Institut Pertanian Bogor

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Institut Pertanian Bogor

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Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle.

Drača, Dijana; Mijatović, Sanja; Krajnović, Tamara; Kaluđerović, Goran N; Wessjohann, Ludger A; Maksimović-Ivanić, Danijela

(2019)

TY  - JOUR
AU  - Drača, Dijana
AU  - Mijatović, Sanja
AU  - Krajnović, Tamara
AU  - Kaluđerović, Goran N
AU  - Wessjohann, Ludger A
AU  - Maksimović-Ivanić, Danijela
PY  - 2019
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3484
UR  - http://ar.iiarjournals.org/content/39/10/5403
AB  - BACKGROUND/AIM Tubugi-1 is a more stable and accessible synthetic counterpart of natural tubulysins. This study aimed to evaluate its cytotoxic potential against anaplastic human melanoma cells. MATERIALS AND METHODS The viability of A-375 cells was determined by 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and crystal violet assay. The type of cell death and proliferative rate were investigated using flow cytometry and fluorescent microscopy, while the molecular background was evaluated by western blot. RESULTS Tubugi-1 reduced the viability of A-375 cells, inducing massive micronucleation, followed by augmented expression of inhibitor of nuclear factor-κB and caspase-2, typical of a mitotic catastrophe. Disturbed proliferation and G2M block with prominent caspase activity, weakened the expression of B-cell lymphoma 2 and B-cell lymphoma 2-associated X transient up-regulation, coexisted with intensive autophagy. Specific inhibition of autophagy by chloroquine resulted in conversion from mitotic catastrophe to rapid apoptosis. CONCLUSION Multilevel anticancer action of tubugi-1 is extended by co-application of an autophagy inhibitor, giving a new dimension in further preclinical advancement of this potential agent.
T2  - Anticancer Research
T1  - Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle.
IS  - 10
VL  - 39
DO  - 10.21873/anticanres.13734
SP  - 5403
EP  - 5415
ER  - 
@article{
author = "Drača, Dijana and Mijatović, Sanja and Krajnović, Tamara and Kaluđerović, Goran N and Wessjohann, Ludger A and Maksimović-Ivanić, Danijela",
year = "2019",
abstract = "BACKGROUND/AIM Tubugi-1 is a more stable and accessible synthetic counterpart of natural tubulysins. This study aimed to evaluate its cytotoxic potential against anaplastic human melanoma cells. MATERIALS AND METHODS The viability of A-375 cells was determined by 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and crystal violet assay. The type of cell death and proliferative rate were investigated using flow cytometry and fluorescent microscopy, while the molecular background was evaluated by western blot. RESULTS Tubugi-1 reduced the viability of A-375 cells, inducing massive micronucleation, followed by augmented expression of inhibitor of nuclear factor-κB and caspase-2, typical of a mitotic catastrophe. Disturbed proliferation and G2M block with prominent caspase activity, weakened the expression of B-cell lymphoma 2 and B-cell lymphoma 2-associated X transient up-regulation, coexisted with intensive autophagy. Specific inhibition of autophagy by chloroquine resulted in conversion from mitotic catastrophe to rapid apoptosis. CONCLUSION Multilevel anticancer action of tubugi-1 is extended by co-application of an autophagy inhibitor, giving a new dimension in further preclinical advancement of this potential agent.",
journal = "Anticancer Research",
title = "Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle.",
number = "10",
volume = "39",
doi = "10.21873/anticanres.13734",
pages = "5403-5415"
}
Drača, D., Mijatović, S., Krajnović, T., Kaluđerović, G. N., Wessjohann, L. A.,& Maksimović-Ivanić, D.. (2019). Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle.. in Anticancer Research, 39(10), 5403-5415.
https://doi.org/10.21873/anticanres.13734
Drača D, Mijatović S, Krajnović T, Kaluđerović GN, Wessjohann LA, Maksimović-Ivanić D. Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle.. in Anticancer Research. 2019;39(10):5403-5415.
doi:10.21873/anticanres.13734 .
Drača, Dijana, Mijatović, Sanja, Krajnović, Tamara, Kaluđerović, Goran N, Wessjohann, Ludger A, Maksimović-Ivanić, Danijela, "Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle." in Anticancer Research, 39, no. 10 (2019):5403-5415,
https://doi.org/10.21873/anticanres.13734 . .
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