Thursday, November 21, 2013
This week in therapeutics
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Integrin b3 (GPIIIa;
nucleotide binding protein (G protein) a13 (GNA13)
Mouse studies suggest
selectively inhibiting CD61 interactions with GNA13 could help prevent
thrombosis with fewer bleeding side effects than marketed CD61 antagonists.
In mouse thrombosis assays, a peptide inhibitor that selectively blocked
binding of Gna13 to the intracellular C terminus of Cd61 suppressed occlusive
thrombosis as effectively as the integrin inhibitor Integrilin
but unlike Integrilin the peptide did not cause secondary bleeding. Next
steps include assessing the inhibitor's subunit specificity toward other b-integrins
as well as toxicity and pharmacology in animal models.
& Co. Inc. markets the integrin a2bb3 (GPIIb/IIIa;
inhibitors Integrilin and Aggrastat
& Johnson markets the CD41/CD61 mAb ReoPro
to prevent thrombosis in cardiovascular indications (see Riding the integrin
wave, page 4).
Published online Nov. 21, 2013
Patent application filed;
available for licensing
Shen, B. et al. Nature;
published online Oct. 27, 2013;
Contact: Xiaoping Du, University of Illinois at Chicago, Chicago,
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