More information on this family may be found on the IUPHAR-DB family and introduction pages.
The apelin receptor (APJ, nomenclature as agreed by NC-IUPHAR on apelin receptors, [9]) responds to apelin, a 36 amino-acid peptide derived initially from bovine stomach. apelin-36, apelin-13 and [Pyr1]apelin-13 are the predominant endogenous ligands which are cleaved from a 77 amino-acid precursor peptide (ENSG00000171388) by a so far unidentified enzymatic pathway [10].
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Receptors 
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Chandrasekaran, B; Dar, O; McDonagh, T. (2008) The role of apelin in cardiovascular function and heart failure. Eur. J. Heart Fail., 10 (8): 725-32. [PMID:18583184]
Davenport, AP; Pitkin, SL; Maguire, JJ. (2007) Apelins. in Encyclopedic Reference of Molecular Pharmacology Edited by Offermanns, S; Rosenthal, W Springer. 201–206
Japp, AG; Newby, DE. (2008) The apelin-APJ system in heart failure: pathophysiologic relevance and therapeutic potential. Biochem. Pharmacol., 75 (10): 1882-92. [PMID:18272138]
Langelaan, DN; Bebbington, EM; Reddy, T; Rainey, JK. (2009) Structural insight into G-protein coupled receptor binding by apelin. Biochemistry, 48 (3): 537-48. [PMID:19123778]
Lee, DK; George, SR; O'Dowd, BF. (2006) Unravelling the roles of the apelin system: prospective therapeutic applications in heart failure and obesity. Trends Pharmacol. Sci., 27 (4): 190-4. [PMID:16530855]
Pitkin, SL; Maguire, JJ; Bonner, TI; Davenport, AP. (2010) International Union of Basic and Clinical Pharmacology. LXXIV. Apelin receptor nomenclature, distribution, pharmacology, and function. Pharmacol. Rev., 62 (3): 331-42. [PMID:20605969]
Sorli, SC; van den Berghe, L; Masri, B; Knibiehler, B; Audigier, Y. (2006) Therapeutic potential of interfering with apelin signalling. Drug Discov. Today, 11 (23-24): 1100-6. [PMID:17129829]
1. Cayabyab, M., Hinuma, S., Farzan, M., Choe, H., Fukusumi, S., Kitada, C., Nishizawa, N., Hosoya, M., Nishimura, O., Messele, T., Pollakis, G., Goudsmit, J., Fujino, M. and Sodroski, J. (2000) Apelin, the natural ligand of the orphan seven-transmembrane receptor APJ, inhibits human immunodeficiency virus type 1 entry. J Virol., 74: 11972-11976. [PMID:11090199]
2. El Messari, S; Iturrioz, X; Fassot, C; De Mota, N; Roesch, D; Llorens-Cortes, C. (2004) Functional dissociation of apelin receptor signaling and endocytosis: implications for the effects of apelin on arterial blood pressure. J. Neurochem., 90 (6): 1290-301. [PMID:15341513]
3. Fan, X., Zhou, N., Zhang, X., Mukhtar, M., Lu, Z., Fang, J., DuBois, G. C. and Pomerantz, R. J. (2003) Structural and functional study of the apelin-13 peptide, an endogenous ligand of the HIV-1 coreceptor, APJ. Biochemistry., 42: 10163-10168. [PMID:12939143]
4. Hosoya, M., Kawamata, Y., Fukusumi, S., Fujii, R., Habata, Y., Hinuma, S., Kitada, C., Honda, S., Kurokawa, T., Onda, H., Nishimura, O. and Fujino, M. (2000) Molecular and functional characteristics of APJ. Tissue distribution of mRNA and interaction with the endogenous ligand apelin. J Biol Chem., 275: 21061-21067. [PMID:10777510]
5. Katugampola, S. D., Maguire, J. J., Matthewson, S. R. and Davenport, A. P. (2001) [(125)I]-(Pyr(1))Apelin-13 is a novel radioligand for localizing the APJ orphan receptor in human and rat tissues with evidence for a vasoconstrictor role in man. Br J Pharmacol., 132: 1255-1260. [PMID:11250876]
6. Kawamata, Y., Habata, Y., Fukusumi, S., Hosoya, M., Fujii, R., Hinuma, S., Nishizawa, N., Kitada, C., Onda, H., Nishimura, O. and Fujino, M. (2001) Molecular properties of apelin: tissue distribution and receptor binding. Biochim Biophys Acta., 1538: 162-171. [PMID:11336787]
7. Lee, D. K., Saldivia, V. R., Nguyen, T., Cheng, R., George, S. R. and O'Dowd, B. F. (2005) Modification of the terminal residue of apelin-13 antagonizes its hypotensive action. Endocrinology., 146: 231-236. [PMID:15486224]
8. Medhurst, A. D., Jennings, C. A., Robbins, M. J., Davis, R. P., Ellis, C., Winborn, K. Y., Lawrie, K. W., Hervieu, G., Riley, G., Bolaky, J. E., Herrity, N. C., Murdock, P. and Darker, J. G. (2003) Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin. J Neurochem., 84: 1162-1172. [PMID:12603839]
9. Pitkin, SL; Maguire, JJ; Bonner, TI; Davenport, AP. (2010) International Union of Basic and Clinical Pharmacology. LXXIV. Apelin receptor nomenclature, distribution, pharmacology, and function. Pharmacol. Rev., 62 (3): 331-42. [PMID:20605969]
10. Tatemoto, K., Hosoya, M., Habata, Y., Fujii, R., Kakegawa, T., Zou, M. X., Kawamata, Y., Fukusumi, S., Hinuma, S., Kitada, C., Kurokawa, T., Onda, H. and Fujino, M. (1998) Isolation and characterization of a novel endogenous peptide ligand for the human APJ receptor. Biochem Biophys Res Commun., 251: 471-476. [PMID:9792798]
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Potency order determined for heterologously expressed human APJ receptor (pD2 values range from 9.5 to 8.6). APJ may also act as a co-receptor with CD4 for isolates of human immunodeficiency virus, with apelin blocking this function [1]. A modified apelin-13 peptide, apelin-13(F13A) was reported to block the hypotensive response to apelin in rat in vivo [7], however, this peptide exhibits agonist activity in HEK293 cells stably expressing the recombinant APJ receptor [3].