Covalent or non-covalent interactions with DNA are the basis for many potential biomedical applications of copper complexes, ranging from DNA structural probes and footprinting agents to anticancer drugs to gene delivery. Ideally, a complex binds selectively to a specific DNA sequence, conformation or higher order structure or causes a permanent structural transition or conformational change. The literature in this field has been constantly growing over the past two to three decades as new applications were emerging. This review gives an overview of the state-of-the-art of DNA-binding Cu complexes designed for applications in bioinorganic and medicinal inorganic chemistry, with a focus on the most relevant ligand classes, i.e. amino acids and peptides, phenanthrolines and phenanthroline-like ligands, terpyridines, porphyrins, Schiff bases and (thio)semicarbazones, polyaza macrocycles and tripodal ligands. (C) 2018 Elsevier B.V. All rights reserved.