubility properties of the native peptide sequence, which are further complicated by the composition of amylin receptors. These are complexes of the calcitonin receptor with receptor activity-modifying proteins. This review explores what is known of the structure-function relationships of amylin and provides insights that can be drawn from the closely related peptide, CGRP. We also describe how this information is aiding the development of more potent and stable amylin mimetics, including peptide hybrids.

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Section: Structure/function – Detailed Informationmentioning

confidence: 97%

Amylin structure–function relationships and receptor pharmacology: implications for amylin mimetic drug development

Bower

Hay

2016

British J Pharmacology

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Amylin and Related Proteins: Physiology and Pathophysiology

Cooper

2001

Comprehensive Physiology

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The sections in this article are: Protein Chemistry of Amylin Isolation, Structure, Nomenclature, and Evolutionary Relationships Chemical Synthesis Molecular Structure of Soluble Amylin Amylin as the Monomer of Islet Amyloid Molecular Biology Preproamylin Structure and Chromosomal Location of the Human Amylin Gene A Disease‐Associated Mutation in Human Amylin Biosynthesis and Secretion of Amylin Measurement of Amylin Concentrations Tissue Localization and Content Regulation of Biosynthesis Amylin in Extra‐Islet Tissues Circulating Concentrations and Pancreatic Secretion Effects of Secretion Modulators Amylin Secretion in Humans The Amylin Family: Role in the Regulation of Fuel Metabolism Insulin Resistance In Vivo Actions in Skeletal Muscle Role of Calcitonin Gene‐Related Peptide in Skeletal Muscle Metabolism Actions in the Liver Adipose Tissue Regulation of Pancreatic Function Endocrine Pancreas Exocrine Pancreas Regulation of The Gastrointestinal Tract Effects on Gastric Function Intestinal Function Actions in The Central Nervous System: Modulation of Appetite Actions in The Cardiovascular System Calcitonin Gene‐Related Peptide Adrenomedullin Biological Actions of Adrenomedullin in the Cardiovascular System Vascular Actions of Amylin Renal Function Role of Amylin in the Regulation of Renal Function Adrenomedullin: Roles in Renal Function and Sodium Homeostasis Effects on Calcium Metabolism and Bone Actions of Amylin Other Biological Actions Respiratory System Effects in Endocrine Tissues Other than Pancreas Effects in the Immune System Receptors for Amylin and Related Proteins Receptor Nomenclature Pharmacological and Biochemical Studies Calcitonin Receptors Specific Calcitonin Gene‐Related Peptide Binding Sites that Can Interact with Amylin Amylin Binding to Skeletal Muscle and Liver Biochemical Characterization of Putative Amylin and Calcitonin Gene‐Related Peptide Receptors Disease Associations Insulin‐Dependent Diabetes Mellitus Animal Models of Insulin Resistance, Obesity, and Diabetes Obesity and Non‐Insulin‐Dependent Diabetes Mellitus in Humans Other Diabetic Syndromes Amylin in Endocrine Neoplasms Relationship to Aging Other Diseases Conclusion and Future Prospects

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Biotinyl analogues of amylin as biologically active probes for amylin/CGRP receptor recognition

Cited by 2 publications

References 16 publications

Amylin structure–function relationships and receptor pharmacology: implications for amylin mimetic drug development

Amylin structure–function relationships and receptor pharmacology: implications for amylin mimetic drug development

Amylin and Related Proteins: Physiology and Pathophysiology

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