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Cardiovascular disease


Integrin b3 (GPIIIa; CD61); G protein alpha 13 (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 eptifibatide, 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.
Merck & Co. Inc. markets the integrin a2bb3 (GPIIb/IIIa; CD41/CD61) inhibitors Integrilin and Aggrastat tirofiban and Johnson & Johnson markets the CD41/CD61 mAb ReoPro abciximab to prevent thrombosis in cardiovascular indications (see Riding the integrin wave, page 4).

SciBX 6(45); doi:10.1038/scibx.2013.1289
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, Ill.