Results 211 to 220 of about 644,957 (254)

Dihydropyrimidine derivatives as MDM2 inhibitors

Chemical Biology & Drug Design, 2023
AbstractOne of the chief pathways to regulate p53 levels is MDM2 protein, which negatively controls p53 by direct inhibition. Many cancers overproduce MDM2 protein to interrupt p53 functions. Therefore, impeding MDM2's binding to p53 can reactivate p53 in tumor cells may suggest an effective approach for tumor therapy.
Ali Mehri, Karim Mahnam, Hajar Sirous, Mahmoud Aghaei, Leila Rafiei, Mahboubeh Rostami   +5 more
openaire   +2 more sources

p53-Mdm2 Interaction Inhibitors as Novel Nongenotoxic Anticancer Agents

Current Cancer Drug Targets, 2018
Background: Cancer is a major global health problem with high mortality rate. Most of the clinically used anticancer agents induce apoptosis through genotoxic stress at various stages of cell cycle and activation of p53.
Surendra Kumar Nayak, Gopal Khatik, Harish Kumar Chopra   +2 more
exaly   +2 more sources

Binding of an inhibitor of the p53/MDM2 Interaction to MDM2

Chemical Communications, 2003
The mode of action of the secondary metabolite chlorofusin, which antagonises the interaction between p53 and MDM2, involves direct binding to the N-terminal domain of MDM2.
Duncan, Sara J., Cooper, Matthew A., Williams, Dudley H.   +2 more
openaire   +5 more sources

MDM2/MDMX inhibitor peptide: WO2008106507

Expert Opinion on Therapeutic Patents, 2009
The evidence that some human cancers show wild-type p53 and overexpressed levels of MDM2 and/or MDMX has fueled the search for new therapeutic agents that could rescue p53 from the inhibition of MDM2 and MDMX. Recent data, suggesting a distinct and complementary mode of action of MDM2 and MDMX in the regulation of the pro-apoptotic activity of p53 ...
MACCHIARULO, Antonio, PELLICCIARI, Roberto   +1 more
openaire   +3 more sources

Mdm2 inhibitors as a platform for the design of P-glycoprotein inhibitors

Bioorganic & Medicinal Chemistry Letters, 2020
Chemoresistance is thought to be the cause of low treatment efficacy and mortality in more than 90% of patients with advanced cancer. The activation of drug efflux by P-glycoprotein is the key mechanism of resistance. All known P-gp inhibitors are used only in the combination therapy.
T. Grigoreva, A. Romanova, A. Sagaidak, S. Vorona, D. Novikova, V. Tribulovich   +5 more
openaire   +2 more sources

Small Molecule Inhibitors of the p53-MDM2

Current Medicinal Chemistry, 2008
Recent researches have discovered that MDM2 (murine double minute 2, or HDM2 for the human congener) protein is the main negative regulator of p53, which is an attractive therapeutic target in oncology because its tumor-suppressor activity which can be stimulated to eradicate tumor cells.
Chun-Qi, Hu, Yong-Zhou, Hu
openaire   +2 more sources

MDM2 Inhibitors for Pancreatic Cancer Therapy

Mini-Reviews in Medicinal Chemistry, 2010
MDM2 protein negatively regulates p53 and is found to be elevated in cancer cells. An attractive approach towards targeting MDM2 is the use of small molecule inhibitors that bind to MDM2 and disrupt the MDM2-p53 interaction. Our laboratory has been at the forefront in testing MDM2 inhibitors in pancreatic adenocarcinoma (PaCa), a deadly disease with ...
A.S. Azmi, P.A. Philip, K. Almhanna, F.W. Beck, Z.K. Kafri, F.H. Sarkar, R.M. Mohammad   +6 more
openaire   +2 more sources

MDM2 inhibitors for cancer therapy

Trends in Molecular Medicine, 2007
The tumor suppressor p53 is a powerful antitumoral molecule frequently inactivated by mutations or deletions in cancer. However, half of all human tumors express wild-type p53, and its activation by antagonizing its negative regulator murine double minute 2 (MDM2) might offer a new therapeutic strategy.
openaire   +2 more sources

Use of a Retroinverso p53 Peptide as an Inhibitor of MDM2

Journal of the American Chemical Society, 2004
An N-terminal helical region of the tumor suppressor p53 binds in a hydrophobic cleft of the oncoprotein MDM2. A retroinverso isomer of the natural N-terminal helical peptide was found to interact with MDM2 using the same hydrophobic residues, Phe, Trp, and Leu.
Kaori, Sakurai, Hak Suk, Chung, Daniel, Kahne   +2 more
openaire   +2 more sources

Small Molecule Inhibitors of p53/MDM2 Interaction

Current Topics in Medicinal Chemistry, 2005
The discovery of the key negative regulator MDM2 (mouse double minute 2, also termed HDM2 for its human equivalent) provided a great opportunity to manipulate the levels of the tumor suppressor p53 in cancer cells. Activation of p53 in tumor cells by inhibiting the interaction of MDM2 with p53 has therefore been the focus of a large effort in drug ...
Nader, Fotouhi, Bradford, Graves
openaire   +2 more sources