Revista Brasileira de Ciências Farmacêuticas
Print version ISSN 1516-9332
SILVA, Thais Horta Álvares da; BUTERA, Anna Paola; LEAL, Daniel Henriques Soares and ALVES, Ricardo José. Angiogenesis inhibitors antitumor agents: pharmacophore models to anb3 antagonists. Rev. Bras. Cienc. Farm. [online]. 2007, vol.43, n.1, pp. 1-17. ISSN 1516-9332. http://dx.doi.org/10.1590/S1516-93322007000100002.
Cancer is one of the leading causes of death. Angiogenesis, the growth of new blood vessels, is essential for tumor development and spreading. Integrins are a family of surface receptors that are involved in angiogenesis. The anb3 integrin plays an important role in tumor angiogenesis. anb3 inhibitors have direct effects to prevent tumor metastases, growth and angiogenesis. In vitro screening of cyclic peptide libraries led to highly active and anb3-selective compounds. Non-peptidic anb3 antagonists were also designed and synthesized. The crystal structure of the anb3 integrin in complex with RGD ligant allowed structure-based rational design of ligands and validation of pharmacophore model to anb3 antagonists.
Keywords : Angiogenesis; Cancer therapy; anb3 integrin antagonists; Integrins.