Drug intelligence / Profile preview

NCT02

Development stage
Preclinical
Lead developer
University of Nebraska Medical Center
Modality
Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
01

Overview

NCT02 is a small molecule molecular glue degrader that targets Cyclin K (CCNK) and its associated kinase, Cyclin-dependent kinase 12 (CDK12). Developed by researchers at the University of Nebraska Medical Center, NCT02 induces the proteasomal degradation of Cyclin K, a protein found to be overexpressed in pancreatic ductal adenocarcinoma (PDAC) and associated with poor patient survival. By depleting Cyclin K, NCT02 inhibits PDAC cell proliferation and induces G1-S cell cycle arrest. Preclinical studies have shown that NCT02 sensitizes pancreatic cancer cells to standard-of-care chemotherapy (gemcitabine and paclitaxel) and PARP inhibitors (olaparib or niraparib), suggesting its potential as a therapeutic agent for pancreatic cancer.

02

Targets

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

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