Ghaddhab Chiraz, Vuissoz Jean-Marc, Deladoëy Johnny
Endocrinology Service and Research Center, Sainte-Justine University Hospital Center, Department of Pediatrics, Université de Montréal , Montreal, QC , Canada.
Division of Pediatric Endocrinology, University Children's Hospital Basel (UKBB), University of Basel , Basel , Switzerland.
Front Endocrinol (Lausanne). 2017 Feb 8;8:17. doi: 10.3389/fendo.2017.00017. eCollection 2017.
The adrenocorticotropic hormone (ACTH) is a pituitary hormone derived from a larger peptide, the proopiomelanocortin (POMC), as are the MSHs (α-MSH, β-MSH, and γ-MSH) and the β-LPH-related polypeptides (Figure 1A). ACTH drives adrenal steroidogenesis and growth of the adrenal gland. ACTH is a 39 amino acid polypeptide that binds and activates its cognate receptor [melanocortin receptor 2 (MC2R)] through the two regions HFRW and KKRRP. Most POMC-derived polypeptides contain the HFRW sequence that is conserved through evolution. This explains the difficulties in developing selective agonists or antagonists to the MCRs. In this review, we will discuss the clinical aspects of the role of ACTH in physiology and disease, and potential clinical use of selective ACTH antagonists.
促肾上腺皮质激素（ACTH）是一种源自较大肽原阿黑皮素原（POMC）的垂体激素，促黑素（α-MSH、β-MSH和γ-MSH）以及β-促脂素相关多肽也是如此（图1A）。ACTH驱动肾上腺类固醇生成和肾上腺生长。ACTH是一种由39个氨基酸组成的多肽，它通过HFRW和KKRRP这两个区域结合并激活其同源受体[黑皮质素受体2（MC2R）]。大多数源自POMC的多肽都含有在进化过程中保守的HFRW序列。这就解释了开发MCRs选择性激动剂或拮抗剂存在困难的原因。在本综述中，我们将讨论ACTH在生理学和疾病中作用的临床方面，以及选择性ACTH拮抗剂的潜在临床应用。
