Identifying 2PHDO as a SOCE inhibitor from Chinese herbal extracts.
Curr Pharm Biotechnol
; 2023 Jun 14.
Article
en En
| MEDLINE
| ID: mdl-37317920
BACKGROUND: STIM- and Orai-mediated store operated calcium entry (SOCE) is a ubiquitous Ca2+ signaling process, crucial for the proper function of immune, muscle and neuronal systems. To treat SOCE-related disorder or diseases of these systems, and to mechanistically dissect activation and function of SOCE, specific SOCE inhibitors are needed. However, strategies for developing new SOCE modifiers are still limited. Methodology: In this study, we identified a novel SOCE inhibitor named 2PHDO from a small pool of Chinese herbal extracts used for treating psoriasis. It could block SOCE and SOCE-mediated NFAT translocation in multiple types of cells with a half inhibitory concentration around 1 µM. At this concentration, 2PHDO was specific for SOCE. Mechanistically, 2PHDO didn't affect the activation of STIM1 or its physical coupling with Orai1. Rather, 2PHDO inhibited SOCE via its actions on Orai1. Results: 2PHDO may serve as a good template for developing new medicines aiming to treat SOCE related diseases. Conclusion: Overall, we proved the feasibility of screening and identification of novel SOCE inhibitors from active monomers of Chinese herbal medicine.
Texto completo:
1
Bases de datos:
MEDLINE
Idioma:
En
Revista:
Curr Pharm Biotechnol
Año:
2023
Tipo del documento:
Article
País de afiliación:
China