Reversible aqueous ph sensitive lipidizing reagents, compositions and methods ofuse

摘要

The present invention provides lipidized conjugates comprising an amino group-containing biologically active substance and a lipophilic group capable of penetrating a biological membrane. Under neutral or mildly acidic conditions, including those found in vivo, the free amino group-containing biologically active substance is released from the conjugate by hydrolysis of an amide bond. The present invention is also directed to methods of preparing lipidizing agents and lipidized conjugates, pharmaceutical compositions comprising lipidized conjugates and methods of increasing the delivery of amino group-containing substances into a cell. Preferred amino group-containing substances include peptides, proteins and derivatives thereof.