Conopeptides from the venoms of marine snails have attracted much interest as leads in drug design. Currently, one drug, Prialt(®), is on the market as a treatment for chronic neuropathic pain. Conopeptides target a range of ion channels, receptors and transporters, and are typically small, relatively stable peptides that are generally amenable to production using solid-phase peptide synthesis. With only a small fraction of the predicted diversity of conopeptides examined so far, these peptides represent an exciting and largely untapped resource for drug discovery. Recent efforts at chemically re-engineering conopeptides to improve their biopharmaceutical properties promise to accelerate the translation of these fascinating marine peptides to the clinic.