The rich chemical and structural versatility of transition metal complexes provide numerous novel paths to be pursued in the design of molecules that exert particular chemical of physicochemical effects that could operate over specific biological targets. However, the poor cell permeability of metallodrugs represents an important barrier for their therapeutic use. The conjugation between metal complexes and a functional peptide vector can be regarded as a versatile and potential strategy to improve their bioavailability and accumulation inside cells, and the site selectivity of their effect. This perspective lies on reviewing the recent advances on the design of metallopeptide conjugates for biomedical applications. Additionally, we highlight the studies where this approach has been directed towards the incorporation of redox active metal centers in living organisms for modulating the cellular redox balance, as a tool with application in anticancer therapy

We acknowledge financial support by Consolider Ingenio CSD/CSD2010-00065 from MICINN of Spain. We also thank the Catalan DIUE of the Generalitat de Catalunya (2014 SGR 862). X.R. thanks financial support from INNPLANTA project INP-2011-0059-PCT-420000-ACT1