Targeting G-quadruplex DNA Structures by EMICORON has a strong antitumor efficacy against advanced models of human colon cancer

Research output: Contribution to journal › Journal article › Research › peer-review

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Targeting G-quadruplex DNA Structures by EMICORON has a strong antitumor efficacy against advanced models of human colon cancer. / Porru, Manuela; Artuso, Simona; Salvati, Erica; Bianco, Armandodoriano; Franceschin, Marco; Diodoro, Maria Grazia; Passeri, Daniela; Orlandi, Augusto; Savorani, Francesco; D'Incalci, Maurizio; Biroccio, Annamaria; Leonetti, Carlo.

In: Molecular Cancer Therapeutics, Vol. 14, No. 11, 2015, p. 2541-2551.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Porru, M, Artuso, S, Salvati, E, Bianco, A, Franceschin, M, Diodoro, MG, Passeri, D, Orlandi, A, Savorani, F, D'Incalci, M, Biroccio, A & Leonetti, C 2015, 'Targeting G-quadruplex DNA Structures by EMICORON has a strong antitumor efficacy against advanced models of human colon cancer', Molecular Cancer Therapeutics, vol. 14, no. 11, pp. 2541-2551. https://doi.org/10.1158/1535-7163.MCT-15-0253

APA

Porru, M., Artuso, S., Salvati, E., Bianco, A., Franceschin, M., Diodoro, M. G., Passeri, D., Orlandi, A., Savorani, F., D'Incalci, M., Biroccio, A., & Leonetti, C. (2015). Targeting G-quadruplex DNA Structures by EMICORON has a strong antitumor efficacy against advanced models of human colon cancer. Molecular Cancer Therapeutics, 14(11), 2541-2551. https://doi.org/10.1158/1535-7163.MCT-15-0253

Vancouver

Porru M, Artuso S, Salvati E, Bianco A, Franceschin M, Diodoro MG et al. Targeting G-quadruplex DNA Structures by EMICORON has a strong antitumor efficacy against advanced models of human colon cancer. Molecular Cancer Therapeutics. 2015;14(11):2541-2551. https://doi.org/10.1158/1535-7163.MCT-15-0253

Author

Porru, Manuela ; Artuso, Simona ; Salvati, Erica ; Bianco, Armandodoriano ; Franceschin, Marco ; Diodoro, Maria Grazia ; Passeri, Daniela ; Orlandi, Augusto ; Savorani, Francesco ; D'Incalci, Maurizio ; Biroccio, Annamaria ; Leonetti, Carlo. / Targeting G-quadruplex DNA Structures by EMICORON has a strong antitumor efficacy against advanced models of human colon cancer. In: Molecular Cancer Therapeutics. 2015 ; Vol. 14, No. 11. pp. 2541-2551.

Bibtex

@article{e2d0b892a7814bf9808dcf80be9e5594,
title = "Targeting G-quadruplex DNA Structures by EMICORON has a strong antitumor efficacy against advanced models of human colon cancer",
abstract = "We previously identified EMICORON as a novel G-quadruplex (G4) ligand showing high selectivity for G4 structures over the duplex DNA, causing telomere damage and inhibition of cell proliferation in transformed and tumor cells. Here, we evaluated the antitumoral effect of EMICORON on advanced models of human colon cancer that could adequately predict human clinical outcomes. Our results showed that EMICORON was well tolerated in mice, as no adverse effects were reported, and a low ratio of sensitivity across human and mouse bone marrow cells was observed, indicating a good potential for reaching similar blood levels in humans. Moreover, EMICORON showed a marked therapeutic efficacy, as it inhibited the growth of patient-derived xenografts (PDX) and orthotopic colon cancer and strongly reduced the dissemination of tumor cells to lymph nodes, intestine, stomach, and liver. Finally, activation of DNA damage and impairment of proliferation and angiogenesis are proved to be key determinants of EMICORON antitumoral activity. Altogether, our results, performed on advanced experimental models of human colon cancer that bridge the translational gap between preclinical and clinical studies, demonstrated that EMICORON had an unprecedented antitumor activity warranting further studies of EMICORON-based combination treatments. Mol Cancer Ther; 14(11); 2541-51. {\textcopyright}2015 AACR.",
author = "Manuela Porru and Simona Artuso and Erica Salvati and Armandodoriano Bianco and Marco Franceschin and Diodoro, {Maria Grazia} and Daniela Passeri and Augusto Orlandi and Francesco Savorani and Maurizio D'Incalci and Annamaria Biroccio and Carlo Leonetti",
note = "{\textcopyright}2015 American Association for Cancer Research.",
year = "2015",
doi = "10.1158/1535-7163.MCT-15-0253",
language = "English",
volume = "14",
pages = "2541--2551",
journal = "Molecular Cancer Therapeutics",
issn = "1535-7163",
publisher = "American Association for Cancer Research (A A C R)",
number = "11",

