Results 11 to 20 of about 10,910 (237)

The Mutant p53-Targeting Compound APR-246 Induces ROS-Modulating Genes in Breast Cancer Cells [PDF]

Translational Oncology, 2018
TP53 is the most frequently mutated gene in human cancer and thus an attractive target for novel cancer therapy. Several compounds that can reactive mutant p53 protein have been identified.
Naoise C. Synnott, Stephen F. Madden, Vladimir J.N. Bykov, John Crown, Klas G. Wiman, Michael J. Duffy   +5 more
doaj   +5 more sources

Mutant p53-reactivating compound APR-246 synergizes with asparaginase in inducing growth suppression in acute lymphoblastic leukemia cells [PDF]

Cell Death and Disease, 2021
Asparaginase depletes extracellular asparagine in the blood and is an important treatment for acute lymphoblastic leukemia (ALL) due to asparagine auxotrophy of ALL blasts.
Sophia Ceder, Sofi E. Eriksson, Ying Yu Liang, Emarndeena H. Cheteh, Si Min Zhang, Kenji M. Fujihara, Julie Bianchi, Vladimir J. N. Bykov, Lars Abrahmsen, Nicholas J. Clemons, Pär Nordlund, Sean G. Rudd, Klas G. Wiman   +12 more
doaj   +2 more sources

APR-246—The Mutant TP53 Reactivator—Increases the Effectiveness of Berberine and Modified Berberines to Inhibit the Proliferation of Pancreatic Cancer Cells [PDF]

Biomolecules, 2022
Pancreatic ductal adenocarcinoma (PDAC) is the most common form of pancreatic cancer. In ~75% of PDAC, the tumor suppressor TP53 gene is mutated. Novel approaches to treat cancer involve compounds called mutant TP53 reactivators.
James Andrew McCubrey, Stephen L. Abrams, Linda S. Steelman, Lucio Cocco, Stefano Ratti, Alberto M. Martelli, Paolo Lombardi, Agnieszka Gizak, Przemysław Duda   +8 more
doaj   +2 more sources

Increased p53 expression induced by APR-246 reprograms tumor-associated macrophages to augment immune checkpoint blockade [PDF]

The Journal of Clinical Investigation, 2022
In addition to playing a major role in tumor cell biology, p53 generates a microenvironment that promotes antitumor immune surveillance via tumor-associated macrophages.
Arnab Ghosh, Judith Michels, Riccardo Mezzadra, Divya Venkatesh, Lauren Dong, Ricardo Gomez, Fadi Samaan, Yu-Jui Ho, Luis Felipe Campesato, Levi Mangarin, John Fak, Nathan Suek, Aliya Holland, Cailian Liu, Mohsen Abu-Akeel, Yonina Bykov, Hong Zhong, Kelly Fitzgerald, Sadna Budhu, Andrew Chow, Roberta Zappasodi, Katherine S. Panageas, Olivier de Henau, Marcus Ruscetti, Scott W. Lowe, Taha Merghoub, Jedd D. Wolchok   +26 more
doaj   +2 more sources

Inhibition of the glutaredoxin and thioredoxin systems and ribonucleotide reductase by mutant p53-targeting compound APR-246 [PDF]

Scientific Reports, 2018
The tumor suppressor p53 is commonly inactivated in human tumors, allowing evasion of p53-dependent apoptosis and tumor progression. The small molecule APR-246 (PRIMA-1Met) can reactive mutant p53 in tumor cells and trigger cell death by apoptosis.
Lena Haffo, Jun Lu, Vladimir J. N. Bykov, Sebastin S. Martin, Xiaoyuan Ren, Lucia Coppo, Klas G. Wiman, Arne Holmgren   +7 more
doaj   +2 more sources

APR-246 as a radiosensitization strategy for mutant p53 cancers treated with alpha-particles-based radiotherapy [PDF]

Cell Death and Disease
Radiation therapy (RT) remains a common treatment for cancer patients worldwide, despite the development of targeted biological compounds and immunotherapeutic drugs.
Or Michaeli, Ishai Luz, Maayan Vatarescu, Tal Manko, Noam Weizman, Yevgeniya Korotinsky, Alexandra Tsitrina, Alex Braiman, Lior Arazi, Tomer Cooks   +9 more
doaj   +2 more sources

Phase Ib study of eprenetapopt (APR-246) in combination with pembrolizumab in patients with advanced or metastatic solid tumors. [PDF]

ESMO Open, 2022
BACKGROUND: We conducted a phase I, multicenter, open-label, dose-finding, and expansion study to determine the safety and preliminary efficacy of eprenetapopt (APR-246) combined with pembrolizumab in patients with advanced/metastatic solid tumors ...
Park H, Shapiro GI, Gao X, Mahipal A, Starr J, Furqan M, Singh P, Ahrorov A, Gandhi L, Ghosh A, Hickman D, Gallacher PD, Wennborg A, Attar EC, Awad MM, Das S, Dumbrava EE.   +16 more
europepmc   +3 more sources

Mechanistic studies of APR-246 in leukemia [PDF]

, 2013
PRIMA-1and its analog APR-246 are novel drugs that restore the active conformation of mutated and unfolded p53 protein and induce apoptosis and cell death in various tumors in pre-clinical models.
Ali, Dina Mahmoud
core   +3 more sources

Targeting of mutant p53 and the cellular redox balance by APR-246 as a strategy for efficient cancer therapy [PDF]

Frontiers in Oncology, 2016
TP53 is the most frequently mutated gene in cancer. The p53 protein activates transcription of genes that promote cell cycle arrest or apoptosis, or regulate cell metabolism and other processes . Missense mutations in TP53 abolish specific DNA binding of
Vladimir J.N. Bykov, Qiang eZhang, Meiqiongzi eZhang, Sophia eCeder, Lars eAbrahmsen, Klas G Wiman   +5 more
doaj   +2 more sources

A combination of p53-activating APR-246 and phosphatidylserine-targeting antibody potently inhibits tumor development in hormone-dependent mutant p53-expressing breast cancer xenografts [PDF]

Breast Cancer: Targets and Therapy, 2018
Yayun Liang,1 Benford Mafuvadze,1 Cynthia Besch-Williford,2 Salman M Hyder1 1Deparment of Biomedical Sciences and Dalton Cardiovascular Research Center, Columbia, MO, USA; 2IDEXX BioResearch, Columbia, MO, USA Background: Between 30 and 40% of human ...
Liang Y, Mafuvadze B, Besch-Williford C, Hyder SM   +3 more
doaj   +2 more sources