Cytotoxic agents

Abstract

A cytotoxic agent that can be activated by exposure to light is provided. This agent comprises a metal cluster and a molecule containing a photocleavable group. The molecule forms a structure that at least partially surrounds the metal cluster to prevent the metal cluster from interacting with the surrounding environment, and upon exposure to light, the cleavage of the photocleavable group alters the structure of the molecule so that the metal cluster can interact with the surrounding environment.

Claims

1. An agent comprising a metal cluster and a molecule containing a photocleavable group, The molecule is an agent that forms a structure that at least partially surrounds the metal cluster to prevent the metal cluster from interacting with the surrounding environment, and, upon exposure to light, alters the structure of the molecule so that the photocleavable group cleavages, allowing the metal cluster to interact with the surrounding environment.

2. The activator according to claim 1, wherein the molecule comprises an oligonucleotide.

3. The agent according to claim 1 or 2, wherein the structure is a hairpin including a loop and a double-stranded stem.

4. The activator according to claim 3, as dependent on claim 2, wherein the loop comprises 7 to 12 nucleotides, optionally 9 nucleotides.

5. The activator according to claim 3 or claim 4, as dependent on claim 2, wherein all nucleotides in the loop are cytosine.

6. The activator according to any one of claims 3 to 5, wherein the double-stranded stem has a length of at least 6 base pairs, and optionally 8 base pairs or 9 base pairs.

7. The activator according to any one of claims 2 to 6, wherein the photocleavable group is located at or near the end of the loop.

8. The activator according to any one of claims 1 to 7, wherein the photocleavable group can be cleaved by light having a wavelength of 315 nm to 2000 nm.

9. The activator according to any one of claims 1 to 8, wherein the metal cluster contains or consists of silver.

10. The activator according to any one of claims 1 to 9, wherein the metal cluster comprises 20 or fewer atoms.

11. A pharmaceutical formulation comprising an activator according to any one of claims 1 to 10 and a carrier.

12. An agent according to any one of claims 1 to 10 or a preparation according to claim 11 for use as a pharmaceutical.

13. An agent according to any one of claims 1 to 10 or a formulation according to claim 11 for use in the treatment of proliferative diseases or the proliferation of microorganisms or infections.

14. The aforementioned use is, (i) A step of administering the activating agent or the preparation to the target, (ii) A step of exposing the object to light having a wavelength that can cleave the photocleavable group. An agent or formulation for use according to claim 13, comprising:

15. The agent or formulation for use according to claim 14, wherein the step of exposing the subject to light (step (ii)) is performed within 60 minutes after the step of administering the agent or formulation to the subject (step (i)).

16. The activating agent is administered in a dose of 10 μM or more, the activating agent or formulation for use according to any one of claims 13 to 15.

17. The agent or formulation for use according to any one of claims 13 to 16, wherein the agent or formulation is administered by infusion.

18. An in vitro method for reducing and / or preventing the growth of microorganisms, (i) A step of bringing the agent according to any one of claims 1 to 10 or the formulation according to claim 11 into contact with the growth of microorganisms or a surface, (ii) A step of growing the microorganism or exposing the surface to light having a wavelength that can cleave the photocleavable group, Methods that include...

19. The use or method described above further comprises the step of pre-treating the agent with a transfection reagent prior to step (i), the agent or formulation for use according to claim 14 or claim 15, or, if dependent on claim 14, claim 16 or claim 17, or the method according to claim 18.

20. Pretreatment of the aforementioned agent is to (a) Precomplex reagents with an optional ratio of activator to precomplex reagent of 30:1 to 70:1, and (b) Transfection reagents in an optional ratio of agonist to transfection reagent between 10:1 and 30:

1. The method according to claim 19, comprising processing in a manner.

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