Store-Operated Calcium Entry Inhibitors: Structural Diversity, Mechanisms of Action, and Optimization Strategies
- 1Institute of Cytology of Russian Academy of Science, Tikhoretsky Ave. 4, 194064 St. Petersburg, Russia
- 2Center of Genetic Reprogramming and Gene Therapy, Institute of Cytology of Russian Academy of Science, Tikhoretsky Ave. 4, 194064 St. Petersburg, Russia
Abstract
Store-operated calcium entry (SOCE) is a ubiquitous calcium influx pathway critically involved in numerous physiological processes. Dysregulated SOCE contributes to the pathogenesis of cardiovascular disorders, cancer, and neurodegenerative diseases, making SOCE modulators promising therapeutic candidates. This review provides an overview of the major chemical classes of classical SOCE inhibitors that target Orai and STIM proteins. We focus on structure–activity relationships (SARs), mechanisms of action, strategies for enhancing inhibitory potency and selectivity, and discuss the limitations and side-effect profiles of these compounds. This comprehensive analysis identifies SOC channels as promising therapeutic targets and outlines future directions for rational drug design and the development of clinically viable SOCE modulators.
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BibTeX
@article{zakharova2026storeoperated,
title = {{Store-Operated Calcium Entry Inhibitors: Structural Diversity, Mechanisms of Action, and Optimization Strategies}},
author = {Anastasiia A. Zakharova and Dmitriy A. Grekhnev and Elena V. Kaznacheyeva and Vladimir A. Vigont},
journal = {International Journal of Molecular Sciences},
year = {2026},
month = oct,
doi = {10.3390/ijms27209077},
url = {https://www.mdpi.com/1422-0067/27/20/9077},
note = {CC BY 4.0},
}
RIS
TY - JOUR
TI - Store-Operated Calcium Entry Inhibitors: Structural Diversity, Mechanisms of Action, and Optimization Strategies
AU - Anastasiia A. Zakharova
AU - Dmitriy A. Grekhnev
AU - Elena V. Kaznacheyeva
AU - Vladimir A. Vigont
PY - 2026
DA - 2026/10/13
JO - International Journal of Molecular Sciences
DO - 10.3390/ijms27209077
UR - https://www.mdpi.com/1422-0067/27/20/9077
AB - Store-operated calcium entry (SOCE) is a ubiquitous calcium influx pathway critically involved in numerous physiological processes. Dysregulated SOCE contributes to the pathogenesis of cardiovascular disorders, cancer, and neurodegenerative diseases, making SOCE modulators promising therapeutic candidates. This review provides an overview of the major chemical classes of classical SOCE inhibitors that target Orai and STIM proteins. We focus on structure–activity relationships (SARs), mechanisms of action, strategies for enhancing inhibitory potency and selectivity, and discuss the limitations and side-effect profiles of these compounds. This comprehensive analysis identifies SOC channels as promising therapeutic targets and outlines future directions for rational drug design and the development of clinically viable SOCE modulators.
SN - 1422-0067
ER -