The development of imatinib as a therapeutic agent for chronic myeloid leukemia

M Deininger, E Buchdunger, BJ Druker - Blood, 2005 - ashpublications.org
Imatinib has revolutionized drug therapy of chronic myeloid leukemia (CML). Preclinical
studies were promising but the results of clinical trials by far exceeded expectations …

Chronic myeloid leukemia: mechanisms of blastic transformation

D Perrotti, C Jamieson, J Goldman… - The Journal of clinical …, 2010 - Am Soc Clin Investig
The BCR-ABL1 oncoprotein transforms pluripotent HSCs and initiates chronic myeloid
leukemia (CML). Patients with early phase (also known as chronic phase [CP]) disease …

Human chronic myeloid leukemia stem cells are insensitive to imatinib despite inhibition of BCR-ABL activity

AS Corbin, A Agarwal, M Loriaux… - The Journal of …, 2011 - Am Soc Clin Investig
Imatinib therapy, which targets the oncogene product BCR-ABL, has transformed chronic
myeloid leukemia (CML) from a life-threatening disease into a chronic condition. Most …

Pyruvate anaplerosis is a targetable vulnerability in persistent leukaemic stem cells

KM Rattigan, Z Brabcova, D Sarnello, MM Zarou… - Nature …, 2023 - nature.com
Deregulated oxidative metabolism is a hallmark of leukaemia. While tyrosine kinase
inhibitors (TKIs) such as imatinib have increased survival of chronic myeloid leukaemia …

Mechanisms of resistance to ABL kinase inhibition in chronic myeloid leukemia and the development of next generation ABL kinase inhibitors

AB Patel, T O'Hare… - Hematology/Oncology …, 2017 - hemonc.theclinics.com
Every year, more than 8000 new cases of chronic myeloid leukemia (CML) are diagnosed in
the United States. 1 BCR-ABL1, a fusion protein kinase derived from a reciprocal …

Pushing the limits of targeted therapy in chronic myeloid leukaemia

T O'hare, MS Zabriskie, AM Eiring… - Nature Reviews …, 2012 - nature.com
Tyrosine kinase inhibitor (TKI) therapy targeting the BCR-ABL1 kinase is effective against
chronic myeloid leukaemia (CML), but is not curative for most patients. Minimal residual …

Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary CML but does not eliminate the quiescent fraction

M Copland, A Hamilton, LJ Elrick, JW Baird, EK Allan… - Blood, 2006 - ashpublications.org
Abstract Dasatinib (BMS-354825), a novel dual SRC/BCR-ABL kinase inhibitor, exhibits
greater potency than imatinib mesylate (IM) and inhibits the majority of kinase mutations in …

Microenvironmental protection of CML stem and progenitor cells from tyrosine kinase inhibitors through N-cadherin and Wnt–β-catenin signaling

B Zhang, M Li, T McDonald… - Blood, The Journal …, 2013 - ashpublications.org
Tyrosine kinase inhibitors (TKIs) are highly effective in treatment of chronic myeloid
leukemia (CML) but do not eliminate leukemia stem cells (LSCs), which remain a potential …

Bone marrow niche trafficking of miR-126 controls the self-renewal of leukemia stem cells in chronic myelogenous leukemia

B Zhang, LXT Nguyen, L Li, D Zhao, B Kumar, H Wu… - Nature medicine, 2018 - nature.com
Leukemia stem cells (LSCs) in individuals with chronic myelogenous leukemia
(CML)(hereafter referred to as CML LSCs) are responsible for initiating and maintaining …

Effective targeting of quiescent chronic myelogenous leukemia stem cells by histone deacetylase inhibitors in combination with imatinib mesylate

B Zhang, AC Strauss, S Chu, M Li, Y Ho, KD Shiang… - Cancer cell, 2010 - cell.com
Imatinib mesylate (IM) induces remission in chronic myelogenous leukemia (CML) patients
but does not eliminate leukemia stem cells (LSCs), which remain a potential source of …