Apelin and its Receptor: An Overview
Journal Title: Journal of Clinical and Diagnostic Research - Year 2019, Vol 13, Issue 6
Abstract
ABSTRACT 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.
Authors and Affiliations
Rajeev Gandham, ME Sumathi, CD Dayanand, SR Sheela, P Kiranmayee
Keywords
Related Articles
- EP ID EP605017
- DOI 10.7860/JCDR/2019/41074.12930
- Views 129
- Downloads 0
Retroperitoneal Multicystic Mesothelioma in a Young Male
Abstract Multicystic Peritoneal Mesotheliomas (MPMs) are rare tumours characterised by recurrent mesothelial inclusion cysts. Less than 200 cases have been reported worldwide. Only 10 cases have been reported from India....
Bilateral Isolated Nasal Cleft Management: A Facile Solution or a Treatment Conundrum?
ABSTRACT Alar defects are usually secondary to trauma or nasal tumour excision. Congenital alar defects are rare of which isolated bilateral nasal clefts are extremely sparse. Reconstruction of these bilateral nasal cle...
Evaluation of DNA Damage in Type 1 Diabetes Patients
ABSTRACT Introduction: DNA damage due to oxidative stress leads to progression of diabetic complications. The association between DNA damage and diabetes mellitus has prompted to study the extent of DNA damage and factor...
Molluscum Contagiosum of Cervix – A Case Report
Molluscum Contagiosum (MC) is a common viral infection of skin caused by a double stranded DNA Pox virus affecting both adults and children. MC is primarily an infection of school-going children (one to five years), occa...
Dental Students’ Perception of Dentine Hypersensitivity and Awareness about its Management
ABSTRACT Introduction: Dentine hypersensitivity is a common painful oral condition that can interfere with drinking, eating, tooth brushing and even breathing. Successful management depends on the identification and elim...