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 <FONT FACE=Symbol>anb</FONT>3 integrin plays an important role in tumor angiogenesis. <FONT FACE=Symbol>anb</FONT>3 inhibitors have direct effects to prevent tumor metastases, growth and angiogenesis. In vitro screening of cyclic peptide libraries led to highly active and <FONT FACE=Symbol>anb</FONT>3-selective compounds. Non-peptidic <FONT FACE=Symbol>anb</FONT>3 antagonists were also designed and synthesized. The crystal structure of the <FONT FACE=Symbol>anb</FONT>3 integrin in complex with RGD ligant allowed structure-based rational design of ligands and validation of pharmacophore model to <FONT FACE=Symbol>anb</FONT>3 antagonists.
Angiogenesis; Cancer therapy; <FONT FACE=Symbol>anb</FONT>3 integrin antagonists; Integrins
