Issue 95, 2019
From the journal:

Chemical Communications

The hydrophobically-tagged MDM2–p53 interaction inhibitor Nutlin-3a-HT is more potent against tumor cells than Nutlin-3a†

Florian Nietzold,‡a   Stefan Rubner‡a  and  Thorsten Berg ORCID logo *a  

* Corresponding authors

a Institute of Organic Chemistry, Leipzig University, Johannisallee 29, 04103 Leipzig, Germany
E-mail: tberg@uni-leipzig.de
Fax: +49 341 9736599

Abstract

We present the first application of hydrophobic tagging to a non-covalent inhibitor of protein–protein interactions. Nutlin-3a-HT, created by fusing the hydrophobic tag HyT13 to the MDM2–p53 interaction inhibitor Nutlin-3a, prevented cellular accumulation of MDM2 upon p53 reactivation, and had a stronger effect on cell viability and the induction of apoptosis than Nutlin-3a.

Graphical abstract: The hydrophobically-tagged MDM2–p53 interaction inhibitor Nutlin-3a-HT is more potent against tumor cells than Nutlin-3a

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Article information

DOI
https://doi.org/10.1039/C9CC07795B
Article type
Communication
Submitted
04 Oct 2019
Accepted
04 Nov 2019
First published
05 Nov 2019
This article is Open Access
Creative Commons BY license

Chem. Commun., 2019,55, 14351-14354

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The hydrophobically-tagged MDM2–p53 interaction inhibitor Nutlin-3a-HT is more potent against tumor cells than Nutlin-3a

F. Nietzold, S. Rubner and T. Berg, Chem. Commun., 2019, 55, 14351 DOI: 10.1039/C9CC07795B

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