ChemInform Abstract: Epothilones: Microtubule Stabilizing Agents with Enhanced Activity Against Multidrug-Resistant Cell Lines and Tumors

ChemInform ◽  
2001 ◽  
Vol 32 (12) ◽  
pp. no-no
Author(s):  
Christina R. Harris ◽  
Aaron Balog ◽  
Kenneth Savin ◽  
Samuel J. Danishefsky ◽  
Ting Chao Chou ◽  
...  
2019 ◽  
Vol 63 (3) ◽  
pp. 1434-1439 ◽  
Author(s):  
Lyn M. Huff ◽  
Sachi Horibata ◽  
Robert W. Robey ◽  
Matthew D. Hall ◽  
Michael M. Gottesman

1992 ◽  
Vol 50 (6) ◽  
pp. 906-911 ◽  
Author(s):  
C. H. M. Versantvoort ◽  
H. J. Broxterman ◽  
N. Feller ◽  
H. Dekker ◽  
C. M. Kuiper ◽  
...  

Nature ◽  
1985 ◽  
Vol 316 (6031) ◽  
pp. 820-823 ◽  
Author(s):  
Norbert Kartner ◽  
Deanna Evernden-Porelle ◽  
Grace Bradley ◽  
Victor Ling

1993 ◽  
Vol 21 (4) ◽  
pp. 378S-378S
Author(s):  
James A. L. Fenton ◽  
Alex Paton ◽  
Nigel Groome ◽  
J. Roger Warr ◽  
Martin G. Rumsby

1990 ◽  
Vol 2 (7) ◽  
pp. 249-259 ◽  
Author(s):  
Kuntebommanahalli N. Thimmaiah ◽  
Julie K. Horton ◽  
Xiao-dong Qian ◽  
William T. Beck ◽  
Janet A. Houghton ◽  
...  

2012 ◽  
Vol 2012 ◽  
pp. 1-15 ◽  
Author(s):  
Benjamin Wiench ◽  
Tolga Eichhorn ◽  
Malte Paulsen ◽  
Thomas Efferth

Chemotherapy is a mainstay of cancer treatment. Due to increased drug resistance and the severe side effects of currently used therapeutics, new candidate compounds are required for improvement of therapy success. Shikonin, a natural naphthoquinone, was used in traditional Chinese medicine for the treatment of different inflammatory diseases and recent studies revealed the anticancer activities of shikonin. We found that shikonin has strong cytotoxic effects on 15 cancer cell lines, including multidrug-resistant cell lines. Transcriptome-wide mRNA expression studies showed that shikonin induced genetic pathways regulating cell cycle, mitochondrial function, levels of reactive oxygen species, and cytoskeletal formation. Taking advantage of the inherent fluorescence of shikonin, we analyzed its uptake and distribution in live cells with high spatial and temporal resolution using flow cytometry and confocal microscopy. Shikonin was specifically accumulated in the mitochondria, and this accumulation was associated with a shikonin-dependent deregulation of cellular Ca2+and ROS levels. This deregulation led to a breakdown of the mitochondrial membrane potential, dysfunction of microtubules, cell-cycle arrest, and ultimately induction of apoptosis. Seeing as both the metabolism and the structure of mitochondria show marked differences between cancer cells and normal cells, shikonin is a promising candidate for the next generation of chemotherapy.


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