scholarly journals JARID1 ‐targeted histone H3 demethylase inhibitors exhibit anti‐proliferative activity and overcome cisplatin resistance in canine oral melanoma cell lines

Author(s):  
Savannah J. Tobin ◽  
Hong Chang ◽  
Michael S. Kent ◽  
Alexander E. Davies
Author(s):  
Jardena Nordenberg ◽  
Israela Perlmutter ◽  
Gad Lavie ◽  
Einat Beery ◽  
Orit Uziel ◽  
...  

Author(s):  
K. Shimizu ◽  
T. Murata ◽  
K. Hiramoto ◽  
M. Narita ◽  
M. Inui ◽  
...  

2017 ◽  
Vol 68 (6) ◽  
pp. 1174-1176
Author(s):  
Corina Danciu ◽  
Ersilia Alexa ◽  
Stefana Avram ◽  
Daliana Minda ◽  
Ioana Zinuca Pavel ◽  
...  

Total polyphenol content and anti proliferative activity of five green tea extracts available on the Romanian pharmaceuticals market was analyzed. Results show dose-dependent anti proliferative activity of the selected samples against B164A5 mouse melanoma and A375 human melanoma cell lines. Sample 3, the richest sample in polyphenols showed the highest anti proliferative potential against the screened melanoma cell lines.


Author(s):  
Sara Huerta-Yepez ◽  
S. Ekmekcioglu ◽  
C. M. Rivera-Pazos ◽  
G. Antonio-Andres ◽  
Mario I. Vega ◽  
...  

Author(s):  
Roberto Campagna ◽  
Eleonora Salvolini ◽  
Veronica Pompei ◽  
Valentina Pozzi ◽  
Alessia Salvucci ◽  
...  

2021 ◽  
Vol 22 (2) ◽  
pp. 537
Author(s):  
Paula Wróblewska-Łuczka ◽  
Aneta Grabarska ◽  
Magdalena Florek-Łuszczki ◽  
Zbigniew Plewa ◽  
Jarogniew J. Łuszczki

(1) Cisplatin (CDDP) is used in melanoma chemotherapy, but it has many side effects. Hence, the search for natural substances that can reduce the dose of CDDP, and CDDP-related toxicity, is highly desired. Coumarins have many biological properties, including anticancer and antiproliferative effects. (2) An in vitro 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay on two human melanoma cell lines (FM55P and FM55M2) examined the antitumor properties of CDDP and five naturally occurring coumarins (osthole, xanthotoxin, xanthotoxol, isopimpinellin, and imperatorin). The antiproliferative effects produced by combinations of CDDP with the coumarins were assessed using type I isobolographic analysis. (3) The most potent anticancer properties of coumarins were presented by osthole and xanthotoxol. These compounds were characterized by the lowest median inhibitory concentration (IC50) values relative to the FM55P and FM55M2 melanoma cells. Isobolographic analysis showed that for both melanoma cell lines, the combination of CDDP and osthole exerted synergistic and additive interactions, while the combination of CDDP and xanthotoxol exerted additive interactions. Combinations of CDDP with xanthotoxin, isopimpinellin, and imperatorin showed antagonistic and additive interactions in two melanoma cell lines. (4) The combination of CDDP and osthole was characterized by the most desirable synergistic interaction. Isobolographic analysis allows the selection of potential candidates for cancer drugs among natural substances.


Cancers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 2012
Author(s):  
Kathryn M. Appleton ◽  
Charuta C. Palsuledesai ◽  
Sean A. Misek ◽  
Maja Blake ◽  
Joseph Zagorski ◽  
...  

The Ras/MEK/ERK pathway has been the primary focus of targeted therapies in melanoma; it is aberrantly activated in almost 80% of human cutaneous melanomas (≈50% BRAFV600 mutations and ≈30% NRAS mutations). While drugs targeting the MAPK pathway have yielded success in BRAFV600 mutant melanoma patients, such therapies have been ineffective in patients with NRAS mutant melanomas in part due to their cytostatic effects and primary resistance. Here, we demonstrate that increased Rho/MRTF-pathway activation correlates with high intrinsic resistance to the MEK inhibitor, trametinib, in a panel of NRAS mutant melanoma cell lines. A combination of trametinib with the Rho/MRTF-pathway inhibitor, CCG-222740, synergistically reduced cell viability in NRAS mutant melanoma cell lines in vitro. Furthermore, the combination of CCG-222740 with trametinib induced apoptosis and reduced clonogenicity in SK-Mel-147 cells, which are highly resistant to trametinib. These findings suggest a role of the Rho/MRTF-pathway in intrinsic trametinib resistance in a subset of NRAS mutant melanoma cell lines and highlight the therapeutic potential of concurrently targeting the Rho/MRTF-pathway and MEK in NRAS mutant melanomas.


Sign in / Sign up

Export Citation Format

Share Document