Exploration of N-alkyl-2-[(4-oxo-3-(4-sulfamoylphenyl)-3,4-dihydroquinazolin-2-yl)thio]acetamide derivatives as anticancer and radiosensitizing agents

2019 ◽  
Vol 88 ◽  
pp. 102956 ◽  
Author(s):  
Aiten M. Soliman ◽  
Mostafa M. Ghorab
Keyword(s):  
Radiosensitizing Agents

scholarly journals Deregulated MicroRNA Signature Following Glioblastoma Irradiation

2019 ◽  
Vol 26 (1) ◽  
pp. 107327481984722 ◽  
Author(s):  
Eman A. Toraih ◽  
Aya El-Wazir ◽  
Hoda Y. Abdallah ◽  
Mohamed A. Tantawy ◽  
Manal S. Fawzy
Keyword(s):  
Brain Tumor ◽  
Effective Treatment ◽  
Tumor Cells ◽  
Resistance To Treatment ◽  
Radiosensitizing Agents ◽  
Ectopic Overexpression

Glioblastoma (GBM), the most common and aggressive brain tumor in adults, shows resistance to treatment, particularly radiotherapy. One method for effective treatment is using a group of radiosensitizers that make tumor cells responsive to radiotherapy. A class of molecules whose expression is affected by radiotherapy is the microRNAs (miRNAs) that present promising regulators of the radioresponse. Eighteen miRNAs (miR-26a, -124, -128, -135b, -145, -153, -181a/b, -203, -21, -210, -212, -221/222, -223, -224, -320, and -590), involved in the pathogenesis of GBM and its radioresponsive state, were reviewed to identify their role in GBM and their potential as radiosensitizing agents. MicroRNAs-26a, -124, -128, -145, -153, -181a/b, -203, -221/222, -223, -224, -320, and -590 promoted GBM radiosensitivity, while microRNAs-135b, -21, -210, and -212 encouraged radioresistance. Ectopic overexpression of the radiosensitivity promoting miRNAs and knockdown of the radioresistant miRNAs represent a prospective radiotherapy enhancement opportunity. This offers a glimmer of hope for a group of the most unfortunate patients known to medicine.

Antagonism between radiosensitizing agents

1988 ◽  
Vol 61 (730) ◽  
pp. 976-977
Author(s):  
M. E. Watts ◽  
M. F. Dennis ◽  
M. Woodcock
Keyword(s):  
Radiosensitizing Agents

ChemInform Abstract: POTENTIAL RADIOSENSITIZING AGENTS. DINITROIMIDAZOLES

1979 ◽  
Vol 10 (40) ◽  
Author(s):  
K. C. AGRAWAL ◽  
K. B. BEARS ◽  
R. K. SEHGAL ◽  
J. N. BROWN ◽  
P. E. RIST ◽  
...  
Keyword(s):  
Radiosensitizing Agents

Capsaicin, a novel radiosensitizer, acts via a TRPV6 mediated phenomenon.

2011 ◽  
Vol 29 (7_suppl) ◽  
pp. 23-23 ◽  
Author(s):  
L. Klotz ◽  
N. Venier ◽  
A. J. Colquhoun ◽  
H. Sasaki ◽  
D. A. Loblaw ◽  
...  
Keyword(s):  
Ionizing Radiation ◽  
Western Blot ◽  
Colony Formation ◽  
Transient Receptor Potential ◽  
Significant Inhibition ◽  
Treatment Modalities ◽  
Transient Receptor Potential Vanilloid ◽  
Protein Markers ◽  
Radiosensitizing Agents

23 Background: Radiosensitizing agents sensitize cells to the lethal effects of ionizing radiation (IR). This permits use of lower doses of radiation to achieve equivalent cancer control thereby minimizing adverse effects to normal tissues. Given their lack of toxicity compounds occurring naturally in the diet make ideal potential radiosensitizing agents. Capsaicin, a compound found in the Capsicum sp. of plants, is a widely consumed food additive in areas with low PCa incidence. Traditionally capsaicin is used to treat chronic pain syndromes; however, recently evidence using in vitro PCa models describes its anti-carcinogenic potential. The transient receptor potential vanilloid-receptor (TRPV)-1 and TRPV6 cation selective channels are thought to be partly responsible for mediating these effects. TRPV-1 and TRPV-6 expression is up-regulated in PCa tissue correlating directly with increasing tumor grade. This suggests TRPV1 and/or TRPV6 may be potential therapeutic targets for capsaicin mediated interventions in PCa patients. As IR and capsaicin both promote apoptosis and inhibit cell cycle progression in vitro we hypothesize an at least additive effect of combining these two therapies. Methods: Using clonogenic assays we assessed the effect of ionizing radiation (1-8 Gy) and/or capsaicin (1-10μ M) on colony formation rates in 4 human PCa cell lines (LNCaP, PC3, PC3AR2, DU145). Proliferative, apoptotic, TRPV-6 protein markers were assessed using Western blot analyses. Results: Exposure of cells to capsaicin (1-10μ M) or IR (1-8Gy) caused significant dose-dependent inhibition of colony formation (p<0.001). Combining capsaicin with IR resulted in further significant inhibition of colony formation rates (P<0.001). Western blot analyses showed LNCaP cells treated with capsaicin and/or IR to have increased expression of pro- apoptotic proteins BAX and Bad, tumor-suppressor proteins p21 and p27 and reduced androgen-receptor. Additionally, capsaicin monotherapy caused a dramaticalteration in TRPV1 and TRPV6 expression. Conclusions: These studies confirm the radiosensitizing capacity of capsaicin in PCa cells in vitro. Ongoing studies are further delineating the mechanism of interaction of these treatment modalities. No significant financial relationships to disclose.

Sign in / Sign up

Export Citation Format

Share Document