Background: In vitro (1R,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val (MTCA-KKV) adheres activated platelets, targets P-selectin and GPIIb/IIIa. This led to the development of MTCA-KKV as thrombus targeting nano-medicine. Methods: MTCA-KKV was characterized by nano-feature, anti-thrombotic activity, thrombolytic activity, thrombus target and targeting release. Results: In vivo 0.01 μmol/kg of MTCA-KKV formed nano-particles less than 100 nm in diameter, targeted thrombus, released anti-thrombotic and thrombolytic pharmacophores, prevented thrombosis and dissolved blood clots. Conclusion: Based on the profiles of targeting thrombus, targeting release, inhibiting thrombosis and dissolving blood clots MTCA-KKV is a promising nano-medicine.
Zhao, S., Li, Z., Huang, F., Wu, J., Gui, L., Zhang, X., … Zhao, M. (2019). Nano-scaled MTCA-KKV: For targeting thrombus, releasing pharmacophores, inhibiting thrombosis and dissolving blood clots in vivo. International Journal of Nanomedicine, 14, 4817–4831. https://doi.org/10.2147/IJN.S206294