University of Washington

Narendra Pal Singh

Tomikazu Sasaki

Henry C Lai

Henry Chiu-Yuen Lai

Steve J Oh

The invention relates to covalent conjugates between endoperoxides and small peptides and organic compounds that bind to molecular cavities on the transferrin or lactoferrin receptor, and the use of compositions comprising these conjugates to treat cancer, hyperproliferative disorders, inflammatory diseases, and infections.

Covalent conjugates between endoperoxides and transferrin and lactoferrin receptor-binding agents

In one aspect, the invention provides covalent conjugates between artemisinin-related endoperoxides and iron-carrying proteins. In some embodiments, the covalent conjugates comprise artelinate and holotransferrin. In another aspect, the invention provides methods for administering the covalent conjugates of the invention to treat cancer and infections by pathogens that bind iron-carrying proteins.

Covalent conjugates between artemisinin-related endoperoxides and iron-carrying proteins and methods of use

Compounds having an artemisinin-related endoperoxide moiety covalently coupled to a hydrazone moiety through a linker. Compositions and methods for treating cancer using the compounds.

Conjugates of artemisinin-related endoperoxides and hydrazone derivatives for the treatment of cancer

Methods of inhibiting or killing cancer cells are disclosed wherein compounds having an endoperoxide moiety that is reactive with heme are administered under conditions which enhance intracellular iron concentrations. Representative endoperoxide compounds include endoperoxide bearing sesquiterpene compounds such as artemisinin and its analogs, arteflene and its analogs, 1,2,4-trioxanes and 1,2,4,5-tetraoxanes. Intracellular iron concentrations may be enhanced by the administration of iron salts or complexes.

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Lynnwood, WA, United States of America

Narendra Pal Singh