Fullerenes have been considered as excellent candidates for photosensitizers (PSs) in photodynamic therapy (PDT). Fullerenes are reported to generate reactive oxygen species (ROSs), through energy transfer (singlet oxygen 1O2, Type II reaction) and electron transfer (reduced active oxygen radicals such as superoxide anion radical O2-• and hydroxyl radical •OH, Type I reaction) in an effective way (Figure 1a).1,2 In our previous study, we reported the synthesis of fullerene-PEG conjugates and demonstrated their ability for photoinduced DNA damage and ROS generation upon visible light irradiation.2 In this work, we report the synthesis of a highly water-soluble fullerene-peptide conjugate. The fullerene-peptide conjugates are well-dispersed in aqueous media in comparation to fullerene-PEG conjugates, as indicated by dynamic light scattering (DLS) measurement as well as cryo-TEM microscopy. The ROSs generation capacity of fullerene-peptide conjugate, detected by electron paramagnetic resonance (EPR), DNA damage and in vitro photocytotoxicity tests will also be presented. Figure 1