Inhibitors and their uses
AssigneeThe University of Nottingham
InventorsChristopher James Hayes, John David Brook, Ami Ketley
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Abstract
The invention relates to inhibitors of CDK12 (cyclin-dependent kinase 12), and there use in the treatment or prevention of a disorder in a subject caused by the generation of repeat expansion transcripts.
Claims40
An inhibitor for use in the treatment or prevention of a disorder in a subject caused by the generation of repeat expansion transcripts, wherein the inhibitor is an inhibitor of CDK12 (cyclin-dependent kinase 12).
The inhibitor for use according to any preceding claim, wherein the repeat expansion transcript comprises RNA from a CTG DNA repeat;
- a CCTG DNA repeat;
- a CGG DNA repeat;
- a GGGGCC DNA repeat;
- a ATTCT DNA repeat;
- a TGGAA DNA repeat or a CAG DNA repeat.
The inhibitor for use according to any preceding claim, wherein the inhibitor is specific for CDK12.
The inhibitor for use according to any preceding claim, wherein the inhibitor is not an inhibitor of CDK9 activity or availability.
The inhibitor for use according to any preceding claim, wherein the inhibitor is administered, or arranged to be administered, in combination with at least one other therapeutic agent.
The inhibitor for use according to any preceding claim, wherein the use is in combination with an oligonucleotide that targets the DMPK gene.
The inhibitor for use according to any preceding claim, wherein the inhibitor is administered, or arranged to be administered, intermittently.
Use of a CDK12 inhibitor in the preparation of a medicament for the treatment or prevention of a disorder caused by the generation of repeat expansion transcripts in a subject.
A method of treatment or prevention of a disorder caused by the generation of repeat expansion transcripts in a subject, comprising administering an inhibitor of CDK12 to the subject.
A method of screening for a therapeutic agent for a disorder caused by the generation of repeat expansion transcripts comprising:
- providing a molecule for screening;
- detecting if the molecule inhibits the activity of CDK12,
- wherein detection of inhibition of CDK12 selects the molecule as a potential candidate therapeutic agent.
A composition comprising a CDK12 inhibitor and a pharmaceutically acceptable carrier.
The inhibitor, method, use, or composition substantially as described herein, optionally with reference to the accompanying figures.
Dependencies are inferred from the claim text.