Targeting of molecules to large vessel endothelium using epcr

Details Targeting of molecules to large vessel endothelium using epcr Targeting of molecules to large vessel endothelium using epcr

A - Human Necessities

61

K

A61K 45/06 (2006.01) A61K 47/48 (2006.01) A61K 51/10 (2006.01)

Patent

CA 2341586

Endothelial protein C receptor (EPCR) is found primarily on endothelial cells of large vessels. EPCR translocates from the plasma membrane surface to the nucleus. Molecules which bind to EPCR can be carried from the plasma membrane surface to the nucleus. These molecules include antibodies to EPCR and activated protein C. Protein C, which also binds to EPCR, can be internalized by endothelial cells, but does not enter the nucleus. Thus, EPCR translocation from the plasma membrane to the nucleus provides a means of delivering nucleic acid such as DNA, proteins such as transcription factors, diagnostic agents or other types of drugs to the nucleus of endothelial cells, particularly those on large blood vessels. Conjugates of the materials to be delivered to the nucleus can be formed by ionic or covalent coupling. For example, proteins, including fusion proteins, can be directly conjugated to an anti-EPCR monoclonal antibody. Covalent attachment of positively charged polymers, such as polylysine, to an anti-EPCR antibody allows nucleic acid to bind by ionic charges. Streptavidin and biotin can also be used to conjugate molecules to anti-EPCR antibodies. These conjugated antibodies are transported to the nucleus by EPCR. Examples demonstrate selective transport to the nucleus which is mediated by EPCR. Molecules transported include activated protein C, antibodies to EPCR, and streptavidin-biotin conjugates. Modification of anti- EPCR monoclonal antibodies by covalently coupling to polylysine allows binding of an expression vector to the modified antibody and translocation to the nucleus.

Le récepteur endothétial de la protéine C (EPCR) se trouve principalement sur les cellules endothéliales des gros vaisseaux. EPCR passe de la surface de la membrane cellulaire au noyau. Les molécules qui se lient à EPCR peuvent être transportées de ladite surface au noyau, elles comprennent des anticorps dirigés contre EPCR et une protéine C activée. Les cellules endothéliales peuvent internaliser la protéine C, qui se lie également à EPCR, mais qui n'entre pas dans le noyau. Ainsi, le passage d'EPCR de la membrane au noyau permet d'apporter des acides nucléiques tel que l'ADN, des protéines telles que des facteurs de transcription, des agents diagnostiques ou d'autres types de médicaments au noyau des cellules endothéliales, notamment à celles des gros vaisseaux sanguins. Des conjugués des matériaux à apporter au noyau peuvent être formés par couplage ionique ou covalent. Par exemple, des protéines, notamment des protéines de fusion, peuvent être conjuguées directement à un anticorps monoclonal anti-EPCR. L'attache covalente de polymères chargés positivement, tels que la polylysine, à un anticorps anti-EPCR, permet la liaison des acides nucléiques par des charges ioniques. La streptavidine et la biotine peuvent également être utilisées pour conjuguer des molécules aux anticorps anti-EPCR. Des exemples montrent qu'EPCR sert de médiateur pour le transport sélectif vers le noyau. Les molécules transportées comprennent une protéine C activée, des anticorps anti-EPCR, et des conjugués streptavine/biotine. La modification des anticorps

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