}

RIS

TY - JOUR

T1 - Targeting G-quadruplex DNA Structures by EMICORON has a strong antitumor efficacy against advanced models of human colon cancer

AU - Porru, Manuela

AU - Artuso, Simona

AU - Salvati, Erica

AU - Bianco, Armandodoriano

AU - Franceschin, Marco

AU - Diodoro, Maria Grazia

AU - Passeri, Daniela

AU - Orlandi, Augusto

AU - Savorani, Francesco

AU - D'Incalci, Maurizio

AU - Biroccio, Annamaria

AU - Leonetti, Carlo

N1 - ©2015 American Association for Cancer Research.

PY - 2015

Y1 - 2015

N2 - We previously identified EMICORON as a novel G-quadruplex (G4) ligand showing high selectivity for G4 structures over the duplex DNA, causing telomere damage and inhibition of cell proliferation in transformed and tumor cells. Here, we evaluated the antitumoral effect of EMICORON on advanced models of human colon cancer that could adequately predict human clinical outcomes. Our results showed that EMICORON was well tolerated in mice, as no adverse effects were reported, and a low ratio of sensitivity across human and mouse bone marrow cells was observed, indicating a good potential for reaching similar blood levels in humans. Moreover, EMICORON showed a marked therapeutic efficacy, as it inhibited the growth of patient-derived xenografts (PDX) and orthotopic colon cancer and strongly reduced the dissemination of tumor cells to lymph nodes, intestine, stomach, and liver. Finally, activation of DNA damage and impairment of proliferation and angiogenesis are proved to be key determinants of EMICORON antitumoral activity. Altogether, our results, performed on advanced experimental models of human colon cancer that bridge the translational gap between preclinical and clinical studies, demonstrated that EMICORON had an unprecedented antitumor activity warranting further studies of EMICORON-based combination treatments. Mol Cancer Ther; 14(11); 2541-51. ©2015 AACR.

AB - We previously identified EMICORON as a novel G-quadruplex (G4) ligand showing high selectivity for G4 structures over the duplex DNA, causing telomere damage and inhibition of cell proliferation in transformed and tumor cells. Here, we evaluated the antitumoral effect of EMICORON on advanced models of human colon cancer that could adequately predict human clinical outcomes. Our results showed that EMICORON was well tolerated in mice, as no adverse effects were reported, and a low ratio of sensitivity across human and mouse bone marrow cells was observed, indicating a good potential for reaching similar blood levels in humans. Moreover, EMICORON showed a marked therapeutic efficacy, as it inhibited the growth of patient-derived xenografts (PDX) and orthotopic colon cancer and strongly reduced the dissemination of tumor cells to lymph nodes, intestine, stomach, and liver. Finally, activation of DNA damage and impairment of proliferation and angiogenesis are proved to be key determinants of EMICORON antitumoral activity. Altogether, our results, performed on advanced experimental models of human colon cancer that bridge the translational gap between preclinical and clinical studies, demonstrated that EMICORON had an unprecedented antitumor activity warranting further studies of EMICORON-based combination treatments. Mol Cancer Ther; 14(11); 2541-51. ©2015 AACR.

U2 - 10.1158/1535-7163.MCT-15-0253

DO - 10.1158/1535-7163.MCT-15-0253

M3 - Journal article

C2 - 26304235

VL - 14

SP - 2541

EP - 2551

JO - Molecular Cancer Therapeutics

JF - Molecular Cancer Therapeutics

SN - 1535-7163

IS - 11

ER -

ID: 147987233