Results 31 to 40 of about 644,957 (254)

A p53-independent role for the MDM2 antagonist Nutlin-3 in DNA damage response initiation. [PDF]

, 2011
BACKGROUND: The mammalian DNA-damage response (DDR) has evolved to protect genome stability and maximize cell survival following DNA-damage. One of the key regulators of the DDR is p53, itself tightly regulated by MDM2. Following double-strand DNA breaks
Valentine, Jane M., Kumar Sonia, Abdeladim Moumen, Moumen, Abdeladim, Kumar, S, Valentine Jane M, Jane M Valentine, Moumen, A, Moumen Abdeladim, Valentine, JM, Sonia Kumar, Kumar, Sonia   +11 more
core   +2 more sources

Inhibition of the MDM2/p53 Interaction Design, Synthesis and Evaluation of MDM2 Inhibitors [PDF]

, 2015
Numerous essential cellular processes are regulated by protein-protein interactions (PPIs) and PPIs have therefore been recognised as potential new drug targets. The transcription factor p53 is often referred to as the guardian of the genome due to its
Pettersson, Mariell
core   +1 more source

Targeting the MDM2-p53 pathway in dedifferentiated liposarcoma

Frontiers in Oncology, 2022
Dedifferentiated liposarcoma (DDLPS) is an aggressive adipogenic cancer with poor prognosis. DDLPS tumors are only modestly sensitive to chemotherapy and radiation, and there is a need for more effective therapies.
Raymond S. Traweek, Brandon M. Cope, Christina L. Roland, Emily Z. Keung, Elise F. Nassif, Derek J. Erstad   +5 more
doaj   +1 more source

Chemical classification of MDM2 inhibitors

International Journal of Pharmaceutical Chemistry and Analysis, 2021
MDM2 inhibitors class of anti-neoplastic drugs has been evolve after the successful discovery of the nutlins and other potent inhibitors. MDM2 inhibitors can specifically target the tumour cells in the body, by selectively reactivating the inhibited p53 function in the tumour cells.None of the compound of this class has been entered into the market ...
Chirag J Gohil, Malleshappa N Noolvi, Chhaganbhai N Patel, Dhrubo Jyoti Sen   +3 more
openaire   +2 more sources

A yeast two-hybrid system for the screening and characterization of small-molecule inhibitors of protein–protein interactions identifies a novel putative Mdm2-binding site in p53

BMC Biology, 2017
Background Protein–protein interactions (PPIs) are fundamental to the growth and survival of cells and serve as excellent targets to develop inhibitors of biological processes such as host-pathogen interactions and cancer cell proliferation.
Jin Huei Wong, Mohammad Alfatah, Mei Fang Sin, Hong May Sim, Chandra S. Verma, David P. Lane, Prakash Arumugam   +6 more
doaj   +1 more source

Natural products targeting the p53-MDM2 pathway and mutant p53: Recent advances and implications in cancer medicine

Genes and Diseases, 2018
The p53 tumor suppressor plays a major role in controlling the initiation and development of cancer by regulating cell cycle arrest, apoptosis, senescence, and DNA repair.
Jiang-Jiang Qin, Xin Li, Courtney Hunt, Wei Wang, Hui Wang, Ruiwen Zhang   +5 more
doaj   +1 more source

Malignant progression of liver cancer progenitors requires lysine acetyltransferase 7–acetylated and cytoplasm‐translocated G protein GαS

Hepatology, EarlyView., 2022
KAT7‐acetylated and cytoplasm‐translocated G‐protein GαS enhances IL‐6 effect and drives HCC progenitor cell progression. Abstract Background and Aims Hepatocarcinogenesis goes through HCC progenitor cells (HcPCs) to fully established HCC, and the mechanisms driving the development of HcPCs are still largely unknown.
Ye Zhou, Kaiwei Jia, Suyuan Wang, Zhenyang Li, Yunhui Li, Shan Lu, Yingyun Yang, Liyuan Zhang, Mu Wang, Yue Dong, Luxin Zhang, Wannian Zhang, Nan Li, Yizhi Yu, Xuetao Cao, Jin Hou   +15 more
wiley   +1 more source

Novel Allosteric Mechanism of Dual p53/MDM2 and p53/MDM4 Inhibition by a Small Molecule

Frontiers in Molecular Biosciences, 2022
Restoration of the p53 tumor suppressor for personalised cancer therapy is a promising treatment strategy. However, several high-affinity MDM2 inhibitors have shown substantial side effects in clinical trials.
Vera V. Grinkevich, Aparna Vema, Karin Fawkner, Natalia Issaeva, Virginia Andreotti, Eleanor R. Dickinson, Elisabeth Hedström, Clemens Spinnler, Alberto Inga, Lars-Gunnar Larsson, Anders Karlén, Margareta Wilhelm, Perdita E. Barran, Andrei L. Okorokov, Galina Selivanova, Joanna E. Zawacka-Pankau   +15 more
doaj   +1 more source

Novel Inhibitors for MDM2-MDM4 E3 Ligase Potently Induce p53-Indepedent Apoptosis in Drug-Resistant Leukemic Cells

Molecules
MDM2 and MDM4 are major negative regulators of tumor suppressor p53. Beyond regulating p53, MDM2 possesses p53-independent activity in promoting cell cycle progression and tumorigenesis via its RING domain ubiquitin E3 ligase activity. MDM2 and MDM4 form
Rati Lama, Joseph M. Fose, Diana Martín, Inés G. Muñoz, Eunice S. Wang, Pamela J. Sung, Sherry R. Chemler, Xinjiang Wang   +7 more
doaj   +1 more source

Oncogenic DMTF1β promotes cancer cell motility by regulating autophagy through ULK1 stabilization

Molecular Oncology, EarlyView.
In the current study, we demonstrate that the oncogene DMTF1β regulates ULK1 stability by reducing its proteasomal degradation in cancer cells. This stabilization enables ULK1 to induce autophagy, which in turn facilitates cancer cell migration. Consequently, reduced DMTF1β levels lead to decreased autophagy and impaired cancer cell migration.
Jun Xu, Nicolas J. Niklaus, Anna M. Schläfli, Igor Tokarchuk, Magali Humbert, Federico La Manna, Bich Vu, David Maul, Ramin Radpour, Marianna Kruithof‐de Julio, Inti Zlobec, Jörn Dengjel, Bruce E. Torbett, Mario P. Tschan   +13 more
wiley   +1 more source