2. Academic Validation
  3. Poloxin-2HT+: changing the hydrophobic tag of Poloxin-2HT increases Plk1 degradation and apoptosis induction in tumor cells

Poloxin-2HT+: changing the hydrophobic tag of Poloxin-2HT increases Plk1 degradation and apoptosis induction in tumor cells

  • Org Biomol Chem. 2019 Mar 20;17(12):3113-3117. doi: 10.1039/c9ob00080a.
Stefan Rubner 1,  Sabine Schubert,  Thorsten Berg
Affiliations

Affiliation

  • 1 Institute of Organic Chemistry, Leipzig University, Johannisallee 29, 04103 Leipzig, Germany. tberg@uni-leipzig.de.
PMID: 30848278 DOI: 10.1039/c9ob00080a
Abstract

We report the hydrophobically-tagged PLK1 PBD inhibitor Poloxin-2HT+, which selectively degrades the tumor target PLK1 and induces Apoptosis in human tumor cells with higher potency than the hydrophobically-tagged inhibitor Poloxin-2HT. Our data provide further evidence that hydrophobically tagged inhibitors of protein-protein interactions can target and destroy disease-relevant proteins.

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