Introduction: The vascular endothelium is a layer of endothelial cells lining the lumen of blood vessels, lymphatic vessels, the heart and other organs. Normal endothelium protects cardiovascular diseases, while vascular endothelial pathology is the main cause of many cardiovascular diseases. Aim: Here we summarize current knowledge about endothelial function from bench to bedside. Methods: We review the studies demonstrating the significance of vascular endothelium and evaluating the potential role of drugs targeting endothelial function in the management of cardiovascular diseases. Results: Endothelial dysfunction is a discovered phenomenon that makes a significant contribution to the pathophysiology of numerous cardiovascular conditions associated with vasoconstriction, thrombosis and inflammatory conditions. In clinical settings, the assessment of endothelial functions is attracting increasing attention due to its growing importance for cardiovascular diseases. Since cardiovascular endothelial dysfunction is also detected in patients with heart failure, it is expected to play an important role as a predictive predictor of cardiovascular events. Moreover, vascular endothelial function may be the goal of a comprehensive treatment of diseases for the prevention of cardiovascular diseases. Conclusion: Recent publications have highlighted emerging modulators of endothelial functions, and potential therapeutic and diagnostic goals with major clinical consequences.