scholarly journals Identification of a new class of WNT1 inhibitor: Cancer cells migration, G-quadruplex stabilization and target validation

Oncotarget ◽  
2015 ◽  
Vol 7 (42) ◽  
pp. 67986-68001
Author(s):  
Lien-Cheng Chang ◽  
Tsung-Chih Chen ◽  
Shiag-Jiun Chen ◽  
Chun-Liang Chen ◽  
Chia-Chung Lee ◽  
...  
2020 ◽  
Vol 63 (6) ◽  
pp. 3090-3103 ◽  
Author(s):  
Jussara Amato ◽  
Giulia Miglietta ◽  
Rita Morigi ◽  
Nunzia Iaccarino ◽  
Alessandra Locatelli ◽  
...  

2013 ◽  
Vol 23 (24) ◽  
pp. 6721-6727 ◽  
Author(s):  
Jyoti Mareddy ◽  
Suresh Babu Nallapati ◽  
Jayasree Anireddy ◽  
Yumnam Priyadarshini Devi ◽  
Lakshmi Narasu Mangamoori ◽  
...  

2015 ◽  
Vol 2 (1) ◽  
pp. 1
Author(s):  
Christopher G. Hill ◽  
John F. McDonald

The molecular basis of cancer is not merely the consequence of structural and/or regulatory mutations in genes, but additionally to disruptions in networks of regulatory interactions existing among these genes and other components of the genome. Disruptions in network relationships may manifest as the loss, gain or reversal of functionally significant interactive gene relationships in cancer cells. In this study, we first employ an unsupervised (Pearson correlation) approach to quantitatively estimate the overall change in network relationships between precursor (control) ovarian surface epithelial cells and ovarian cancer epithelial cells. We find that ovarian cancer cells display a significant overall reduction in correlated gene network interactions relative to normal precursor cells reflective of an overall loss of regulatory control.  We next focus on gene relationships that qualitatively change between normal and cancer samples. We find that biological processes significantly over represented among differentially expressed genes are substantially different from those associated with genes involved in qualitatively disrupted network interactions. Our findings provide novel insights into the processes underlying ovarian cancer and identify a potential new class of genes for targeted therapy.


RSC Advances ◽  
2017 ◽  
Vol 7 (75) ◽  
pp. 47297-47308 ◽  
Author(s):  
Maysaa M. Saleh ◽  
Charles A. Laughton ◽  
Tracey D. Bradshaw ◽  
Christopher J. Moody

Maintenance of telomeres – specialized complexes that protect the ends of chromosomes – is provided by the enzyme complex telomerase, which is a key factor that is activated in more than 80% of cancer cells, but absent in most normal cells.


2021 ◽  
Author(s):  
Nafisa S. Sirazhetdinova ◽  
Dmitry S Baev ◽  
Victor A. Savelyev ◽  
Tatyana S. Golubeva ◽  
Lyubov S. Klimenko ◽  
...  

Abstract Anthraquinones are of significant interest due to their biological activity, coloring properties and synthetic applications. Here, we describe a mild and convenient method for modification of 1-ethynyl-4-hydroxyanthraquinone that was obtained from the Sonogashira reaction of 1-hydroxy-4-iodoanthraquinone with alkynes. The copper(I) catalyzed one-pot three component reaction (A3-coupling) of the new 1-ethynyl-4-hydroxyanthraquinone with secondary amines and formaldehyde was the main approach for the synthesis of nitrogen substituted 1-[3-(amino)prop-1-ynyl]-4-hydroxyanthraquinones. The influence of different substituent in the amine on reaction rate and yield has been evaluated. The cytotoxicity of 1-ethynyl-4-hydroxyanthraquinones was evaluated using the conventional MTT assay. Among all the compounds synthesized, anthraquinone-propargylamine derivatives 28, 29, 30 and 34 possess most promising cytotoxic potential towards glioblastoma cancer cells; compounds 14 and 19 shown selectivity towards the prostate cancer cells DU-145, and 18, and 24 – towards breast cancer cells MCF-7. The grown inhibition on these cancer cells of 18 and 24 was comparable to those of standard drug Doxorubicin. Molecular modeling of new compounds in DNA G-quadruplex binding site was performed to help understand the observed SAR trends.


2011 ◽  
Vol 54 (5) ◽  
pp. 1140-1156 ◽  
Author(s):  
Valentina Casagrande ◽  
Erica Salvati ◽  
Antonello Alvino ◽  
Armandodoriano Bianco ◽  
Alina Ciammaichella ◽  
...  

2019 ◽  
Vol 47 (12) ◽  
pp. 6059-6072 ◽  
Author(s):  
Ashok Nuthanakanti ◽  
Ishtiyaq Ahmed ◽  
Saddam Y Khatik ◽  
Kayarat Saikrishnan ◽  
Seergazhi G Srivatsan

Abstract Comprehensive understanding of structure and recognition properties of regulatory nucleic acid elements in real time and atomic level is highly important to devise efficient therapeutic strategies. Here, we report the establishment of an innovative biophysical platform using a dual-app nucleoside analog, which serves as a common probe to detect and correlate different GQ structures and ligand binding under equilibrium conditions and in 3D by fluorescence and X-ray crystallography techniques. The probe (SedU) is composed of a microenvironment-sensitive fluorophore and an excellent anomalous X-ray scatterer (Se), which is assembled by attaching a selenophene ring at 5-position of 2′-deoxyuridine. SedU incorporated into the loop region of human telomeric DNA repeat fluorescently distinguished subtle differences in GQ topologies and enabled quantify ligand binding to different topologies. Importantly, anomalous X-ray dispersion signal from Se could be used to determine the structure of GQs. As the probe is minimally perturbing, a direct comparison of fluorescence data and crystal structures provided structural insights on how the probe senses different GQ conformations without affecting the native fold. Taken together, our dual-app probe represents a new class of tool that opens up new experimental strategies to concurrently investigate nucleic acid structure and recognition in real time and 3D.


2020 ◽  
Vol 56 (91) ◽  
pp. 14251-14254
Author(s):  
Marco Deiana ◽  
Jan Jamroskovic ◽  
Ikenna Obi ◽  
Nasim Sabouri

The G4-interactive binding interactions enable one to tune the optical properties of Phen-DC3, allowing the detection of G4 structures in cancer cells.


2018 ◽  
Vol 13 (4) ◽  
pp. 909-914 ◽  
Author(s):  
Gayan Mirihana Arachchilage ◽  
Prakash Kharel ◽  
Joshua Reid ◽  
Soumitra Basu

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