Here, with the goal of effectively treating hypertension and cutting down on the accompanying adverse effects due to systemic activation, we explored the mechanism by which hypertension is caused by dysregulated TRPV4‐KCa2.3 interaction; we also identified a potentially therapeutic small molecule like a pin targeting impaired endothelial TRPV4‐KCa2.3 interaction (Fig 1A). The gene discussed is TRPV4; the disease is hypertensive disorder.