Very late antigen 4 (VLA4) antagonists as anti-inflammatory agents.
In recent years antagonists of very late antigen-4 (VLA4, also known as integrin alpha(4) beta(1)) have shown great promise in treating inflammatory disorders in a number of animal models. The most advanced in this endeavor is a humanized anti-alpha(4) antibody, Antegren, which is in phase II clinical trials for multiple sclerosis. The first reported small-molecule VLA4 antagonist to advance into clinical trials is currently in phase I as an aerosol for treating asthma. A number of peptides, cyclic peptides and peptidomimetics have been disclosed and are in preliminary stages of development.
Lin
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KC
Biogen, Cambridge, MA 02142, USA. KoChung_Lin@Biogen.com
Castro
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AC
D000595:Amino Acid Sequence; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000627:therapeutic use; D000911:Antibodies, Monoclonal / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D003500:Cyclization; D015195:Drug Design; D004341:Drug Evaluation; D006801:Humans; D039041:Integrin alpha4beta1; D016023:Integrins / Q000037:antagonists & inhibitors*; D018716:Molecular Mimicry; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry / Q000627:therapeutic use; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000911:Antibodies, Monoclonal; D039041:Integrin alpha4beta1; D016023:Integrins; D010455:Peptides; D016201:Receptors, Lymphocyte Homing