Apelins, ELABELA, and their derivatives: Peptidic regulators of the cardiovascular system and beyond. Issue 1 (30th March 2018)

• Record Type: Journal Article
• Authors: Murza, Alexandre; Trân, Kien; Bruneau‐Cossette, Laurent; Lesur, Olivier; Auger‐Messier, Mannix; Lavigne, Pierre; Sarret, Philippe; Marsault, Éric
• Other Names: Lubell William D. guestEditor.
• Is Part Of: Peptide science. Volume 111:Issue 1(2019)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2018-03-30
• Subjects: apelin -- APJ receptor -- cardiovascular diseases -- ELABELA -- Toddler; Peptides -- Periodicals; 572.6505
• DOI: 10.1002/pep2.24064
• Languages: English
• ISSNs: 2475-8817

Abstract

Abstract: The apelinergic system emerges as an important regulator of cardiovascular functions via its actions on the heart, vasculature, and kidney. It also possesses additional beneficial properties, via its actions on the pancreas and skeletal muscle, on type 2 diabetes. The apelinergic system distinguishes itself by the presence of two structurally distinct sets of endogenous ligands, the Apelins (–13, −17, and −36) and Elabela, which both activate the apelin (APJ) receptor. In the past decade, numerous peptidic ligands have been used to better understand the structure–activity relationship of apelin (and more recently Elabela), providing important tools to rationalize how ligand modifications impact receptor structure and dynamics as well as its downstream signaling. The recently disclosed structure of the apelin receptor in complex with an analogue of apelin‐17 provides an important tool in this quest. In this review, we first summarize the physiopharmacology of the apelinergic system, then, review existing knowledge on the various ligands of the apelin receptor with an emphasis on peptidic ligands, although small molecules are covered as well. Throughout this work, we tried to integrate existing knowledge of ligands' pharmacological profiles with structure and signaling profile. Abstract :