Abstract
The cystic fibrosis transmembrane conductance regulator (CFTR) gets activated via the cAMP signaling pathway and is present in various secretory epithelial cells, including conjunctival and corneal epithelial cells. Activation of CFTR leads to fluid secretion in both mouse and human ocular surfaces. Dry eye disease is a significant health problem for which limited therapeutic options are available. In this review, on the one hand, small molecule CFTR activators with different chemical structures are summarized, and on the other hand, the pharmacological activity test and structural optimization of small molecule CFTR activators in the treatment of dry eye are outlined. The purpose of this review is to highlight the important role of CFTR activators in the treatment of dry eye disease and their potential as a new strategy for the treatment of dry eye disease.