Key result
Poor isoform selectivity limits clinical translation of SOCE inhibitors despite therapeutic potential across cardiovascular diseases.
This review highlights the complex spatiotemporal regulation of STIM/Orai-mediated SOCE in cardiovascular diseases and the need for highly specific, isoform-selective inhibitors for clinical translation.
entry that drives vasoconstriction, smooth muscle proliferation, platelet activation, and cardiac hypertrophy. Dysregulated SOCE is closely associated with hypertension, atherosclerosis, pulmonary hypertension, and thromboembolic disorders. However, SOCE is not a simple binary pathway but operates within a complex regulatory network. Beyond the core STIM-Orai axis, auxiliary proteins including transient receptor potential canonical 1 (TRPC1), tetraspanin 18 (Tspan18), tropomyosin 3 (TPM3), SOCE-associated regulatory factor (SARAF), and A-kinase anchoring protein 79/150 (AKAP79/150) modulate SOCE amplitude, kinetics, and downstream signaling in a cell- and context-dependent manner. Moreover, the functional consequences of SOCE are highly heterogeneous: Orai1 protects adult cardiomyocytes but promotes pathological hypertrophy in neonatal cells, posing a therapeutic dilemma. Although preclinical studies have shown efficacy of SOCE inhibitors, clinical translation remains hindered by poor isoform selectivity, suboptimal pharmacokinetics, lack of tissue-specific delivery, disease-stage-dependent effects, and absence of validated biomarkers. Importantly, recent evidence has definitively ruled out amlodipine-induced CRAC channel activation at therapeutic concentrations, confirming it as an experimental artifact. This review systematically summarizes the molecular complexity, functional diversity, and translational barriers of STIM/Orai-mediated SOCE, aiming to inform precision therapeutic strategies for cardiovascular diseases.
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Liao et al. (2026) conducted a review in Cardiovascular diseases (hypertension, atherosclerosis, pulmonary hypertension, cardiac hypertrophy, thromboembolic disorders). STIM/Orai-mediated store-operated calcium entry (SOCE) modulators was evaluated. STIM/Orai-mediated store-operated calcium entry plays a highly heterogeneous role in cardiovascular diseases, with clinical translation of SOCE inhibitors currently hindered by poor isoform selectivity.
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