Apelin and its Receptor: An Overview
Apelin protein is an endogenous ligand of Apelin Receptor (APJ). APJ is a member of G-protein coupled receptor family. Both apelin and its receptor express extensively in the human body. Apelin receptor activation occurs by its cognate peptide ligand, apelin and many physiological effects, including...
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| Format: | Article |
| Language: | English |
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JCDR Research and Publications Private Limited
2019-06-01
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| Series: | Journal of Clinical and Diagnostic Research |
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| Online Access: | https://jcdr.net/articles/PDF/12930/41074_CE[Ra1]_F(SL)_PF1(AG_SHU)_PFA(SL)_PB(AG_SL)_PN(SL).pdf |
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| author | Rajeev Gandham ME Sumathi CD Dayanand SR Sheela P Kiranmayee |
| author_facet | Rajeev Gandham ME Sumathi CD Dayanand SR Sheela P Kiranmayee |
| author_sort | Rajeev Gandham |
| collection | DOAJ |
| description | Apelin protein is an endogenous ligand of Apelin Receptor (APJ). APJ is a member of G-protein coupled receptor family. Both apelin and its receptor express extensively in the human body. Apelin receptor activation occurs by its cognate peptide ligand, apelin and many physiological effects, including vasodilation, vasoconstriction, angiogenesis, fluid homeostasis, neuroendocrine response to stress and energy metabolism. Apelin derived from its precursor might yield a number of bioactive peptides. Apelin is synthesised as an immature single peptide (preproapelin) which consists of 77 amino acids. In the endoplasmic reticulum, preproapelin is cleaved by endopeptidases to a 55 amino acid proapelin and subsequently, to various biologically active apelin-36, apelin-17 and apelin-13 isoforms. Post-translation, the apelin containing the pyroglutamate group at N-terminus of the peptide is modified to pyroglutamate apelin 13. In adipocytes, proprotein convertase subtilisin/kexin 3 directly cleaves the proapelin to apelin 13 and does not produce any longer isoforms. In contrast, Angiotensin Converting Enzyme 2- (ACE-2) cleaves at proline-phenylalanine site at C-terminus and renders apelin 13 and apelin 36 inactive. To date, ACE-2 is the only known enzyme for apelin degradation. The C-terminal region is responsible for receptor binding and subsequent activation. Prior research suggests the role of apelin and its receptor in pathogenesis of various conditions including preeclampsia, hypertension, cardiovascular diseases, diabetes mellitus, obesity and cancer. Despite its established importance and link to therapeutic target, the precise role of this apelin/APJ remain obscure. In this attempt, we summarised the structure, chemistry, biosynthesis, expression and gene regulation, distribution, receptor binding mechanism, biological functions and therapeutic applications along with the associated recent advances. |
| first_indexed | 2024-04-12T06:39:36Z |
| format | Article |
| id | doaj.art-d39e0a445ef64ab1b04eb746d5f2ab54 |
| institution | Directory Open Access Journal |
| issn | 2249-782X 0973-709X |
| language | English |
| last_indexed | 2024-04-12T06:39:36Z |
| publishDate | 2019-06-01 |
| publisher | JCDR Research and Publications Private Limited |
| record_format | Article |
| series | Journal of Clinical and Diagnostic Research |
| spelling | doaj.art-d39e0a445ef64ab1b04eb746d5f2ab542022-12-22T03:43:45ZengJCDR Research and Publications Private LimitedJournal of Clinical and Diagnostic Research2249-782X0973-709X2019-06-01136BE01BE0610.7860/JCDR/2019/41074.12930Apelin and its Receptor: An OverviewRajeev Gandham0ME Sumathi1CD Dayanand2SR Sheela3P Kiranmayee4PhD Scholar, Department of Biochemistry, Sri Devaraj Urs Medical College, SDUAHER, Tamaka, Kolar, Karnataka, India.Professor and Head, Department of Biochemistry, Sri Devaraj Urs Medical College, SDUAHER, Tamaka, Kolar, Karnataka, India.Professor, Head of Allied Health Sciences, Department of Biochemistry, Sri Devaraj Urs Medical College, SDUAHER, Tamaka, Kolar, Karnataka, India.Professor and Head, Department of Obstetrics and Gynaecology, Sri Devaraj Urs Medical College, SDUAHER, Tamaka, Kolar, Karnataka, India.Assistant Professor, Department of Cell Biology and Molecular Genetics, Sri Devaraj Urs Medical College, SDUAHER, Tamaka, Kolar, Karnataka, India.Apelin protein is an endogenous ligand of Apelin Receptor (APJ). APJ is a member of G-protein coupled receptor family. Both apelin and its receptor express extensively in the human body. Apelin receptor activation occurs by its cognate peptide ligand, apelin and many physiological effects, including vasodilation, vasoconstriction, angiogenesis, fluid homeostasis, neuroendocrine response to stress and energy metabolism. Apelin derived from its precursor might yield a number of bioactive peptides. Apelin is synthesised as an immature single peptide (preproapelin) which consists of 77 amino acids. In the endoplasmic reticulum, preproapelin is cleaved by endopeptidases to a 55 amino acid proapelin and subsequently, to various biologically active apelin-36, apelin-17 and apelin-13 isoforms. Post-translation, the apelin containing the pyroglutamate group at N-terminus of the peptide is modified to pyroglutamate apelin 13. In adipocytes, proprotein convertase subtilisin/kexin 3 directly cleaves the proapelin to apelin 13 and does not produce any longer isoforms. In contrast, Angiotensin Converting Enzyme 2- (ACE-2) cleaves at proline-phenylalanine site at C-terminus and renders apelin 13 and apelin 36 inactive. To date, ACE-2 is the only known enzyme for apelin degradation. The C-terminal region is responsible for receptor binding and subsequent activation. Prior research suggests the role of apelin and its receptor in pathogenesis of various conditions including preeclampsia, hypertension, cardiovascular diseases, diabetes mellitus, obesity and cancer. Despite its established importance and link to therapeutic target, the precise role of this apelin/APJ remain obscure. In this attempt, we summarised the structure, chemistry, biosynthesis, expression and gene regulation, distribution, receptor binding mechanism, biological functions and therapeutic applications along with the associated recent advances.https://jcdr.net/articles/PDF/12930/41074_CE[Ra1]_F(SL)_PF1(AG_SHU)_PFA(SL)_PB(AG_SL)_PN(SL).pdfangiogenesisangiotensin converting enzyme-2apelin receptorg-protein coupled receptorvasodilator |
| spellingShingle | Rajeev Gandham ME Sumathi CD Dayanand SR Sheela P Kiranmayee Apelin and its Receptor: An Overview Journal of Clinical and Diagnostic Research angiogenesis angiotensin converting enzyme-2 apelin receptor g-protein coupled receptor vasodilator |
| title | Apelin and its Receptor: An Overview |
| title_full | Apelin and its Receptor: An Overview |
| title_fullStr | Apelin and its Receptor: An Overview |
| title_full_unstemmed | Apelin and its Receptor: An Overview |
| title_short | Apelin and its Receptor: An Overview |
| title_sort | apelin and its receptor an overview |
| topic | angiogenesis angiotensin converting enzyme-2 apelin receptor g-protein coupled receptor vasodilator |
| url | https://jcdr.net/articles/PDF/12930/41074_CE[Ra1]_F(SL)_PF1(AG_SHU)_PFA(SL)_PB(AG_SL)_PN(SL).pdf |
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