Article - Can MDM2 Inhibition With Nutlins Indirec
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Posted On: 12/20/2017 7:33:33 PM
Article - Can MDM2 Inhibition With Nutlins Indirectly Restore p53 Function?
“The E3 ubiquitin-protein ligase MDM2 regulatory protein inhibits TP53 tumor suppressor gene transcription. MDM2's own transcription is triggered by p53 — making up the MDM2-p53 feedback loop that regulates normal p53 levels in healthy cells.3,9
In cancers harboring wild-type TP53, which is frequently seen in multiple myeloma, AML, and most other leukemias, for example, p53 is dysregulated by MDM2 oncogene overexpression — opening the door to the possibility of indirect p53 restoration using MDM2 antagonists.3,4,9
Both TP53 mutations and amplified MDM2 gene expression–triggered MDM2 protein production are associated with metastasis, treatment resistance, and poor prognosis in several solid and hematologic malignancies.3,4,6”
http://www.cancertherapyadvisor.com/multiple-...le/718766/
“The E3 ubiquitin-protein ligase MDM2 regulatory protein inhibits TP53 tumor suppressor gene transcription. MDM2's own transcription is triggered by p53 — making up the MDM2-p53 feedback loop that regulates normal p53 levels in healthy cells.3,9
In cancers harboring wild-type TP53, which is frequently seen in multiple myeloma, AML, and most other leukemias, for example, p53 is dysregulated by MDM2 oncogene overexpression — opening the door to the possibility of indirect p53 restoration using MDM2 antagonists.3,4,9
Both TP53 mutations and amplified MDM2 gene expression–triggered MDM2 protein production are associated with metastasis, treatment resistance, and poor prognosis in several solid and hematologic malignancies.3,4,6”
http://www.cancertherapyadvisor.com/multiple-...le/718766/
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