Abstract: A method for inhibiting the activity of a natural polyamine transporter comprising the step of contacting the transporter with an inhibitorily effective amount of a compound of formula (I) or (II): wherein L is a linker; R1=H, methyl, ethyl or propyl; R2=H or methyl; 0<x<3; 0<y<3; 2<v<5; and 2<w<8. Such a method is particularly useful for treating disorders involving the control of polyamine transport.

Abstract: A method for inhibiting the activity of a natural polyamine transporter comprising the step of contacting the transporter with an inhibitorily effective amount of a compound of formula (I) or (II): wherein L is a linker; R1=H, methyl, ethyl or propyl; R2=H or methyl; 0<x<3; 0<y<3; 2<v<5; and 2<w<8. Such a method is particularly useful for treating disorders involving the control of polyamine transport.

Abstract: Described herein are novel specific, pure competitive inhibitors of natural polyamine transport in mammalian cells. Despite their low molecular weight, the inhibitors of the present invention stay virtually impermeant to the cell and display minor non-specific effects while exhibiting a very high affinity for the carrier. More specifically described are synthetic derivatives of original polyamines, wherein the original polyamine is modified to comprise an amido group immediately linked to the polyamine backbone. A side chain may be anchored to the amido group and provide for the formation of dimeric synthetic derivatives or its labelling and subsequent usage as a marker for the polyamine transporter.