Clark, AJ; Forfar, R; Hussain, M; Jerman, J; McIver, E; Taylor, D; Chan, L
(2016)
ACTH Antagonists.
Frontiers in Endocrinology, 7.
p. 101.
ISSN 1664-2392
https://doi.org/10.3389/fendo.2016.00101
SGUL Authors: Clark, Adrian John L
Abstract
Adrenocorticotropin (ACTH) acts via a highly selective receptor that is a member of the melanocortin receptor subfamily of type 1 G protein-coupled receptors. The ACTH receptor, also known as the melanocortin 2 receptor (MC2R), is unusual in that it is absolutely dependent on a small accessory protein, melanocortin receptor accessory protein (MRAP) for cell surface expression and function. ACTH is the only known naturally occurring agonist for this receptor. This lack of redundancy and high degree of ligand specificity suggests that antagonism of this receptor could provide a useful therapeutic aid and a potential investigational tool. Clinical situations in which this could be useful include (1) Cushing's disease and ectopic ACTH syndrome - especially while preparing for definitive treatment of a causative tumor, or in refractory cases, or (2) congenital adrenal hyperplasia - as an adjunct to glucocorticoid replacement. A case for antagonism in other clinical situations in which there is ACTH excess can also be made. In this article, we will explore the scientific and clinical case for an ACTH antagonist, and will review the evidence for existing and recently described peptides and modified peptides in this role.
Item Type: |
Article
|
Additional Information: |
Copyright © 2016 Clark, Forfar, Hussain, Jerman, McIver, Taylor and Chan. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
Keywords: |
Cushing’s syndrome, G protein-coupled receptor, adrenocorticotropin hormone, congenital adrenal hyperplasia, high throughput screening, peptide hormone antagonists, receptor antagonism, receptor modelling, adrenocorticotropin hormone, receptor antagonism, Cushing's syndrome, congenital adrenal hyperplasia, high throughput screening, G protein-coupled receptor, receptor modelling, peptide hormone antagonists, Cushing’s syndrome, G protein-coupled receptor, adrenocorticotropin hormone, congenital adrenal hyperplasia, high throughput screening, peptide hormone antagonists, receptor antagonism, receptor modelling |
SGUL Research Institute / Research Centre: |
Academic Structure > Infection and Immunity Research Institute (INII) |
Journal or Publication Title: |
Frontiers in Endocrinology |
ISSN: |
1664-2392 |
Language: |
eng |
Dates: |
Date | Event |
---|
5 August 2016 | Published | 8 July 2016 | Accepted |
|
Publisher License: |
Creative Commons: Attribution 4.0 |
PubMed ID: |
27547198 |
Web of Science ID: |
WOS:000385310500001 |
![](http://static.pubmed.gov/portal/portal3rc.fcgi/2745237/img/27842) |
Go to PubMed abstract |
URI: |
https://openaccess.sgul.ac.uk/id/eprint/108609 |
Publisher's version: |
https://doi.org/10.3389/fendo.2016.00101 |
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