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Updated: Feb 16, 2026

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors
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Published on: June 7, 2016

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Homocysteine directly interacts and activates the angiotensin II type I receptor to aggravate vascular injury

Tuoyi Li1,2, Bing Yu1, Zhixin Liu3

  • 1Department of Physiology and Pathophysiology, School of Basic Medical Sciences, Peking University; Key Laboratory of Molecular Cardiovascular Science, Ministry of Education, Beijing, 100191, China.

Nature Communications
|January 4, 2018
PubMed

Insights

High homocysteine levels worsen vascular injury by activating the angiotensin II type 1 receptor. Blocking this receptor may prevent such damage, offering a new therapeutic strategy for cardiovascular diseases.

Area of Science:

  • Cardiovascular Biology
  • Molecular Pharmacology
  • Vascular Medicine

Background:

  • Hyperhomocysteinemia (HHcy) is a known risk factor for cardiovascular diseases.
  • The precise mechanisms by which HHcy exacerbates vascular injury are not fully understood.

Purpose of the Study:

  • To elucidate the molecular mechanisms linking HHcy and vascular injury.
  • To investigate the role of the angiotensin II type 1 (AT1) receptor in HHcy-induced vascular damage.

Main Methods:

  • Utilized mouse models with genetic AT1 receptor deletion and AT1 receptor blockers.
  • Employed bioluminescence resonance energy transfer (BRET) for receptor conformational analysis.
  • Conducted molecular dynamics and site-directed mutagenesis studies.

Main Results:

  • HHcy-aggravated abdominal aortic aneurysm was abolished in mice lacking or treated with AT1 receptor blockers.
  • Homocysteine directly activates AT1 receptor signaling, displacing angiotensin II.
  • Distinct AT1 receptor conformational changes were observed upon binding of homocysteine versus angiotensin II.

Conclusions:

  • Homocysteine directly binds and activates the AT1 receptor through specific interactions (salt bridge, disulfide bond).
  • Blocking the AT1 receptor is a potential therapeutic strategy to mitigate HHcy-associated vascular injuries, including aneurysms.

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