PBA2, a novel inhibitor of imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia

2016 ◽  
Vol 383 (2) ◽  
pp. 220-229 ◽  
Author(s):  
Pranav Gupta ◽  
Rishil J. Kathawala ◽  
Liuya Wei ◽  
Fang Wang ◽  
XiaoKun Wang ◽  
...  
Keyword(s):  
Chronic Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Imatinib Resistant ◽  
T315i Mutation

HS-438, a new inhibitor of Imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia

2014 ◽  
Vol 348 (1-2) ◽  
pp. 50-60 ◽  
Author(s):  
Sun-Mi Yun ◽  
Kyung Hee Jung ◽  
Soo Jung Kim ◽  
Zhenghuan Fang ◽  
Mi Kwon Son ◽  
...  
Keyword(s):  
Chronic Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Imatinib Resistant ◽  
T315i Mutation

scholarly journals CD-200 induces apoptosis and inhibits Bcr-Abl signaling in imatinib-resistant chronic myeloid leukemia with T315I mutation

2015 ◽  
Vol 47 (1) ◽  
pp. 253-261 ◽  
Author(s):  
ZHENGHUAN FANG ◽  
KYUNG HEE JUNG ◽  
HONG HUA YAN ◽  
SOO JUNG KIM ◽  
MI KWON SON ◽  
...  
Keyword(s):  
Chronic Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Imatinib Resistant ◽  
T315i Mutation

Abstract 5389: Novel kinase inhibitor for imatinib-resistant chronic myeloid leukemia with T315I mutation

2015 ◽  
Author(s):  
Soon-Sun Hong ◽  
Soo Jung Kim ◽  
Kyung Hee Jung ◽  
Hong Hua Yan ◽  
Zhenghuan Fang ◽  
...  
Keyword(s):  
Chronic Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Kinase Inhibitor ◽  
Imatinib Resistant ◽  
T315i Mutation

PHA-680626 Exhibits Anti-Proliferative and Pro-Apoptotic Activity on Imatinib-Resistant Chronic Myeloid Leukemia Cell Lines and Primary CD34+ Cells by Inhibition of Both Bcr-Abl Tyrosine Kinase and Aurora Kinases.

Blood ◽  
2007 ◽  
Vol 110 (11) ◽  
pp. 4568-4568
Author(s):  
Artur Gontarewicz ◽  
Stefan Balabanov ◽  
Gunhild Keller ◽  
Jens Panse ◽  
Mirja Bernhardt ◽  
...  
Keyword(s):  
Chronic Myeloid Leukemia ◽  
Cell Lines ◽  
Myeloid Leukemia ◽  
Histone H3 ◽  
Leukemia Cell ◽  
Aurora Kinase ◽  
Aurora Kinases ◽  
Imatinib Resistant ◽  
Cd34 Cells ◽  
T315i Mutation

Abstract Emergence of resistance to Imatinib complicates the treatment of chronic myeloid leukemia (CML). Second-generation Bcr-Abl inhibitors are capable to overcome resistance mediated by most mutations except T315I. As this mutation is causative for ∼20% of clinically observed resistances, the need for novel treatment strategies becomes obvious. Here, we report on a novel kinase inhibitor PHA-680626 exhibiting strong inhibitory activity on both Bcr-Abl and Aurora kinases. Significant anti-proliferative and pro-apoptotic effects were observed in human BCR-ABL positive cell lines and murine BaF3 cells ectopically expressing wt BCR-ABL or the Imatinib resistant BCR-ABL mutants M351T, E255K and T315I. Treatment with PHA-680626 decreased phosphorylation of CrkL and histone H3. As CrkL represents a typical down-stream target of Bcr-Abl while histone H3 phosphorylation is an indicator for Aurora kinase B activity, these findings indicate that effects of PHA-680626 are mediated via inhibition of both pathways. Moreover, high antiproliferative activity of PHA-680626 was observed in primary CD34+ cells derived from CML patients at diagnosis or in blast crisis as well as from an individual harbouring the T315I mutation. Thus, both Bcr-Abl and Aurora kinase inhibition contribute to the efficacy of PHA-680626 against Imatinib-resistant BCR-ABL positive leukemias, particularly those harbouring the T315I mutation.

scholarly journals Prevalence of BCR-ABL T315I Mutation in Malaysian Patients with Imatinib-Resistant Chronic Myeloid Leukemia

2018 ◽  
Vol 19 (12) ◽  
pp. 3317-3320 ◽  
Author(s):  
Yuslina Mat Yusoff ◽  
Zahidah Abu Seman ◽  
Norodiyah Othman ◽  
Nor Rizan Kamaluddin ◽  
Ezalia Esa ◽  
...  
Keyword(s):  
Chronic Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Imatinib Resistant ◽  
T315i Mutation

scholarly journals MicroRNA expression profiling in Imatinib-resistant Chronic Myeloid Leukemia patients without clinically significant ABL1-mutations

2009 ◽  
Vol 8 (1) ◽  
pp. 69 ◽  
Author(s):  
Edurne San José-Enériz ◽  
José Román-Gómez ◽  
Antonio Jiménez-Velasco ◽  
Leire Garate ◽  
Vanesa Martin ◽  
...  
Keyword(s):  
Chronic Myeloid Leukemia ◽  
Expression Profiling ◽  
Myeloid Leukemia ◽  
Microrna Expression ◽  
Imatinib Resistant ◽  
Clinically Significant

scholarly journals Mechanisms of AXL overexpression and function in Imatinib-resistant chronic myeloid leukemia cells

Oncotarget ◽  
2011 ◽  
Vol 2 (11) ◽  
pp. 874-885 ◽  
Author(s):  
Maeva Dufies ◽  
Arnaud Jacquel ◽  
Nathalie Belhacene ◽  
Guillaume Robert ◽  
Thomas Cluzeau ◽  
...  
Keyword(s):  
Chronic Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Leukemia Cells ◽  
Imatinib Resistant ◽  
And Function
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