Metallodrugs having improved pharmacological properties, and methods of manufacture and use thereof
First Claim
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1. A compound for catalytically inactivating a biochemical target of interest, comprising:
- a ligand moiety which binds to the biochemical target; and
a metal binding moiety,wherein the ligand moiety is heterologous to the metal binding moiety, wherein the ligand moiety and the metal binding moiety are covalently linked, wherein the compound binds to the biochemical target with an affinity of between about 104 M−
1 and about 0.7×
107 M−
1, and wherein the compound has an off rate (koff) for its target which is similar to that for the catalytic turnover (kcat) of the metal binding moiety.
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Abstract
It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.
15 Citations
44 Claims
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1. A compound for catalytically inactivating a biochemical target of interest, comprising:
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a ligand moiety which binds to the biochemical target; and a metal binding moiety, wherein the ligand moiety is heterologous to the metal binding moiety, wherein the ligand moiety and the metal binding moiety are covalently linked, wherein the compound binds to the biochemical target with an affinity of between about 104 M−
1 and about 0.7×
107 M−
1, and wherein the compound has an off rate (koff) for its target which is similar to that for the catalytic turnover (kcat) of the metal binding moiety. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44)
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Specification