Background:
Mouse Double Minute 2 protein (MDM2) is a cellular regulator of p53 tumor
suppressor (p53). Inhibition of the interaction between MDM2 and p53 proteins is a promising anticancer
therapy.
Objective:
This updated patent review is an attempt to compile the research and achievements of the
various researchers working on small molecule MDM2 inhibitors from 2010 to date. We provide an
outlook into the future for therapy based on MDM2 inhibition by presenting an overview of the most
relevant patents which have recently appeared in the literature.
Methods:
Literature and recent patents focusing on the anticancer potential of MDM2-p53 interaction
inhibitors and its applications have been analyzed. We put the main emphasis on the most perspective
compounds which are or were examined in clinical trials.
Results:
Literature data indicated that MDM2 inhibitors are therapeutically effective in specific types
of cancer or non-cancer diseases. A great number of patents and research work around new MDM2-
p53 interaction inhibitors, possible combinations, new indications, clinical regimens in previous years
prove that this targeted therapy is in the scope of interest for many business and academic research
groups.
Conclusion:
Novel MDM2 inhibitors thanks to higher potency and better ADME properties have
shown effectiveness in preclinical and clinical development however the final improvement of therapeutic
potential for MDM2 inhibitors might depend on the useful combination therapy and exploring
new cancer and non-cancer indications.
Discovery, X-ray structure and CPP-conjugation enabled uptake of p53/MDM2 macrocyclic peptide inhibitors