Agonizing integrin antagonists?
A recent study published in Nature Medicine reports that low-dose treatment with RGD-mimetic integrin inhibitors may paradoxically enhance angiogenesis and tumor growth. This work implies that delivery of these agents should be redesigned in order to avoid nanomolar plasma concentrations and to improve their efficacy to treat human cancers.
Weis
Sara M
SM
Moores UCSD Cancer Center and Department of Pathology, University of California, San Diego, La Jolla, CA 92093, USA.
Stupack
Dwayne G
DG
Cheresh
David A
DA
D000818:Animals; D001567:Benzocycloheptenes / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006801:Humans; D016023:Integrins / Q000037:antagonists & inhibitors*; D009361:Neoplasm Invasiveness; D009369:Neoplasms / Q000097:blood / Q000098:blood supply / Q000188:drug therapy* / Q000473:pathology; D009389:Neovascularization, Pathologic / Q000188:drug therapy* / Q000473:pathology; D010456:Peptides, Cyclic / Q000494:pharmacology*; D015398:Signal Transduction / Q000187:drug effects; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000494:pharmacology
C514976:5-(7-((4-(pyridin-2-ylamino)butyrylamino)methyl)-6,9-dihydro-5H-benzocyclohepten-5-yl)acetic acid; D001567:Benzocycloheptenes; D016023:Integrins; D010456:Peptides, Cyclic; C507169:cyclic arginine-glycine-aspartic acid peptide; D005680:gamma-Aminobutyric Acid