公开(公告)号：EP2575848A2

公开(公告)日：2013-04-10

申请号：EP11789344.6

申请日：2011-05-26

申请人： Ben-Gurion University of The Negev Research and Development Authority

发明人： DAVID, Ayelet ,  ASHKENASY, Gonen ,  SHAMAY, Yossi

IPC分类号： A61K38/00 ,  C07K1/00

CPC分类号： C07K9/001 ,  A61K47/32 ,  A61K47/64 ,  A61K49/0002 ,  A61K49/0056

摘要： The caged cell-penetrating peptide (cCPP) conjugates of this invention are ideal for intracellular delivery of a broad variety of cargoes including various nanoparticulate pharmaceutical carriers (liposomes, micelles, microparticles, nanoparticles, polymer-conjugates). The conjugates comprise a detectable agent or a therapeutic agent, and the conjugates provide a novel strategy for site-specific delivery of the same to appropriate tissues in the subject. Versatile application of the conjugates in diagnostics and imaging is described.

公开(公告)号：EP2274017B1

公开(公告)日：2016-04-13

申请号：EP09738558.7

申请日：2009-02-11

申请人： Ben Gurion University Of The Negev Research And Development Authority

发明人： DAVID, Ayelet ,  ASHKENASY, Gonen ,  SHAMAY, Yosi

IPC分类号： A61K47/48 ,  A61K49/00 ,  A61P35/00

CPC分类号： A61K47/64 ,  A61K31/704 ,  A61K47/549 ,  A61K47/58 ,  A61K47/59 ,  A61K47/62 ,  A61K47/65 ,  A61K49/0017 ,  G01N33/5091

摘要： The site-specific expression of selectins on endothelial cells of blood vessels during angiogenesis provides an opportunity to target anti-cancer drugs to the vascular endothelium to extend the range of the therapeutic effect. This invention describes an innovative drug targeting strategy for the selective delivery of the anticancer drugs to endothelial cells by means of polymer-drug conjugates modified with a carbohydrate ligand for the vascular selectins. A model chemotherapeutic drug, doxorubicin, and the E-selectin ligand, sLex, are attached to a biocompatible polymer (HPMA). The selective binding, cellular uptake, intracellular fate, and cell cytotoxicity of the polymer-bound drug are investigated in human endothelial cells.