Article Figures & Data
Figures
- Fig. 1.
Alignment of human, rat, and mouse apelin receptors. *, identical amino acids, :, conserved amino acid substitution; ., semiconserved amino acid substitution.
- Fig. 2.
Sequence alignment of mammalian, fish and amphibian apelin-36 amino acid sequences. *, identical amino acids; :, conserved amino acid substitution; ., semiconserved amino acid substitution. Residues that differ from the human sequence are highlighted in red.
- Fig. 3.
Amino acid sequence of the endogenous apelin receptor agonists apelin-36 (a), apelin-17 (b), (Pyr1)apelin-13 (c), and apelin-13 (d). Shaded residues are those identical in all peptides. The post-translational modification of the N-terminal glutamate of apelin-13 to pyroglutamate is shown in dark gray. ACE2 cleaves apelin-36 and apelin-13 at the position shown (Vickers et al., 2002). *, residues found to be important for binding and activation of the apelin receptor by apelin-13 (Fan et al., 2003; Medhurst et al., 2003; El Messari et al., 2004).
- Fig. 4.
Cyclic apelin analogs drawn from the sequences reported by Hamada et al. (2008) (a) and Macaluso et al. (2009) (b).
Tables
Family name Apelin receptor Ligand Apelin Official IUPHAR receptor name Apelin receptor Human gene name APLNR Rat gene name aplnr Mouse gene name aplnr Ligand Action Affinity (pIC50) References Apelin-36 Full agonist 8.6–8.3 Hosoya et al., 2000; Kawamata et al., 2001; Fan et al., 2003; Medhurst et al., 2003 Apelin-17 Full agonist 9.0–7.9 Medhurst et al., 2003; El Messari et al., 2004 (Pyr1)apelin-13 Full agonist 8.9–8.0 Hosoya et al., 2000; Medhurst et al., 2003; El Messari et al., 2004 Apelin-13 Full agonist 9.2–8.8 Fan et al., 2003; Medhurst et al., 2003 Ligand Action Affinity (pKd) Reference ALX40–4C Nonspecific antagonist 5.5 Zhou et al., 2003 Apelin-13(F13A) Functional antagonist N.D. Lee et al., 2005 N.D., not determined.
Ligand Affinity (pKD) Expression System Reference [125I]apelin-13 N.D. HEK-293 cells Fan et al., 2003 [125I](Pyr1)apelin-13 9.7–9.2 Human/Rat tissue Katugampola et al., 2001; El Messari et al., 2004 [125I](Pyr1)[Nle75,Tyr77]apelin-13 8.4–10.7 CHO-A10 cells/HEK-293 cells Hosoya et al., 2000; Hashimoto et al., 2005 [3H](Pyr1)[Met(O)11]apelin-13 8.6 HEK-293 cells Medhurst et al., 2003 [125I][Nle75,Tyr77]apelin-36 11.2 CHO-A10 cells Kawamata et al., 2001 N.D., not determined.
In this issue
International Union of Basic and Clinical Pharmacology. LXXIV. Apelin Receptor Nomenclature, Distribution, Pharmacology, and Function
Jump to section
- Article
- Abstract
- I. Introduction
- II. The Apelin Receptor: Recommendations for Nomenclature
- III. Receptor Structure
- IV. Endogenous Agonists
- V. Receptor Distribution
- VI. Apelin Peptide Distribution
- VII. Synthetic Agonists
- VIII. Antagonists
- IX. Radiolabeled Ligands
- X. Physiological Roles
- XI. Pathophysiological Roles
- XII. Single-Nucleotide Polymorphisms
- XIII. Knockout Mouse Models
- XIV. Conclusion
- Acknowledgments.
- Footnotes
- References
- Figures & Data
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