title: Integrin-based therapeutics: biological basis, clinical use and new drugs.
abstract: Integrins are activatable molecules that are involved in adhesion and signalling. Of the 24 known human integrins, 3 are currently targeted therapeutically by monoclonal antibodies, peptides or small molecules: drugs targeting the platelet αIIbβ3 integrin are used to prevent thrombotic complications after percutaneous coronary interventions, and compounds targeting the lymphocyte α4β1 and α4β7 integrins have indications in multiple sclerosis and inflammatory bowel disease. New antibodies and small molecules targeting β7 integrins (α4β7 and αEβ7 integrins) and their ligands are in clinical development for the treatment of inflammatory bowel diseases. Integrin-based therapeutics have shown clinically significant benefits in many patients, leading to continued medical interest in the further development of novel integrin inhibitors. Of note, almost all integrin antagonists in use or in late-stage clinical trials target either the ligand-binding site or the ligand itself.
authors.affiliation: La Jolla Institute for Allergy and Immunology, 9420 Athena Circle Drive, La Jolla, Califoria 92037, USA, and the Department of Bioengineering, University of California San Diego, 9500 Gilman Drive, La Jolla, California 92093 USA.
authors.forename: Klaus
authors.initials: K
authors.lastname: Ley
authors.affiliation: La Jolla Institute for Allergy and the Immunology, 9420 Athena Circle Drive, La Jolla, Califoria 92037, USA, and the Inflammatory Bowel Disease Center, Division of Gastroenterology, University of California San Diego, 9500 Gilman Drive, La Jolla, California 92093 USA.
authors.forename: Jesus
authors.initials: J
authors.lastname: Rivera-Nieves
authors.affiliation: Immunology and the Inflammatory Bowel Disease Center, Division of Gastroenterology, University of California San Diego, 9500 Gilman Drive, La Jolla, California 92093 USA.
authors.forename: William J
authors.initials: WJ
authors.lastname: Sandborn
authors.affiliation: Division of Haematology-Oncology, Department of Medicine, University of California San Diego, 9500 Gilman Drive, La Jolla, California 92093 USA.
authors.forename: Sanford
authors.initials: S
authors.lastname: Shattil
mesh_terms: D000818:Animals; D000911:Antibodies, Monoclonal / Q000008:administration & dosage* / Q000276:immunology; D001665:Binding Sites / Q000187:drug effects / Q000276:immunology; D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000276:immunology; D002986:Clinical Trials as Topic / Q000379:methods; D055808:Drug Discovery / Q000379:methods / Q000639:trends*; D006801:Humans; D016023:Integrins / Q000037:antagonists & inhibitors* / Q000276:immunology; D009103:Multiple Sclerosis / Q000188:drug therapy / Q000276:immunology
chemical_list: D000911:Antibodies, Monoclonal; D016023:Integrins
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