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

Literature Information

Publication Date 2019-03-08
DOI 10.1039/C9OB00080A
Impact Factor 3.876
Authors

Stefan Rubner, Sabine Schubert, Thorsten Berg


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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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Organic & Biomolecular Chemistry

Organic & Biomolecular Chemistry
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