Nutlin-3 sensitizes nasopharyngeal carcinoma cells to cisplatin-induced cytotoxicity. 2015

Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
Molecular Pathology Unit, Cancer Research Centre, Institute for Medical Research, Kuala Lumpur 50588, Malaysia.

The small-molecule inhibitor of p53-Mdm2 interaction, Nutlin-3, is known to be effective against cancers expressing wild-type (wt) p53. p53 mutations are rare in nasopharyngeal carcinoma (NPC), hence targeting disruption of p53-Mdm2 interaction to reactivate p53 may offer a promising therapeutic strategy for NPC. In the present study, the effects of Nutlin-3 alone or in combination with cisplatin, a standard chemotherapeutic agent, were tested on C666-1 cells, an Epstein-Barr virus (EBV)-positive NPC cell line bearing wt p53. Treatment with Nutlin-3 activated the p53 pathway and sensitized NPC cells to the cytotoxic effects of cisplatin. The combined treatment also markedly suppressed soft agar colony growth formation and increased apoptosis of NPC cells. The effect of Nutlin-3 on NPC cells was inhibited by knockdown of p53, suggesting that its effect was p53-dependent. Extended treatment with increasing concentrations of Nutlin-3 did not result in emergence of p53 mutations in the C666-1 cells. Collectively, the present study revealed supportive evidence of the effectiveness of combining cisplatin and Nutlin-3 as a potential therapy against NPC.

UI MeSH Term Description Entries
D007093 Imidazoles Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
D009303 Nasopharyngeal Neoplasms Tumors or cancer of the NASOPHARYNX. Cancer of Nasopharynx,Nasopharyngeal Cancer,Cancer of the Nasopharynx,Nasopharynx Cancer,Nasopharynx Neoplasms,Neoplasms, Nasopharyngeal,Cancer, Nasopharyngeal,Cancer, Nasopharynx,Cancers, Nasopharyngeal,Cancers, Nasopharynx,Nasopharyngeal Cancers,Nasopharyngeal Neoplasm,Nasopharynx Cancers,Nasopharynx Neoplasm,Neoplasm, Nasopharyngeal,Neoplasm, Nasopharynx,Neoplasms, Nasopharynx
D010879 Piperazines Compounds that are derived from PIPERAZINE.
D002277 Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for "cancer." Carcinoma, Anaplastic,Carcinoma, Spindle-Cell,Carcinoma, Undifferentiated,Carcinomatosis,Epithelial Neoplasms, Malignant,Epithelioma,Epithelial Tumors, Malignant,Malignant Epithelial Neoplasms,Neoplasms, Malignant Epithelial,Anaplastic Carcinoma,Anaplastic Carcinomas,Carcinoma, Spindle Cell,Carcinomas,Carcinomatoses,Epithelial Neoplasm, Malignant,Epithelial Tumor, Malignant,Epitheliomas,Malignant Epithelial Neoplasm,Malignant Epithelial Tumor,Malignant Epithelial Tumors,Neoplasm, Malignant Epithelial,Spindle-Cell Carcinoma,Spindle-Cell Carcinomas,Tumor, Malignant Epithelial,Undifferentiated Carcinoma,Undifferentiated Carcinomas
D002945 Cisplatin An inorganic and water-soluble platinum complex. After undergoing hydrolysis, it reacts with DNA to produce both intra and interstrand crosslinks. These crosslinks appear to impair replication and transcription of DNA. The cytotoxicity of cisplatin correlates with cellular arrest in the G2 phase of the cell cycle. Platinum Diamminodichloride,cis-Diamminedichloroplatinum(II),cis-Dichlorodiammineplatinum(II),Biocisplatinum,Dichlorodiammineplatinum,NSC-119875,Platidiam,Platino,Platinol,cis-Diamminedichloroplatinum,cis-Platinum,Diamminodichloride, Platinum,cis Diamminedichloroplatinum,cis Platinum
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077274 Nasopharyngeal Carcinoma A carcinoma that originates in the EPITHELIUM of the NASOPHARYNX and includes four subtypes: keratinizing squamous cell, non-keratinizing, basaloid squamous cell, and PAPILLARY ADENOCARCINOMA. It is most prevalent in Southeast Asian populations and is associated with EPSTEIN-BARR VIRUS INFECTIONS. Somatic mutations associated with this cancer have been identified in NPCR, BAP1, UBAP1, ERBB2, ERBB3, MLL2, PIK3CA, KRAS, NRAS, and ARID1A genes. Carcinoma, Nasopharyngeal,Carcinomas, Nasopharyngeal,Nasopharyngeal Carcinomas
D015398 Signal Transduction The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway. Cell Signaling,Receptor-Mediated Signal Transduction,Signal Pathways,Receptor Mediated Signal Transduction,Signal Transduction Pathways,Signal Transduction Systems,Pathway, Signal,Pathway, Signal Transduction,Pathways, Signal,Pathways, Signal Transduction,Receptor-Mediated Signal Transductions,Signal Pathway,Signal Transduction Pathway,Signal Transduction System,Signal Transduction, Receptor-Mediated,Signal Transductions,Signal Transductions, Receptor-Mediated,System, Signal Transduction,Systems, Signal Transduction,Transduction, Signal,Transductions, Signal
D016159 Tumor Suppressor Protein p53 Nuclear phosphoprotein encoded by the p53 gene (GENES, P53) whose normal function is to control CELL PROLIFERATION and APOPTOSIS. A mutant or absent p53 protein has been found in LEUKEMIA; OSTEOSARCOMA; LUNG CANCER; and COLORECTAL CANCER. p53 Tumor Suppressor Protein,Cellular Tumor Antigen p53,Oncoprotein p53,TP53 Protein,TRP53 Protein,p53 Antigen,pp53 Phosphoprotein,Phosphoprotein, pp53
D017209 Apoptosis A regulated cell death mechanism characterized by distinctive morphologic changes in the nucleus and cytoplasm, including the endonucleolytic cleavage of genomic DNA, at regularly spaced, internucleosomal sites, i.e., DNA FRAGMENTATION. It is genetically programmed and serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth. Apoptosis, Extrinsic Pathway,Apoptosis, Intrinsic Pathway,Caspase-Dependent Apoptosis,Classic Apoptosis,Classical Apoptosis,Programmed Cell Death,Programmed Cell Death, Type I,Apoptoses, Extrinsic Pathway,Apoptoses, Intrinsic Pathway,Apoptosis, Caspase-Dependent,Apoptosis, Classic,Apoptosis, Classical,Caspase Dependent Apoptosis,Cell Death, Programmed,Classic Apoptoses,Extrinsic Pathway Apoptoses,Extrinsic Pathway Apoptosis,Intrinsic Pathway Apoptoses,Intrinsic Pathway Apoptosis

Related Publications

Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
July 2006, Experimental cell research,
Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
March 2010, Chemico-biological interactions,
Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
November 2018, International journal of pharmaceutics,
Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
October 2020, Molecular and cellular probes,
Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
January 2015, Molecular cancer therapeutics,
Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
May 2016, Oncotarget,
Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
December 2016, Die Pharmazie,
Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
February 2007, International journal of oncology,
Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
March 2012, International journal of cancer,
Yee-Lin Voon, and Munirah Ahmad, and Pooi-Fong Wong, and Roslina Husaini, and Wayne Tiong-Weng Ng, and Chee-Onn Leong, and David Philip Lane, and Alan Soo-Beng Khoo
January 2018, Mini reviews in medicinal chemistry,
Copied contents to your clipboard!