RG7388
Antagonist of MDM2
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
(last updated: 17 Aug 2017 )
SERP Ratings
SERP Comments:
RG7388 is a second-generation inhibitor of the protein-protein interaction that occurs between wild type p53 (a potent tumor suppressor) and the E3 ubiquitin ligase MDM2. High levels of MDM2 are found in several tumor types, resulting in the destruction of p53. Inhibition of this interaction with chemical probes such as RG7388 can restore wild-type p53 activity in cells. Medicinal chemistry efforts to improve the original 'Nutlin' class of MDM2 inhibitors have yield compounds such as RG7388, with improved activity and pharmacokinetic properties.
(last updated: 17 Aug 2017 )
SERP Ratings
SERP Comments:
Potent and optimised MDM2-p53 antagonist that entered into clinical trials. In general, there is only very limited data available with regard to the selectivity of this compound. However, in contrast to some other published compounds from this class, RG7738 appears to only exhibit off-target effects on MDR-1 at concentrations of 5 µM.
(last updated: 16 Nov 2020 )