Rusiecki Rafał 1 , Witkowski Jakub 2 , Jaszczewska-Adamczak Joanna 3 Show Affiliations »
Abstract
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.
Entities: Disease
Gene
Species
Keywords:
Anticancer; LAG3; MDM2 inhibitor; PD-1; combination therapy; molecular targeted therapy; p53; patent
Year: 2019
PMID： 31642413 DOI： 10.2174/1574892814666191022163540
Source DB: PubMed Journal: Recent Pat Anticancer Drug Discov ISSN： 1574-8928 Impact factor: 4.169