Over the last decade important advances have been made in our understanding of the molecular events underlying cellular responses to extracellular signals. Increased understanding of signal transduction mechanisms and gene regulation involved in cardiovascular diseases has created opportunities for the discovery of novel therapeutic compounds useful for the treatment of cardiovascular disorders. One of the best-studied signalling routes is the mitogen activated protein (MAP) kinase signal transduction pathway, which plays a crucial role in many aspects of cardiovascular responses. Here, our current understanding of the MAP kinase pathway is reviewed, as well as recent advances in the design of novel agents that are able to modulate the activity of these signaling cascades.