Title : EGCG binds intrinsically disordered N-terminal domain of p53 and disrupts p53-MDM2 interaction.

Pub. Date : 2021 Feb 12

PMID : 33579943






8 Functional Relationships(s)
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1 EGCG binds intrinsically disordered N-terminal domain of p53 and disrupts p53-MDM2 interaction. epigallocatechin gallate tumor protein p53 Homo sapiens
2 EGCG binds intrinsically disordered N-terminal domain of p53 and disrupts p53-MDM2 interaction. epigallocatechin gallate tumor protein p53 Homo sapiens
3 Using SPR and NMR, here we report a direct, muM interaction between EGCG and the tumor suppressor p53 (KD = 1.6 +- 1.4 muM), with the disordered N-terminal domain (NTD) identified as the major binding site (KD = 4 +- 2 muM). epigallocatechin gallate tumor protein p53 Homo sapiens
4 The EGCG-p53 interaction disrupts p53 interaction with its regulatory E3 ligase MDM2 and inhibits ubiquitination of p53 by MDM2 in an in vitro ubiquitination assay, likely stabilizing p53 for anti-tumor activity. epigallocatechin gallate tumor protein p53 Homo sapiens
5 The EGCG-p53 interaction disrupts p53 interaction with its regulatory E3 ligase MDM2 and inhibits ubiquitination of p53 by MDM2 in an in vitro ubiquitination assay, likely stabilizing p53 for anti-tumor activity. epigallocatechin gallate tumor protein p53 Homo sapiens
6 The EGCG-p53 interaction disrupts p53 interaction with its regulatory E3 ligase MDM2 and inhibits ubiquitination of p53 by MDM2 in an in vitro ubiquitination assay, likely stabilizing p53 for anti-tumor activity. epigallocatechin gallate tumor protein p53 Homo sapiens
7 The EGCG-p53 interaction disrupts p53 interaction with its regulatory E3 ligase MDM2 and inhibits ubiquitination of p53 by MDM2 in an in vitro ubiquitination assay, likely stabilizing p53 for anti-tumor activity. epigallocatechin gallate tumor protein p53 Homo sapiens
8 Our work provides insights into the mechanisms for EGCG"s anticancer activity and identifies p53 NTD as a target for cancer drug discovery through dynamic interactions with small molecules. epigallocatechin gallate tumor protein p53 Homo sapiens