Results 101 to 110 of about 692,269 (276)

The facile and visualizable identification of broad-spectrum inhibitors of MDM2/p53 using co-expressed protein complexes.

, 2019
MDM2 is a well-known oncoprotein overexpressed in a variety of cancers, and the identification of inhibitors that disrupt the MDM2/p53 interaction is of great interest in anticancer drug development.
Peng, Junhui, Qu, Yun, Yang, Jiaxiang, Tong, Yang, Sheng, Yaping, Farrell, Nicholas P, Yang, Yang, Wells, Thomas, Yuan, Siming, Li, Zigang, Liu, Yangzhong, Dong, Zhiqiang, Hu, Hongze   +12 more
core   +1 more source

Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides. [PDF]

, 2019
Herein, we describe the development of a novel staple with an electrophilic warhead to enable the generation of stapled peptide covalent inhibitors of the p53-MDM2 protein-protein interaction (PPI).

core   +2 more sources

NSUN3‐Associated m5C Modification of tRF5‐GlyTCC Suppresses Colorectal Cancer Progression via RPL23‐Linked Nucleolar Stress and p53‐Associated Autophagy and Enhances 5‐FU Sensitivity

Advanced Science, EarlyView.
This study identifies that NSUN3‐mediated m5C modification stabilizes tRF5‐GlyTCC, linking ribosomal homeostasis, nucleolar stress responses, and p53 signaling changes. This regulatory axis suppresses colorectal cancer and enhances chemotherapy response to 5‐FU, positioning tRF5‐GlyTCC as a potential therapeutic target for improving drug sensitivity in
Xinhui Lv, Can Tang, Feiyang Song, Yu Wu, Yafang Chen, Sicong Liu, Ziwen Yuan, Guihua Wang, Xudong Wang   +8 more
wiley   +1 more source

A Multistrategy AI‐Assisted Consensus Screening Pipeline for Discovery of Candidate p53 Monomer Binders

Advanced Intelligent Discovery, EarlyView.
An ultra‐fast small‐sample AI consensus pipeline combines co‐folding and docking to target structure‐lacking p53 monomers. Its optimal mini‐protein binder shows robust interfacial affinity and promising druggability, supplying unprecedented antitumor p53 templates.
Ningyao Li, Xueyi Liu, Qiuyue Li, Chengfeng Yue, Xin Li, Yugang Huang, Xin Deng, Junfei Zhang, Xue Liang, Guodong Ye   +9 more
wiley   +1 more source

Chromosomal Abnormalities, Drug Sensitivity and Resistance in Hematological Malignancies: A Comprehensive Overview by the Francophone Group of Hematological Cytogenetics (GFCH)

American Journal of Hematology, EarlyView.
ABSTRACT Chromosomal abnormalities have a major clinical impact on hematological malignancies, particularly with regard to treatment strategies. To preserve and consolidate fundamental knowledge in this rapidly evolving field, the Francophone Group of Hematological Cytogenetics (Groupe Francophone de Cytogénétique Hématologique, GFCH) conducted a ...
Florence Nguyen‐Khac, Audrey Bidet, Elise Chapiro, Nathalie Douet‐Guilbert, Jean‐Baptiste Gaillard, Nada Assaf, Nathalie Auger, Hend Chaker, Jasmine Chauzeix, Inge Govaerts, Hippolyte Guérineau, Christine Lefebvre, Pauline Roynard, Hélène Guermouche, Lucienne Michaux, Marie‐Bérengère Troadec, Lauren Véronèse   +16 more
wiley   +1 more source

MDM2-mediated degradation of p14ARF: a novel mechanism to control ARF levels in cancer cells.

PLoS ONE, 2015
We here show a new relationship between the human p14ARF oncosuppressor and the MDM2 oncoprotein. MDM2 overexpression in various cancer cell lines causes p14ARF reduction inducing its degradation through the proteasome.
Maria Vivo, Maria Matarese, Maria Sepe, Rosaria Di Martino, Luisa Festa, Viola Calabrò, Girolama La Mantia, Alessandra Pollice   +7 more
doaj   +1 more source

MDM2: current research status and prospects of tumor treatment

Cancer Cell International
Mousedouble minute 2 (MDM2) is one of the molecules activated by p53 and plays an important role in the regulation of p53. MDM2 is generally believed to function as a negative regulator of p53 by facilitating its ubiquitination and subsequent degradation.
Yumei Yao, Qian Zhang, Zhi Li, Hushan Zhang   +3 more
doaj   +1 more source

Efficacy, safety and cost‐effectiveness of CAR‐T therapy

British Journal of Clinical Pharmacology, EarlyView.
CAR T‐cells demonstrate high efficacy in blood cancers, including ALL, MM and DLBCL. Innovations target solid tumours despite challenges such as antigen escape. Combination therapies enhance the delivery and infiltration of CAR T cells. Toxicity, cost and resistance remain major barriers to clinical use.
Emina Karahmet Sher, Amina Džidić‐Krivić, Emma Pinjic, Nejra Selak, Kanita Omerbasic, Alexandar Chupin, Andrej Belancic, Almir Fajkic   +7 more
wiley   +1 more source

Ribosome biogenesis rate, a parameter of sensitivity to chemotherapeutic drugs inhibiting rRNA synthesis

Oncology Reviews
Many drugs currently used in cancer chemotherapy exert their toxic action mainly by inhibiting ribosome biogenesis (RiBi). This is due to the fact that after inhibition of rRNA transcription ribosomal proteins, no longer used for ribosome building, bind ...
Davide Treré, Davide Treré, Lorenzo Montanaro, Lorenzo Montanaro, Massimo Derenzini, Claudio Agostinelli, Claudio Agostinelli, Enrico Derenzini, Enrico Derenzini   +8 more
doaj   +1 more source

A novel inhibitor of MDM2 oncogene blocks metastasis of hepatocellular carcinoma and overcomes chemoresistance

Genes and Diseases, 2019
Overexpression of the MDM2 oncogene and mutations in the p53 tumor suppressor commonly occur in hepatocellular carcinoma (HCC) and are associated with increased mortality due to this disease.
Wei Wang, Bo Hu, Jiang-Jiang Qin, Jian-Wen Cheng, Xin Li, Mehrdad Rajaei, Jia Fan, Xin-Rong Yang, Ruiwen Zhang   +8 more
doaj   +1 more source