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Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin
Open accessAbstract
Apelin peptides have recently been identified to be the endogenous ligands for the G protein‐coupled receptor APJ. However, little is known about the physiological roles of this ligand‐receptor pairing. In the present study we investigated the pharmacology of several apelin analogues at the human recombinant APJ receptor using radioligand binding and functional assays. This has led to the identification of key residues in the apelin peptide required for functional potency and binding affinity through structure–activity studies. In particular, we have identified that replacement of leucine in position 5, or arginine in position 2 and 4 of the C‐terminal apelin peptide, apelin‐13, resulted in significant changes in pharmacology. We also investigated the detailed localization of pre‐proapelin and APJ receptor mRNA in a wide range of human, rat and mouse tissues using quantitative RT–PCR, and carried out a detailed immunohistochemical study of the distribution of the APJ receptor in rat brain and spinal cord. Interestingly, the APJ receptor was not only co‐localized in white matter with GFAP in the spinal cord, but was also clearly localized on neurones in the brain, suggesting that this receptor and its peptide may be involved in a wide range of biological process yet to be determined.
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Citations
Cited by
Apelin, a Newly Identified Adipokine Up-Regulated by Insulin and Obesity
Boucher, J., Masri, B., Daviaud, D., Gesta, S., Guigné, C., Mazzucotelli, A., Castan-Laurell, I., Tack, I., Knibiehler, B., Carpéné, C., et al. (2005) · Endocrinology · doi:10.1210/en.2004-1427 · Cited by 910
The exerkine apelin reverses age-associated sarcopenia
Vinel, C., Lukjanenko, L., Batut, A., Deleruyelle, S., Pradère, J.-P., Le Gonidec, S., Dortignac, A., Geoffre, N., Pereira, O., Karaz, S., et al. (2018) · Nature Medicine · doi:10.1038/s41591-018-0131-6 · Cited by 398
Maguire, J. J., Kleinz, M. J., Pitkin, S. L., & Davenport, A. P. (2009) · Hypertension · doi:10.1161/hypertensionaha.109.134619 · Cited by 323
Regulation of apelin mRNA expression by insulin and glucocorticoids in mouse 3T3-L1 adipocytes
Wei, L., Hou, X., & Tatemoto, K. (2005) · Regulatory Peptides · doi:10.1016/j.regpep.2005.08.003 · Cited by 127
Targeting the apelin system for the treatment of cardiovascular diseases
Chapman, F. A., Maguire, J. J., Newby, D. E., Davenport, A. P., & Dhaun, N. (2023) · Cardiovascular Research · doi:10.1093/cvr/cvad171 · Cited by 104
“26,135 Apelin and pre-proapelin are abundantly expressed in the healthy human placenta, 136 with [Pyr 1 ]apelin-13 the commonest isoform.”
Background
Metadata
- Authors
- Medhurst, A. D., Jennings, C. A., Robbins, M. J., Davis, R. P., Ellis, C., Winborn, K. Y., Lawrie, K. W. M., Hervieu, G., Riley, G., Bolaky, J. E., Herrity, N. C., Murdock, P., & Darker, J. G.
- Venue
- Journal of Neurochemistry
- Publisher
- Wiley
- Published
- 2003-02-18
- Volume
- 84
- Issue
- 5
- Pages
- 1162-1172
- ISSN
- 0022-3042 (ISSN-L)
- 1471-4159
- OpenAlex
- W2000993281
- Cited by
- 448
- References
- 0
- FWCI
- 6.98
- Type
- journal article
- Language
- en
- Open access
- bronze
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- CoChat. (2026). Citation check: Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin. https://app.cochat.ai/papers/10.1046/j.1471-4159.2003.01587.x
- The paper
- Medhurst, A. D., Jennings, C. A., Robbins, M. J., Davis, R. P., Ellis, C., Winborn, K. Y., Lawrie, K. W. M., Hervieu, G., Riley, G., Bolaky, J. E., Herrity, N. C., Murdock, P., & Darker, J. G. (2003). Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin. Journal of Neurochemistry. https://doi.org/10.1046/j.1471-4159.2003.01587.x
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