Living cells may be modified in diverse ways by the combined action of visible light and photosensitizing molecules. The effects appear most frequently as disruptions of subcellular structure, changes in surface membrane function or inhibition of mitotic ability. This review concentrates on the four most thoroughly studied cell types—yeast cells, nerve cells, erythrocytes, and cultured tumor cells. Research on these cells indicates that potency of sensitization depends at least as much on the factors affecting an association between sensitizer and cell prior to illumination as on photochemical properties. While sensitizers which permeate may lead to altered DNA, it appears that surface membrane modification occurs simultaneously and may be critical in the inactivation mechanism. There is much circumstantial evidence suggesting that excited singlet molecular oxygen acts as an intermediate between photoexcited sensitizer and target alteration. Proteins, lipids, and nucleic acids are all susceptible to photosensitized attack, but the correlation between cellular and molecular modification remains ill‐defined. The use of the photodynamic process as a therapeutic technique, particularly in the treatment of malignant tumors, holds great promise, but awaits further research to develop greater selectivity of action.