AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance
T O'Hare, WC Shakespeare, X Zhu, CA Eide… - Cancer cell, 2009 - cell.com
Inhibition of BCR-ABL by imatinib induces durable responses in many patients with chronic
myeloid leukemia (CML), but resistance attributable to kinase domain mutations can lead to …
myeloid leukemia (CML), but resistance attributable to kinase domain mutations can lead to …
Resistance to imatinib: mutations and beyond
P La Rosée, MW Deininger - Seminars in hematology, 2010 - Elsevier
Mechanisms of resistance to the tyrosine kinase inhibitor (TKI) imatinib had been modeled in
vitro even prior to the first reports of clinical resistance in patients with chronic myeloid …
vitro even prior to the first reports of clinical resistance in patients with chronic myeloid …
Potent efficacy of combined PI3K/mTOR and JAK or ABL inhibition in murine xenograft models of Ph-like acute lymphoblastic leukemia
SK Tasian, DT Teachey, Y Li, F Shen… - Blood, The Journal …, 2017 - ashpublications.org
Philadelphia chromosome (Ph)–like B-cell acute lymphoblastic leukemia (Ph-like ALL) is
associated with activated JAK/STAT, Abelson kinase (ABL), and/or phosphatidylinositol 3 …
associated with activated JAK/STAT, Abelson kinase (ABL), and/or phosphatidylinositol 3 …
Pharmacodynamic biomarkers: falling short of the mark?
JF Gainor, DL Longo, BA Chabner - Clinical Cancer Research, 2014 - AACR
In recent years, the clinical development of targeted therapies has been advanced by a
greater understanding of tumor biology and genomics. Nonetheless, drug development …
greater understanding of tumor biology and genomics. Nonetheless, drug development …
In vitro evidence of synergistic efficacy with asciminib combined with reduced dose of ATP-binding pocket tyrosine kinase inhibitors according to the ABL1 kinase …
HJ Han, JJ Kim, D Pyne, A Travas, A Ambalavanan… - Leukemia, 2024 - nature.com
The study initially determined the baseline inhibitory concentration (BIC) for ASC
monotherapy and each ABPI using the K562/WT and BaF3/WT cell lines, respectively …
monotherapy and each ABPI using the K562/WT and BaF3/WT cell lines, respectively …
Higher‐order interactions of Bcr‐Abl can broaden chronic myeloid leukemia (CML) drug repertoire
Y Liu, M Zhang, H Jang, R Nussinov - Protein Science, 2023 - Wiley Online Library
Bcr‐Abl, a nonreceptor tyrosine kinase, is associated with leukemias, especially chronic
myeloid leukemia (CML). Deletion of Abl's N‐terminal region, to which myristoyl is linked …
myeloid leukemia (CML). Deletion of Abl's N‐terminal region, to which myristoyl is linked …
Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines
Abstract Heme oxygenase-1 (HO-1) is a cytoprotective enzyme and a survival-enhancing
factor in a number of cancers. Chronic myeloid leukemia (CML) is a blood cancer caused by …
factor in a number of cancers. Chronic myeloid leukemia (CML) is a blood cancer caused by …
Current views on the interplay between tyrosine kinases and phosphatases in Chronic Myeloid Leukemia
C Boni, C Sorio - Cancers, 2021 - mdpi.com
Simple Summary The chromosomal alteration t (9; 22) generating the BCR-ABL1 fusion
protein represents the principal feature that distinguishes some types of leukemia. An …
protein represents the principal feature that distinguishes some types of leukemia. An …
[HTML][HTML] Prediction of active human dose: learnings from 20 years of Merck KGaA experience, illustrated by case studies
Highlights•A retrospective analysis of active human dose predictions for 15 drugs is
reported.•Case studies illustrate the value of adhering to translational best practices.• …
reported.•Case studies illustrate the value of adhering to translational best practices.• …
[HTML][HTML] LASP1 is a novel BCR-ABL substrate and a phosphorylation-dependent binding partner of CRKL in chronic myeloid leukemia
JJ Frietsch, C Kastner, TGP Grunewald, H Schweigel… - Oncotarget, 2014 - ncbi.nlm.nih.gov
Chronic myeloid leukemia (CML) is characterized by a genomic translocation generating a
permanently active BCR-ABL oncogene with a complex pattern of atypically tyrosine …
permanently active BCR-ABL oncogene with a complex pattern of atypically tyrosine …