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Small Molecule Inhibitors of MDM2-p53 and MDMX-p53 Interactions as New Cancer Therapeutics [PDF]

BioDiscovery, 2013
Inactivation of the function of tumor suppressor p53 is common in human cancers. In approximately half of human cancers, the tumor suppressor function of p53 is inactivated by deletion or mutation of TP53, the gene encoding p53 protein.
Yujun Zhao, Denzil Bernard, Shaomeng Wang   +2 more
doaj   +4 more sources

Inhibitors of MDM2 and MDMX: A Structural Perspective

Future Medicinal Chemistry, 2009
p53 is a potent tumor suppressor with a crucial role in preventing uncontrolled cell proliferation and is therefore frequently deleted or mutated in cancer. For tumors with wild-type p53, its function can be overcome by overactive cellular antagonists, such as the ubiquitin ligase murine double minute clone 2 (MDM2).
Riedinger, Christiane, McDonnell, James
openaire   +4 more sources

In silico identification of prospective p53-MDM2 inhibitors from ASINEX database using a comprehensive molecular modelling approach [PDF]

Scientific Reports
Cancer cells have a higher evolutionary potential than normal cells, which commonly leads to medication resistance and a decrease in the efficacy of existing cancer treatments.
Dushyant D. Kotadiya, Apurva Prajapati, Dharmesh A. Patel, Pooja Thakur, Ruchi Nair, Hitesh D. Patel   +5 more
doaj   +2 more sources

Two Birds with One Stone: NFAT1-MDM2 Dual Inhibitors for Cancer Therapy

Cells, 2020
The tumor suppressor p53 is believed to be the mostly studied molecule in modern biomedical research. Although p53 interacts with hundreds of molecules to exert its biological functions, there are only a few modulators regulating its expression and ...
Wei Wang, Atif Zafar, Mehrdad Rajaei, Ruiwen Zhang   +3 more
doaj   +2 more sources

Identification of new inhibitors of Mdm2–p53 interaction via pharmacophore and structure-based virtual screening

Drug Design, Development and Therapy, 2018
Noor Atatreh,1 Mohammad A Ghattas,1 Sanaa K Bardaweel,2 Sara Al Rawashdeh,1 Mohammad Al Sorkhy1 1Department of Pharmaceutical Sciences, College of Pharmacy, Al Ain University of Science and Technology, Al Ain, Abu Dhabi, United Arab Emirates ...
Atatreh N, Ghattas MA, Bardaweel SK, Al Rawashdeh S, Al Sorkhy M   +4 more
doaj   +1 more source

Fortifying p53 - beyond Mdm2 inhibitors. [PDF]

Aging (Albany NY), 2016
The tumor suppressor p53 is mutated in roughly 50% of all human malignancies. However, in the other 50% of tumors which retain wildtype p53, it appears insufficiently active to confer tumor suppression, through cell cycle arrest or apoptosis. Much of this p53-inactivation occurs through the Mdm2 oncoprotein, the product of a p53-inducible gene. Mdm2 is
Sriraman A, Li Y, Dobbelstein M.
europepmc   +4 more sources

Targeted degradation of MDM2 overcomes feedback regulation of p53 signaling in Merkel cell carcinoma models [PDF]

The Journal of Clinical Investigation
MDM2 is transcriptionally activated by the ST-MYCL-Tip60 complex in virus-positive Merkel cell carcinoma (MCC). MDM2 suppresses p53 and is a rational therapeutic target.
Varsha Ananthapadmanabhan, Simone Bruno, Leonard Vonk, Yu-Chen Cheng, Abeba Teshager, Benjamin K. Eschle, Charles L. Howarth, Joana S. Rodrigues, Julia Schnabel, Ananya Kodali, Prafulla C. Gokhale, Rujuta Kshirsagar, Susanne B. Breitkopf, Kirti Sharma, Joao A. Paulo, Yvonne Li, Andrew D. Cherniack, Franziska Michor, Yogesh Chutake, Joyoti Dey, James A. DeCaprio   +20 more
doaj   +2 more sources

PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective

Acta Materia Medica, 2022
Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed.
Xin Han, Wenyi Wei, Yi Sun
doaj   +1 more source

The Dual Interactions of p53 with MDM2 and p300: Implications for the Design of MDM2 Inhibitors. [PDF]

Int J Mol Sci, 2019
Proteins that limit the activity of the tumour suppressor protein p53 are increasingly being targeted for inhibition in a variety of cancers. In addition to the development of small molecules, there has been interest in developing constrained (stapled) peptide inhibitors. A stapled peptide ALRN_6924 that activates p53 by preventing its interaction with
Kannan S, Partridge AW, Lane DP, Verma CS.   +3 more
europepmc   +6 more sources

An Update on MDMX and Dual MDM2/X Inhibitors

Current Topics in Medicinal Chemistry, 2018
The tumor suppressor protein p53 is inactivated in all types of human cancers, either by negative regulation, by mutation or deletion of its gene. Specifically, in tumors that retain wild-type (wt) p53 status, p53 is inactivated by interaction with negative regulators, such as MDM2 and MDMX. These two proteins are found to be overexpressed in several
Margarida, Espadinha, Valentina, Barcherini, Elizabeth A, Lopes, Maria M M, Santos   +3 more
openaire   +3 more sources