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Target intelligence / Profile preview
Apelin receptor early endogenous ligand (APELA)
- Target
- APELA
- Molecular classification
- Peptide hormone, Endogenous ligand, Secreted protein
01
Overview
Apelin receptor early endogenous ligand (APELA; also known as Elabela, ELA, or Toddler) is a secreted peptide hormone that acts as an endogenous ligand for the G protein-coupled apelin receptor (APLNR/APJ). APELA is essential for embryonic development of the heart and vasculature, supports pluripotency in human embryonic stem cells via PI3K/AKT pathway activation, and plays a central role in vascular tone regulation, angiogenesis, and maternal cardiovascular adaptation during pregnancy. In disease, loss or dysregulation of APELA is linked to preeclampsia, hypertension, and certain cancers. There are no clinically approved drugs targeting APELA directly, but APLNR agonists and mimetics are being tested for heart failure, acute kidney injury, and pregnancy complications. ELABELA is a candidate biomarker for preeclampsia and cardiovascular conditions, with ongoing research into its safety and therapeutic profile.
- Other names
- ElabelaELAToddlerTDLEndeprotein Elabelaprotein Toddlerapelin receptor early endogenous ligandApela
02
Mechanism of action
Balanced agonist of apelin receptor (APLNR): activates both G protein (G(i)) and beta-arrestin pathways; Modulation of PI3K/AKT/mTOR pathway in stem cells for self-renewal; Stimulation of angiogenesis and cellular migration via APLNR activation
03
Biological functions
Ligand for apelin receptor (APLNR/APJ)Regulation of cardiovascular function and fluid homeostasisEmbryonic heart development and morphogenesisPromotion of angiogenesis and vascular developmentMaintenance of embryonic stem cell self-renewal and pluripotency (PI3K/AKT pathway)Regulation of maternal cardiovascular physiology during pregnancy
04
Disease associations
Cardiovascular disease (including hypertension)Preeclampsia and gestational hypertensionThyroid cancerPotential role in intrauterine growth restriction and other pregnancy-related disorders
05
Safety considerations
Potential for off-target cardiovascular and vascular effects, especially during pregnancyChallenges in developing stable peptide analogs for therapeutic use
06
Interacting drugs
No approved drugs directly targeting APELA itself; experimental small molecule agonists and mimetics under development as APLNR agonists
07
Biomarkers
Circulating ELABELA levels as a possible biomarker for preeclampsia risk and cardiovascular diseases
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