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Activation and inhibition of G protein-coupled receptors by cell-penetrating membrane-tethered peptides.
Covic L, Gresser AL, Talavera J, Swift S, Kuliopulos A. Covic L, et al. Proc Natl Acad Sci U S A. 2002 Jan 22;99(2):643-8. doi: 10.1073/pnas.022460899. Proc Natl Acad Sci U S A. 2002. PMID: 11805322 Free PMC article.
Classical ligands bind to the extracellular surface of their cognate receptors and activate signaling pathways without crossing the plasma membrane barrier. We selectively targeted the intracellular receptor-G protein interface by using cell-penetra …
Classical ligands bind to the extracellular surface of their cognate receptors and activate signaling pathways without crossin …
Cell-Penetrating Pepducin Therapy Targeting PAR1 in Subjects With Coronary Artery Disease.
Gurbel PA, Bliden KP, Turner SE, Tantry US, Gesheff MG, Barr TP, Covic L, Kuliopulos A. Gurbel PA, et al. Arterioscler Thromb Vasc Biol. 2016 Jan;36(1):189-97. doi: 10.1161/ATVBAHA.115.306777. Arterioscler Thromb Vasc Biol. 2016. PMID: 26681756 Free PMC article. Clinical Trial.
OBJECTIVE: Pepducins are membrane-tethered, cell-penetrating lipopeptides that target the cytoplasmic surface of their cognate receptor. ...CONCLUSIONS: PZ-128 is a promising antiplatelet agent that provides rapid, specific, dose dependent, and reversi …
OBJECTIVE: Pepducins are membrane-tethered, cell-penetrating lipopeptides that target the cytoplasmic surface of …