Pharmaceutical strategies for endoplasmic reticulum-targeting and their prospects of application

Modern drug delivery system (DDS) exerts its unique superiority as to enhancing drug efficacy while reducing their toxicity, which relies heavily on an accurate route of delivery. Based on the fact that most drugs have their own specific target of action, increasing attention is paid to developing strategies for targeting certain tissues, cell lines, and even intracellular structures. Endoplasmic reticulum (ER) is a dynamic and versatile subcellular organelle that participates in multiple physiological and biochemical processes, supporting the survival and homeostasis-maintenance of cells. Genetic or environmental damages may induce ER stress, which is closely coupled to the occurrence and development of many human diseases and even cancers. In this review, recent progress in strategies of direct ER-targeting with specific molecules or carriers are summarized. We also discuss several advances in fields of indirect ER-targeting. This work may provide a deeper understanding over the ER biology and boost the development of precise intracellular regulation, displaying broad prospects of application.