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The major membrane protein on platelets, integrin \u03b1IIb\u03b23, mediates this response by rapidly transiting from its resting to an activated state in which it serves as a receptor for ligands that can bridge platelets together. Monoclonal antibodies, natural products, and small peptides were all shown to inhibit \u03b1IIb\u03b23 dependent platelet aggregation, and these inhibitors became the forerunners of antagonists that proceeded through preclinical testing and into large patient trials to treat acute coronary syndromes, particularly in the context of percutaneous coronary interventions. Three such \u03b1IIb\u03b23 antagonists, abciximab, eptifibatide, and tirofiban, received Food and Drug Administration approval. Over the past 15 years, millions of patients have been treated with these \u03b1IIb\u03b23 antagonists and many lives have been saved by their administration. With the side effect of increased bleeding and the development of new antithrombotic drugs, the use of \u03b1IIb\u03b23 antagonists is waning. Nevertheless, they are still widely used for the prevention of periprocedural thrombosis during percutaneous coronary interventions. This review focuses on the biology of \u03b1IIb\u03b23, the development of its antagonists, and some of the triumphs and shortcomings of \u03b1IIb\u03b23 antagonism.<\/jats:p>","DOI":"10.1161\/circresaha.112.300570","type":"journal-article","created":{"date-parts":[[2013,4,11]],"date-time":"2013-04-11T18:38:02Z","timestamp":1365705482000},"page":"1189-1200","update-policy":"https:\/\/doi.org\/10.1161\/crossmarkpolicy","source":"Crossref","is-referenced-by-count":151,"title":["Integrin \u03b1IIb\u03b23"],"prefix":"10.1161","volume":"112","author":[{"given":"Kamila","family":"Bledzka","sequence":"first","affiliation":[{"name":"From the Department of Molecular Cardiology, Joseph J. 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