ATP-binding cassette transporter inhibition by tyrosine kinase inhibitor Nilotinib

Pancreatology ◽  
2012 ◽  
Vol 12 (6) ◽  
pp. 550-551
Author(s):  
K. Quint ◽  
F. Rückert ◽  
M. Ocker
2010 ◽  
Vol 38 (8) ◽  
pp. 1371-1380 ◽  
Author(s):  
Marius Dohse ◽  
Christian Scharenberg ◽  
Suneet Shukla ◽  
Robert W. Robey ◽  
Thorsten Volkmann ◽  
...  

Blood ◽  
2002 ◽  
Vol 99 (5) ◽  
pp. 1860-1862 ◽  
Author(s):  
Wolf-K. Hofmann ◽  
Letetia C. Jones ◽  
Nathan A. Lemp ◽  
Sven de Vos ◽  
Harald Gschaidmeier ◽  
...  

The tyrosine kinase inhibitor STI571 is a promising agent for the treatment of advanced Philadelphia chromosome positive (Ph+) acute lymphoblastic leukemia (ALL), but resistance develops rapidly in most patients after an initial response. To identify mechanisms of resistance to STI571, 30 complementary DNAs (including 9 matched samples) obtained from the bone marrow of individuals with Ph+ ALL were analyzed by direct sequencing of a 714–base pair region of ABL encoding for the adenosine triphosphate (ATP)–binding site and the kinase activation loop. A single point mutation was found at nucleotide 1127 (GI6382056) resulting in Glu255Lys. This mutation occurred in 6 of 9 patients (67%) following their treatment with STI571 but not in the samples from patients before beginning treatment with STI571. Glu255Lys is within the motif important for forming the pocket of the ATP-binding site in ABL and it is highly conserved across species. In conclusion, Ph+ ALL samples resistant to STI571 have a unique mutation Glu255Lys of BCR-ABL.


2018 ◽  
Author(s):  
Hiroyuki Iwasaki ◽  
Haruhiko Yamazaki ◽  
Nobuyasu Suganuma ◽  
Yuko Sugawara ◽  
Naoki Gotoh ◽  
...  

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