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Issue 12, 2019
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Poloxin-2HT+: changing the hydrophobic tag of Poloxin-2HT increases Plk1 degradation and apoptosis induction in tumor cells

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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.

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

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Publication details

The article was received on 11 Jan 2019, accepted on 25 Feb 2019 and first published on 08 Mar 2019


Article type: Communication
DOI: 10.1039/C9OB00080A
Org. Biomol. Chem., 2019,17, 3113-3117
  • Open access: Creative Commons BY license
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    Poloxin-2HT+: changing the hydrophobic tag of Poloxin-2HT increases Plk1 degradation and apoptosis induction in tumor cells

    S. Rubner, S. Schubert and T. Berg, Org. Biomol. Chem., 2019, 17, 3113
    DOI: 10.1039/C9OB00080A

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