Apelin receptor C
Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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The apelin receptor (nomenclature as agreed by the NC-IUPHAR Subcommittee on the apelin receptor [18] and subsequently updated [20]) responds to apelin, a 36 amino-acid peptide derived initially from bovine stomach. Apelin-36 (APLN, Q9ULZ1), apelin-13 (APLN, Q9ULZ1) and [Pyr1]apelin-13 (APLN, Q9ULZ1) are the predominant endogenous ligands which are cleaved from a 77 amino-acid precursor peptide (APLN, Q9ULZ1) [22]. A second family of peptides discovered independently and named Elabela [5] or Toddler, that has little sequence similarity to apelin, is present, and functional at the apelin receptor in the adult cardiovascular system [17,25]. The enzymatic pathways generating biologically active apelin and Elabela isoforms have not been determined but both propeptides include sites for potential proprotein convertase processing [21]. Structure-activity relationship Elabela analogues have been described [16,23]. The stoichiometry of apelin receptor-heterotrimeric G protein complexes has been studied using cryogenic-electron microscopy [26].
Receptors
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apelin receptor
C
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Concise Guide to PHARMACOLOGY citation:
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors. Br J Pharmacol. 176 Suppl 1:S27-S156.
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Potency order determined for heterologously expressed human apelin receptor (pD2 values range from 9.5 to 8.6). The apelin receptor may also act as a co-receptor with CD4 for isolates of human immunodeficiency virus, with apelin blocking this function [3]. A modified apelin-13 peptide, apelin-13(F13A) was reported to block the hypotensive response to apelin in rat in vivo [13], however, this peptide exhibits agonist activity in HEK293 cells stably expressing the recombinant apelin receptor [8]. The apelin receptor antagonist, MM54, was reported to suppress tumour growth and increase survival in an intracranial xenograft mouse model of glioblastoma [9].