D-arginine oligomers have been widely used as intracellular delivery vectors both in in vitro andin vivo application.Nevertheless,their intemalization pathway is obscure and conficting resultshave been obtained concer...D-arginine oligomers have been widely used as intracellular delivery vectors both in in vitro andin vivo application.Nevertheless,their intemalization pathway is obscure and conficting resultshave been obtained concerning their intracellular distribution.In this study,we demonstrate that octa-D-arginine(r:)undergoes diffuse localization throughout the cytoplasm and nucleus even atlow concentrations and that rs(r:D-arginine)enters the cells via direct membrane translocation,unlike R:(R:L-arginine),of which endocytosis is the major internalization pathway.The observation that Rs and rg enter the cells through two clearly distinct internalization pathways suggests that the backbone stereochemistry affects the uptake mechanism of oligoarginines.展开更多
基金supported by the National High-Tech Research and Development Program of China(863 Program:2008AA02Z107)the National Natural Science Foundation of China(grant no.30800183)the Scientific Research Foundation for the Returned Overseas,Chinese Scholars,State Education Ministry(Y.-H.Zhang).
文摘D-arginine oligomers have been widely used as intracellular delivery vectors both in in vitro andin vivo application.Nevertheless,their intemalization pathway is obscure and conficting resultshave been obtained concerning their intracellular distribution.In this study,we demonstrate that octa-D-arginine(r:)undergoes diffuse localization throughout the cytoplasm and nucleus even atlow concentrations and that rs(r:D-arginine)enters the cells via direct membrane translocation,unlike R:(R:L-arginine),of which endocytosis is the major internalization pathway.The observation that Rs and rg enter the cells through two clearly distinct internalization pathways suggests that the backbone stereochemistry affects the uptake mechanism of oligoarginines.