MMRi62, a Ferroptosis Inducer Targeting MDM2-MDM4
MDM2 and MDM4 have established cancer drug targets. Additionally, they are also inhibitors of p53 activity and are amplified in many cancer types. In particular, the targeting of MDM2–p53 interactions is a novel strategy that is pursued to unleash the antitumor activity of p53. Furthermore, there needs to cover...
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....
MI-773 is an MDM2 Inhibitor for Adenoid Cystic Carcinoma Therapy
Adenoid Cystic Carcinoma (ACC) is a rare kind of cancer, occurs in different tissues or organs. It commonly happens in salivary glands, and also exists in breast, lung, brain and the paranasal sinuses. The disease causes a lot of death all around the world. p53 (Tumor protein p53) is...
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...
AMG 232 is an Orally Active and Best-in-Class MDM2-p53 Inhibitor
The p53 tumor suppressor induces cell growth arrest and apoptosis in response to DNA damage or stress. And inactivation of the p53 pathway plays an indispensable role in tumor survival. Approximately p53 mutations resulting in loss of its function account for 50% human cancers. And the wild-type p53, present...