IndraLab

Statements

MDM2 binds TP53 and TAD1. 3 / 3
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"The Mdm2:p53-TAD1 interaction has been the target of drug discovery efforts for more than a decade and compounds with low nM binding constants for the Mdm2 pocket are in clinical trials against a variety of human cancers, some of which are characterized by Mdm2 overexpression xref ."
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"ATSP_7041 binds to the p53 binding pocket in the N-terminal domain of Mdm2 by mimicking the interactions of the TAD1 region of p53 with Mdm2."
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"In this case, the entropic penalty for p53-TAD1 binding to Mdm2, -TΔS = +2.2–2.6 kcal mol−1 xref , was much smaller than the value reported herein for binding to MdmX (+8.1 ± 0.1 kcal mol −1 ; xref )."
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