Fullerene derivatives superfamily attracts a serious attention of pharmacologists since some of these variable agents were proven to be not only drug delivery carriers but anti - cancer and immunomodulators as well. Most specifically, photodynamic therapies of malignant tumors are known for the fullerenes engagement. However, there is an obvious deficit of information on the cellular and molecular mechanisms of the fullerenes pharmacological effects which is a true obstacle on the way leading to practical medicinal use of the latters. Particularly, the mode of both direct (immediate) and distant side effects origin along with a fullerenes impact on necrosis, apoptosis and cell proliferation processes are no doubt needed to get far more clearified. It is hardly possible to exaggerate a significance of the fullerene nanoparticles functionalization type, their sizes and surface nanotopology for further promoting of either cytoprotective or cytotoxic effects. Noteworthy, the antioxidant properties of some water soluble fullerene derivatives were revealed while the fullerenes induced ROS formation might be also occurred. One of the most intriguing peculiarity of the fullerenes as pharmacophores consists in capabilities of some of them to intervene into the structure domains of functional proteins including enzymes and organelles linked receptors as well as to play a role of intercalators interacting with DNA double helix which, in turn, leads to a number of crucial consequences such as the biopolymer conformational flexibility shifts, catalytic activity changes, ligand docking affinity impacts in cell signaling pathways. Last not least, the fullerens are about to compete with several natural metabolites and effectots which is itself a valid platform for pharmacological outreach. This Review deals with an Authors’s original attempt to analyse the above mentioned points with an aim to elucidate those properties, methodological and structural, of numerous fullerene adducts that determine their apoptosis- and cell proliferation – modulating effects with a special respect to a target cell / tumor type
