Results 41 to 50 of about 692,269 (276)

Photoactivation of MDM2 Inhibitors: Controlling Protein-Protein Interaction with Light. [PDF]

J Am Chem Soc, 2018
Selectivity remains a major challenge in anticancer therapy, which potentially can be overcome by local activation of a cytotoxic drug. Such triggered activation can be obtained through modification of a drug with a photoremovable protecting group (PPG), and subsequent irradiation in the chosen place and time.
Hansen MJ, Feringa FM, Kobauri P, Szymanski W, Medema RH, Feringa BL.   +5 more
europepmc   +4 more sources

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

Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction

, 2021
Inhibition of murine double minute 2 (MDM2)-p53 protein–protein interaction with small molecules has been shown to reactivate p53 and inhibit tumor growth. Here, we describe rational, structure-guided, design of novel isoindolinone-based MDM2 inhibitors.
Cully, Sarah J., Riedinger, Christiane, Hardcastle, Ian R., Newell, David R., Blackburn, Timothy J., Carbain, Benoit, Endicott, Jane A., Griffin, Roger J., Johnson, Christopher N., Zhang, Bian, Castro, Juan, Tamanini, Emiliano, Chessari, Gianni, Golding, Bernard T., Vinković, Mladen, Hearn, Keisha, Lunec, John, Wedge, Stephen R., Anil, Burcu, Cano, Celine, Ahn, Jong Sook, St. Denis, Jeffrey D., Fazal, Lynsey, Noble, Martin E. M., Bevan, Luke D., Anscombe, Elizabeth, Hobson, Stephen, Reeks, Judith, Jennings, Claire E., Revill, Charlotte H., Williams, Pamela A., Haggerty, Karen, Holvey, Rhian S., Miller, Duncan C., Thomas, Huw, Thompson, Neil T., Bawn, Ruth H., Cons, Ben, Howard, Steven, Wilsher, Nicola E., Buck, Ildiko, Harnor, Suzannah J., Zhao, Yan   +42 more
core   +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

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, Valentine Jane M, Jane M Valentine, Moumen Abdeladim, Sonia Kumar, Kumar, Sonia, Kumar, S, Moumen, A, Valentine, JM   +11 more
core   +2 more sources

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