Document Detail

Mdm2 and MdmX inhibitors for the treatment of cancer: a patent review (2011-present).
MedLine Citation:
PMID:  23374098     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: One of the hallmarks of cancer cells is the inactivation of the p53 pathway either due to mutations in the p53 gene or over-expression of negative regulators, Mdm2 and/or MdmX. Pharmacological disruption of the Mdm2/X-p53 interaction to restore p53 activity is an attractive concept, aiming at a targeted and non-toxic cancer treatment.
AREAS COVERED: The introduction covers the biological role of p53 pathway and its regulation by Mdm2 and MdmX in normal and cancer cells and the current repertoire and development status of inhibitors of the Mdm2/X-p53 interaction for the treatment of cancer. The main part of the article covers patents and patent applications describing small molecule inhibitors of the Mdm2/X-p53 interaction published from 2011 until 2012.
EXPERT OPINION: The area of small molecule Mdm2/X-p53 interaction inhibitor development is progressing fast. Several Phase I clinical studies and preclinical programs are now in progress, however, the clinical proof concept has yet to be demonstrated. Multiple available compounds inhibit Mdm2-p53 interaction with nanomolar affinities, but MdmX is still missing such potent binders. Since research points to a complementary mode of Mdm2 and MdmX action, the future compound classes will possibly want to include dual actions versus Mdm2 and MdmX.
Krzysztof Zak; Aleksandra Pecak; Barbara Rys; Benedykt Wladyka; Alexander Dömling; Lutz Weber; Tad A Holak; Grzegorz Dubin
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Review     Date:  2013-02-04
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  23     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2013 Apr 
Date Detail:
Created Date:  2013-03-14     Completed Date:  2013-09-03     Revised Date:  2014-04-08    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  England    
Other Details:
Languages:  eng     Pagination:  425-48     Citation Subset:  IM    
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MeSH Terms
Antineoplastic Agents / chemistry,  pharmacology*,  therapeutic use
Drug and Narcotic Control
Enzyme Inhibitors / chemistry,  pharmacology*,  therapeutic use
Molecular Structure
Molecular Targeted Therapy*
Neoplasms / drug therapy*,  enzymology,  pathology
Patents as Topic
Proto-Oncogene Proteins c-mdm2 / antagonists & inhibitors*,  metabolism
Signal Transduction / drug effects
Structure-Activity Relationship
Grant Support
1P41GM094055-01/GM/NIGMS NIH HHS; 1R01GM097082-01/GM/NIGMS NIH HHS
Reg. No./Substance:
0/Antineoplastic Agents; 0/Enzyme Inhibitors; EC Proteins c-mdm2

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