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Nat Rev Drug Discov. 2016 Mar;15(3):173-83. doi: 10.1038/nrd.2015.10. Epub 2016 Jan 29.

Integrin-based therapeutics: biological basis, clinical use and new drugs.

Author information

1
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.
2
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.
3
Immunology and the Inflammatory Bowel Disease Center, Division of Gastroenterology, University of California San Diego, 9500 Gilman Drive, La Jolla, California 92093 USA.
4
Division of Haematology-Oncology, Department of Medicine, University of California San Diego, 9500 Gilman Drive, La Jolla, California 92093 USA.

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.

PMID:
26822833
PMCID:
PMC4890615
DOI:
10.1038/nrd.2015.10
[Indexed for MEDLINE]
Free PMC Article

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