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TitleDiscovery of Selective and Orally Bioavailable Heterobifunctional Degraders of Cyclin-Dependent Kinase 2.
Journal, issue, pagesJ Med Chem, Vol. 68, Issue 17, Page 18407-18422, Year 2025
Publish dateSep 11, 2025
AuthorsPhilip N Collier / Xiaozhang Zheng / Melissa Ford / Matthew Weiss / Dapeng Chen / Kunhua Li / Joseph D Growney / Annan Yang / Murugappan Sathappa / Susanne B Breitkopf / Brad Enerson / Tong Liang / Atanu Paul / Rupa Sawant / Lijing Su / Robert J Aversa / Charles Howarth / Kirti Sharma / Juliet Williams / Nicholas P Kwiatkowski /
PubMed AbstractCyclin-dependent kinase 2 (CDK2) plays an important role in cell cycle regulation and has emerged as a compelling target for the treatment of cancer, largely because of its potential to overcome the ...Cyclin-dependent kinase 2 (CDK2) plays an important role in cell cycle regulation and has emerged as a compelling target for the treatment of cancer, largely because of its potential to overcome the resistance associated with CDK4/6 inhibition. Efforts to develop CDK2 inhibitors have historically proven challenging due to undesirable safety profiles associated with inhibiting off-target CDK isoforms. Herein, we describe the structure-guided discovery of a series of orally bioavailable and selective degraders of CDK2. Degrader demonstrated improved phenotypic selectivity compared to a clinical CDK2 inhibitor, with greater specificity for disease-relevant cyclin E1 (CCNE1)-amplified cancer cells vs nonamplified cohort. The antitumor activity of in mice bearing CCNE1-amplified HCC1569 tumors correlated with sustained >90% degradation of CDK2 and sustained 90% inhibition of Rb phosphorylation.
External linksJ Med Chem / PubMed:40833690 / PubMed Central
MethodsEM (single particle)
Resolution3.9 Å
Structure data

49942

9nyr

EMDB-49942, PDB-9nyr:
Cryo-EM structure of CDK2/CyclinE1 in complex with CRBN/DDB1 and Cpd 24
Method: EM (single particle) / Resolution: 3.9 Å

Chemicals

PDB-1b7g:
GLYCERALDEHYDE 3-PHOSPHATE DEHYDROGENASE

ChemComp-ZN:
Unknown entry

Source
  • homo sapiens (human)
KeywordsCELL CYCLE / kinase / degrader / CDK2 / Cyclin E / CRBN

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