2018
DOI: 10.1002/pep2.24064
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Apelins, ELABELA, and their derivatives: Peptidic regulators of the cardiovascular system and beyond

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 lig… Show more

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Cited by 7 publications
(6 citation statements)
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References 129 publications
(194 reference statements)
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“…The X‐ray structure of the apelin receptor complexed with a macrocyclic apelin‐17 analog (AMG3054) was reported recently . This follows several studies of either the ligand in solution, individual transmembrane domains by solution NMR, or site‐directed mutagenesis, as summarized recently . Altogether, these studies provide invaluable structural information on the binding and dynamics of the receptor.…”
Section: Toward Pharmacological Probes and Novel Drugsmentioning
confidence: 70%
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“…The X‐ray structure of the apelin receptor complexed with a macrocyclic apelin‐17 analog (AMG3054) was reported recently . This follows several studies of either the ligand in solution, individual transmembrane domains by solution NMR, or site‐directed mutagenesis, as summarized recently . Altogether, these studies provide invaluable structural information on the binding and dynamics of the receptor.…”
Section: Toward Pharmacological Probes and Novel Drugsmentioning
confidence: 70%
“…This class of modifications also increased plasma stability. Furthermore, aromatic amino acid substitutions of the C‐terminal residue also identified a determinant of signaling, likely associated with the presence of multiple aromatic residues on several transmembrane domains in that area of the binding pocket (i.e., residues Y35, W85, Y88, Y93, and Y299), as observed in the recently reported X‐ray structure of the stabilized apelin receptor (modifications include N‐ and C‐terminus truncations as well as the mutations V117A and W126K) complexed with a macrocyclic apelin‐17 derivative . Additional work in this area relied on the introduction of Pro12Aib and Phe13(4‐Br)Phe, which were beneficial for plasma stability of apelin‐13 and apelin‐17 .…”
Section: Toward Pharmacological Probes and Novel Drugsmentioning
confidence: 78%
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“…(Pyr)-apelin-13 is the most abundant isoform in human plasma and cardiac tissue and is therefore used in this study [19,20]. Apelin-APJ signaling is important for cardiovascular regulation [21][22][23][24][25]. In addition, apelin is an adipokine, a bioactive mediator secreted by adipocytes and therefore, apelinmediated signaling pathways are promising therapeutic targets in different metabolic pathologies [23,24,26].…”
Section: Introductionmentioning
confidence: 99%