Method of delivery of a medicament to a cancer cell using a pathway of plasminogen activator material

A method of delivering a medicament to the surface of a cancer cell and transferring the medicament into the cancer cell using an activated plasminogen activator material such as a plasminogen activator inhibitor type-1 or type-2 (PAI-1, PAI-2). The medicament is coupled to PAI-1 or PAI-2 to form a reaction product that is coupled with the urokinase plasminogen activator (uPA) that is bound to the cell surface by the uPA receptor (uPAR). The medicament is coupled to PAI-1 or PAI-2 (for example, using a preserving agent such as saporin) in such a way that the medicament does not interfere with active sites responsible for binding to uPA or LRP proteins responsible for the internalization of the plasminogen activator material/conjugated medicament. The conjugated medicament prevents the conversion of the plasminogen activator inhibitor material into its latent inactive form. The resulting complex is internalized into the cancer cell to deliver the medicament within the cell.
Download pdf
Abstract/Description: A method of delivering a medicament to the surface of a cancer cell and transferring the medicament into the cancer cell using an activated plasminogen activator material such as a plasminogen activator inhibitor type-1 or type-2 (PAI-1, PAI-2). The medicament is coupled to PAI-1 or PAI-2 to form a reaction product that is coupled with the urokinase plasminogen activator (uPA) that is bound to the cell surface by the uPA receptor (uPAR). The medicament is coupled to PAI-1 or PAI-2 (for example, using a preserving agent such as saporin) in such a way that the medicament does not interfere with active sites responsible for binding to uPA or LRP proteins responsible for the internalization of the plasminogen activator material/conjugated medicament. The conjugated medicament prevents the conversion of the plasminogen activator inhibitor material into its latent inactive form. The resulting complex is internalized into the cancer cell to deliver the medicament within the cell.
Subject(s): 424/193.1
424/197.11
424/542
435/326
435/346
977/806
977/906
977/911
977/912
977/915
977/920
Date Issued: 1997-10-21