Results 1 to 10 of about 1,097 (111)

Rezatapopt: A promising small-molecule “refolder” specific for TP53Y220C mutant tumors [PDF]

Neoplasia: An International Journal for Oncology Research
Inactivation of p53 due to mutation is observed in approximately half of all human cancer cases, therefore, restoration of the tumor suppressor function of oncogenic p53 mutants represents an attractive and rational therapeutic approach.
Kostas A. Papavassiliou, Alice G. Vassiliou, Athanasios G. Papavassiliou   +2 more
doaj   +2 more sources

Two Step Synthesis of a Non-symmetric Acetylcholinesterase Reactivator

Molecules, 2007
The newly developed and very promising acetylcholinesterase reactivator (E)-1- (2-hydroxyiminomethylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide was prepared using two different pathways via a two-step synthesis involving the ...
Kamil Kuca, Daniel Jun, Kamil Musilek
exaly   +3 more sources

Deep learning untangles the resistance mechanism of p53 reactivator in lung cancer cells [PDF]

iScience, 2023
Summary: Tumor suppressor p53 plays a pivotal role in suppressing cancer, so various drugs has been suggested to upregulate its function. However, drug resistance is still the biggest hurdle to be overcome.
Soo Min Lee, Younghyun Han, Kwang-Hyun Cho   +2 more
doaj   +2 more sources

In-silico drug repositioning studies of Candida albicans Nitrogen permease reactivator 1 (Npr1) kinase [PDF]

Scientific Reports
Npr1 is an essential protein in C. albicans, maintains ion homeostasis and nutrient transportation at cell membrane, and regulates the activity of ammonium transporter protein Mep2.
Sanjib Das, Arka Bagchi, Analava Bera, Arunima Biswas, Analabha Roy, Rik Ganguly, Amalesh Mondal, Deepanjan Chattopadhyay, Paromita Saha Mondal, Tanushree Mondal, Subhasree Samanta, Achintya Mohan Goswami, Tanima Saha   +12 more
doaj   +2 more sources

Tannic acid reactivates HIV-1 latency by mediating CBX4 degradation [PDF]

Journal of Virology
HIV-1 can integrate viral DNA into host cell chromosomes and establish a long-term stable latent viral reservoir, a major obstacle in curing HIV-1 infection. The reactivation of latent proviruses with latency-reversing agents (LRAs) is a prerequisite for
Cancan Chen, Zhihan Zhong, Wanying Zhang, Baijin Xia, Liyang Wu, Liting Liang, Yiwen Zhang, Hui Zhang, Xu Zhang, Ting Pan, Linghua Li, Bingfeng Liu   +11 more
doaj   +2 more sources

PK11007 Covalently Inhibits Thioredoxin Reductase 1 to Induce Oxidative Stress and Autophagy Impairment in NSCLC Cells [PDF]

Antioxidants
Selenoprotein thioredoxin reductase 1 (TXNRD1) is frequently upregulated in various cancer cells to sustain cellular redox homeostasis, and its inhibition has emerged as a promising anti-cancer strategy.
Hanziyi Zhou, Shibo Sun, Haowen Liu, Tong Li, Yiran Xu, Rui Yang, Haiyan Liu, Leiyu He, Weiping Xu, Shui Guan, Jianqiang Xu   +10 more
doaj   +2 more sources

MIRA-1, a p53mut reactivator, is active on Temozolomide-resistant glioblastoma in vitro [PDF]

Molecular Biomedicine
Juan Perdomo, Catherine Gratas, François Paris, Francois M. Vallette, Lisa Oliver   +4 more
doaj   +2 more sources

Cholesterol Oxime Olesoxime Assessed as a Potential Ligand of Human Cholinesterases [PDF]

Biomolecules
Olesoxime, a cholesterol derivative with an oxime group, possesses the ability to cross the blood–brain barrier, and has demonstrated excellent safety and tolerability properties in clinical research.
Dora Kolić, Goran Šinko, Ludovic Jean, Mourad Chioua, José Dias, José Marco-Contelles, Zrinka Kovarik   +6 more
doaj   +2 more sources

Pyridinium-2-carbaldoximes with quinolinium carboxamide moiety are simultaneous reactivators of acetylcholinesterase and butyrylcholinesterase inhibited by nerve agent surrogates

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
The pyridinium-2-carbaldoximes with quinolinium carboxamide moiety were designed and synthesised as cholinesterase reactivators. The prepared compounds showed intermediate-to-high inhibition of both cholinesterases when compared to standard oximes. Their
Hyun Myung Lee, Rudolf Andrys, Jakub Jonczyk, Kyuneun Kim, Avinash G. Vishakantegowda, David Malinak, Adam Skarka, Monika Schmidt, Michaela Vaskova, Kamil Latka, Marek Bajda, Young-Sik Jung, Barbara Malawska, Kamil Musilek   +13 more
doaj   +1 more source

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

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   +1 more source