Results 11 to 20 of about 644,957 (254)

Resistance mechanisms to inhibitors of p53-MDM2 interactions in cancer therapy: can we overcome them?

open access: yesCellular & Molecular Biology Letters, 2021
Since the discovery of the first MDM2 inhibitors, we have gained deeper insights into the cellular roles of MDM2 and p53. In this review, we focus on MDM2 inhibitors that bind to the p53-binding domain of MDM2 and aim to disrupt the binding of MDM2 to ...
Lucia Haronikova   +7 more
doaj   +2 more sources

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

open access: yesScientific 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   +5 more
doaj   +2 more sources

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

open access: yesCells, 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   +3 more
doaj   +2 more sources

Strategies for p53 Activation and Targeted Inhibitors of the p53-Mdm2/MdmX Interaction

open access: yesCells
p53 is a tumor suppressor gene and is regarded as one of the most crucial genes in protecting humans against cancer. The protein Mdm2 and its homolog MdmX serve as negative regulators of p53.
Ye Huang   +6 more
doaj   +3 more sources

Recent Small-Molecule Inhibitors of the p53–MDM2 Protein–Protein Interaction

open access: yesMolecules, 2020
This review presents the last decade of studies on the synthesis of various types of small-molecule inhibitors of the p53– Mouse double minute 2 homolog (MDM2) protein–protein interaction.
Anastasia Beloglazkina   +3 more
doaj   +3 more sources

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

open access: yesDrug 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   +4 more
doaj   +1 more source

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

open access: yesThe 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   +20 more
doaj   +2 more sources

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

open access: yesActa 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

Advancements in MDM2 inhibition: Clinical and pre-clinical investigations of combination therapeutic regimens

open access: yesSaudi Pharmaceutical Journal, 2023
Cancer cells often depend on multiple pathways for their growth and survival, resulting in therapeutic resistance and the limited effectiveness of treatments.
Ali M. Alaseem
doaj   +1 more source

MDM2 Inhibition in the Treatment of Glioblastoma: From Concept to Clinical Investigation

open access: yesBiomedicines, 2023
Inhibition of the interaction between MDM2 and p53 has emerged as a promising strategy for combating cancer, including the treatment of glioblastoma (GBM).
Karolina I. Pellot Ortiz   +4 more
doaj   +1 more source

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