Boron-containing hormone analogs and methods of their use in imaging or killing cells having hormone receptors
First Claim
1. A method of targeting boron to cells that contain intracellular receptors comprising contacting the cells with a conjugate comprising a boron containing moiety, wherein the boron containing moiety contains at least nine 10 B atoms, conjugated to a ligand having binding specificity for it least one intracellular receptor of the cells.
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Abstract
Boron containing compounds are targeted to hormonally responsive cells by contacting the cells with a conjugate of a boron containing moiety conjugated to a ligand having binding specificity for an intracellular receptor of the cell. The conjugates are useful for imaging or killing hormonally responsive cells, such as hormonally responsive tumor cells. For target cell killing, the cells are contacted with a 10 B containing moiety conjugated to a ligand having binding specificity for an intracellular hormone receptor of the cells. The 10 B containing moiety becomes associated with the hormone receptor of the cells, which may then be irradiated with neutrons to kill the cells by boron neutron capture. For target cell imaging, the cells are contacted with a 11 B containing moiety conjugated to a ligand having binding specificity for an intracellular hormone receptor of the cells, and the boron that becomes associated with the hormone receptor of the cells may then be imaged using magnetic resonance imaging techniques.
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Citations
23 Claims
- 1. A method of targeting boron to cells that contain intracellular receptors comprising contacting the cells with a conjugate comprising a boron containing moiety, wherein the boron containing moiety contains at least nine 10 B atoms, conjugated to a ligand having binding specificity for it least one intracellular receptor of the cells.
- 2. A method of killing intracellular receptor containing cells comprising contacting the cells with a boron neutron capture agent comprising a 10 B containing moiety, wherein the 10 B containing moiety contains at least nine 10 B atoms, conjugated to a ligand having binding specificity for at least one intracellular receptor of the cells, and then irradiating the cells with neutrons.
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19. A method of killing intracellular receptor containing cells comprising contacting the cells with a boron neutron capture agent comprising a 10 B containing moiety, wherein the 10 B containing moiety contains more than one 10 B atom, conjugated to a ligand having binding specificity for at least one intracellular receptor of the cells, and then irradiating the cells with neutrons.
- 20. A method of killing intracellular receptor containing cells comprising contacting the cells with a boron neutron capture agent comprising a 10 B containing moiety, wherein the 10 B containing moiety comprises at least one carborane residue, conjugated to a ligand having binding specificity for at least one intracellular receptor of the cells, and irradiating the cells with neutrons.
- 22. A method of killing intracellular receptor containing cells comprising contacting the cells with a boron neutron capture agent comprising a 10 B containing moiety, wherein the 10 B containing moiety comprises at least one carboranyl residue, conjugated to a ligand having binding specificity for at least one intracellular receptor of the cells, and irradiating the cells with neutrons.
Specification