Discovery of a highly potent kinase inhibitor capable of overcoming multiple imatinib-resistant ABL mutants for chronic myeloid leukemia (CML)
T Lu, J Cao, F Zou, X Li, A Wang, W Wang… - European Journal of …, 2021 - Elsevier
As the critical driving force for chronic myeloid leukemia (CML), BCR gene fused ABL kinase
has been extensively explored as a validated target of drug discovery. Although imatinib has …
has been extensively explored as a validated target of drug discovery. Although imatinib has …
Discovery and characterization of a novel highly potent and selective type II native and drug-resistant V299L mutant BCR-ABL inhibitor (CHMFL-ABL-039) for Chronic …
J Wu, A Wang, X Li, C Chen, Z Qi, C Hu… - Cancer Biology & …, 2019 - Taylor & Francis
ABSTRACT BCR fused ABL kinase is the critical driving oncogene for chronic myeloid
leukemia (CML) and has been extensively studied as the drug discovery target in the past …
leukemia (CML) and has been extensively studied as the drug discovery target in the past …
Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia
E Weisberg, PW Manley, SW Cowan-Jacob… - Nature Reviews …, 2007 - nature.com
Imatinib, a small-molecule ABL kinase inhibitor, is a highly effective therapy for early-phase
chronic myeloid leukaemia (CML), which has constitutively active ABL kinase activity owing …
chronic myeloid leukaemia (CML), which has constitutively active ABL kinase activity owing …
New Bcr-Abl inhibitors in chronic myeloid leukemia: keeping resistance in check
T O'Hare, CA Eide, MW Deininger - Expert opinion on …, 2008 - Taylor & Francis
Targeted therapy with the Abl kinase inhibitor imatinib has markedly improved the outlook
for patients with chronic myeloid leukemia (CML). Breakpoint cluster region (Bcr)-Abl …
for patients with chronic myeloid leukemia (CML). Breakpoint cluster region (Bcr)-Abl …
[HTML][HTML] 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 …
Abl tyrosine kinase inhibitors for overriding Bcr–Abl/T315I: from the second to third generation
R Tanaka, S Kimura - Expert review of anticancer therapy, 2008 - Taylor & Francis
Treatment of chronic myeloid leukemia (CML) has changed drastically with the emergence
of the Abl tyrosine kinase inhibitor (TKI), imatinib mesylate. However, primary and secondary …
of the Abl tyrosine kinase inhibitor (TKI), imatinib mesylate. However, primary and secondary …
Preclinical development of a novel BCR-ABL T315I inhibitor against chronic myeloid leukemia
Abstract Chronic Myeloid Leukemia (CML) is a myeloproliferative neoplasm primarily due to
the presence of the BCR-ABL fusion gene that produces the constitutively active protein …
the presence of the BCR-ABL fusion gene that produces the constitutively active protein …
Therapeutic Options Against BCR-ABL1 T315I-Positive Chronic Myelogenous Leukemia
A Quintás-Cardama, J Cortes - Clinical Cancer Research, 2008 - AACR
Despite the efficacy of imatinib therapy in chronic myelogenous leukemia, the development
of resistance continues to challenge the treatment of this disease. Mutations within the …
of resistance continues to challenge the treatment of this disease. Mutations within the …
[HTML][HTML] Discovery and characterization of a novel potent type II native and mutant BCR-ABL inhibitor (CHMFL-074) for Chronic Myeloid Leukemia (CML)
F Liu, B Wang, Q Wang, Z Qi, C Chen, LL Kong… - Oncotarget, 2016 - ncbi.nlm.nih.gov
BCR gene fused ABL kinase is the critical driving force for the Philadelphia Chromosome
positive (Ph+) Chronic Myeloid Leukemia (CML) and has been extensively explored as a …
positive (Ph+) Chronic Myeloid Leukemia (CML) and has been extensively explored as a …
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region–abelson (Bcr-Abl) kinase …
X Ren, X Pan, Z Zhang, D Wang, X Lu… - Journal of medicinal …, 2013 - ACS Publications
Bcr-AblT315I mutation-induced imatinib resistance remains a major challenge for clinical
management of chronic myelogenous leukemia (CML). Herein, we report GZD824 (10a) as …
management of chronic myelogenous leukemia (CML). Herein, we report GZD824 (10a) as …