Mitochondria, an eukaryotic organelle, is regarded as the most critical target since it regulates several vital functions in cell physiology. It is the hub of metabolic activity and a source of fascination due to its role in a variety of diseases like cardiovascular, cancer and neurological disorders. Because of the structural and functional discrepancies between normal and cancerous mitochondria (respiratory rate, membrane potential, genetic mutations and energy-producing pathway), mitochondria have garnered substantial attention in cancer therapy. For delivering cytotoxins exclusively to mitochondria, several synthetic strategies are used for mitochondrial dysfunction and cell apoptosis/necrosis. Covalent binding of lipophilic cations (triphenylphosphonium ion, rhodamine, peptides etc) to the molecular-based pharmacophore is the most effective process. Significant mitochondrial accumulations (>1000 folds) can be accomplished by proper selection of cell types, their mitochondrial membrane potential and targeting unit. In this review article, we address various strategies for targeting small molecule-based theranostics to cancerous mitochondria for diagnostic and potential therapeutic purposes that have been published since 2015. Particularly, conventional chemotherapeutic drugs, photosensitizers for photodynamic and photothermal treatment, drug-free agents, intra-mitochondrial aggregation agents and their combination are among the molecular-based agents discussed.
- Drug delivery
ASJC Scopus subject areas
- Physical and Theoretical Chemistry
- Inorganic Chemistry
- Materials Chemistry