[HTML][HTML] The hydrophobically-tagged MDM2–p53 interaction inhibitor Nutlin-3a-HT is more potent against tumor cells than Nutlin-3a
F Nietzold, S Rubner, T Berg - Chemical Communications, 2019 - pubs.rsc.org
F Nietzold, S Rubner, T Berg
Chemical Communications, 2019•pubs.rsc.orgWe 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.
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.
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.
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