All Outputs (2)

Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein (2024)
Journal Article
Allison, M., Davie, R. L., Mogg, A. J., Hampton, S. L., Emsley, J., & Stocks, M. J. (2024). Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein. ACS Medicinal Chemistry Letters, 15(4), 501–509. https://doi.org/10.1021/acsmedchemlett.3c00572

Hereditary angioedema (HAE), a rare genetic disorder, is associated with uncontrolled plasma kallikrein (PKa) enzyme activity leading to the generation of bradykinin swelling in subcutaneous and submucosal membranes in various locations of the body.... Read More about Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein.

Aptamer BT200 blocks interaction of K1405-1408 in the VWF-A1 domain with macrophage LRP1 (2024)
Journal Article
Chan Kwo Chion, A., Byrne, C., Atiq, F., Doherty, D., Aguila, S., Fazavana, J., Lopes, P., Karampini, E., Amin, A., Preston, R. J., Baker, R. I., McKinnon, T. A., Zhu, S., Gilbert, J. C., Emsley, J., Jilma, B., & O'Donnell, J. S. (2024). Aptamer BT200 blocks interaction of K1405-1408 in the VWF-A1 domain with macrophage LRP1. Blood, https://doi.org/10.1182/blood.2024024055

Rondaptivan pegol (previously BT200) is a PEGylated RNA aptamer that binds to the A1 domain of VWF. Recent clinical trials demonstrated that BT200 significantly increased plasma VWF-FVIII levels by attenuating VWF clearance. The biological mechanism(... Read More about Aptamer BT200 blocks interaction of K1405-1408 in the VWF-A1 domain with macrophage LRP1.