Animal venoms are rich sources of bioactive compounds that possess obvious pharmacological, therapeutic and/or biotechnological values. A majority of these compounds are peptides that mainly target enzymes, membrane receptors or ion channels. These peptides are most often in a size range that allows their production in vitro by chemical synthesis or genetic engineering. Unfortunately, they rarely display the required characteristics in terms of selectivity, affinity, stability and targeting with regard to the desired application. In recent years, a number of structural approaches or strategies have been developed to improve the intrinsic potential of venom peptides. They are reviewed herein for their effectiveness.