Tag: MDM2

CMLD010509 is a Highly Specific Inhibitor of the Oncogenic MYC-Driven Translation Program

Multiple myelomas (MM) is a hematological malignancy, it exhibits a clonal proliferation of plasma cells in the bone marrow micro-environment. MM remains a frequently incurable hematological malignancy until today. MYC can directly enhance transcription genes encoding ribosomal proteins, ribosomal RNA, and proteins of the translation initiation complex. Furthermore, most...

MD-224 is a First-in-Class and Highly Potent PROTAC Degrader of MDM2

As previously introduced, the tumor suppressor p53 plays a critical role in the prevention of tumor development. While human, murine double minute 2 (MDM2) protein is a primary endogenous cellular inhibitor of the tumor suppressor p53. And it has been pursued as a promising cancer therapeutic target. A study...

MI-1061 is an Orally Active MDM2 Inhibitor

Inhibition of the MDM2-p53 protein-protein interaction is being actively pursued as a new anticancer therapeutic strategy. Our previous blogs have introduced typical MDM2 or MDM2-p53 inhibitors, including MI-773, RG7112, and AMG 232. Today, I would like to mention another MDM2 inhibitor MI-1061 came from a study from Aguilar A....

RG7112 is the First Clinical and Orally Active MDM2-p53 Inhibitor

Yesterday, I introduced AMG 232 as a potent, selective and orally available inhibitor of p53-MDM2 interaction. Additionally, we have known the significance of MDM2-p53 interaction in cancer development. Today, I’d like to introduce another orally available MDM-2-p53 intreraction inhibitor, RG7112. RG7112 binds selectively to the p53 pocket on the...

BI-0252 is an Orally Active Inhibitor of the MDM2-p53 Interaction

The tumor protein p53 is a pivotal tumor suppressor protein and a mainstay of the body’s cellular anticancer defense system. As a potent transcription factor, TP53 regulates multiple downstream target genes implicated in cell-cycle control, apoptosis, senescence, and DNA repair. In particular, tumor protein p53 (TP53) is one of...

MA242 is a Dual Inhibitor of MDM2 and NFAT1

Overexpression and activation of the murine double minute 2 (MDM2) or nuclear factor of activated T cells 1 (NFAT1) oncoproteins occur frequently in pancreatic cancer. Many MDM2 inhibitors target MDM2-p53 binding and have little or no effect on cancers without functional p53, such as pancreatic cancer. Besides, nuclear factor...