Drug intelligence / Profile preview

Cyclin K degrader

Development stage
Preclinical
Lead developer
RejuvenRx
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01

Overview

RejuvenRx's Cyclin K degrader is a preclinical small molecule designed to induce the targeted degradation of Cyclin K (CCNK). Cyclin K is a regulatory subunit that associates with the cyclin-dependent kinases CDK12 and CDK13, which are essential for the transcription of genes involved in the DNA damage response (DDR) and other critical cellular processes. By utilizing a targeted protein degradation (TPD) approach, this compound triggers the proteasomal degradation of Cyclin K, leading to the functional loss of the CDK12/13 complex. This mechanism results in the downregulation of DDR-related transcripts, genomic instability, and selective apoptosis in cancer cells, particularly those that are transcriptionally addicted or have existing DDR deficiencies.

Other names
CCNK degrader
02

Targets

CRL4 (CRL4 E3 ubiquitin ligase complex)CCNK (Cyclin K)

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