Angiogenesis-driven pathologies, including cancer, are sustained by a preponderance
of angiogenic factors over endogenous inhibitors of new-vessel formation. Restoring this
balance represents a logical therapeutic strategy to treat these pathologies. Therefore,
endogenous inhibitors of angiogenesis, and in particular thrombospondin-1 (TSP-1), are a
powerful source of potential antiangiogenic tools. Different therapeutic approaches have been
proposed to exploit the antiangiogenic properties of TSP-1, including TSP-1 fragments,
synthetic peptides and peptidomimetics, gene therapy strategies and agents that up-regulate
TSP-1 expression. This review focuses on the possibility of exploiting TSP-1 for the design of
antiangiogenic agents, with particular reference on their use in antineoplastic therapies.
