Since its serendipitous discovery over 30 years ago, the translocator protein (18 kDa) has been demonstrated to play an important role in a multitude of critical biological processes. Although implemented as a novel therapeutic and diagnostic tool for a variety of disease states, its most promising role is as a molecular target for anticancer treatments such as photodynamic therapy (PDT). This review gives an overview of the attempts made by researchers to design porphyrin-based photosensitizers for use as anticancer therapeutics in PDT as well as improved imaging agents for diagnostic purposes. With a better understanding of the structure and function of the translocator protein, the synthesis of porphyrins for use in PDT with optimum binding affinities will become ever more possible.