Cystamine is a redox-dependent inverse agonist of the histamine H 4 receptor
Abstract
This study identifies cystamine as a previously unrecognized modulator of H4R. Cystamine inhibits mast cell migration and suppresses H4R-mediated Rac-ERK signaling at concentrations far below those required to inhibit transglutaminase, and it exhibits inverse agonist activity. Docking simulations show that cystamine, but not reduced cysteamine, engages the receptor's orthosteric site, revealing a redox-dependent difference in receptor interaction.
Fields of Study & Subjects
Mast cells and histamine
Phagocytosis and Immune Regulation
Erythrocyte Function and Pathophysiology
Publication details
- Journal / source
- American Journal of Physiology-Cell Physiology
- Volume
- 330
- Issue
- 2
- Pages
- C390–C395
- Publication date
- 2 January 2026
- Language
- EN