Allosteric inhibition of ABL kinases: therapeutic potential in cancer
JK Jones, EM Thompson - Molecular cancer therapeutics, 2020 - AACR
… Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is
effective in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in …
effective in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in …
[HTML][HTML] Allosteric enhancement of the BCR-Abl1 kinase inhibition activity of nilotinib by cobinding of asciminib
B Oruganti, E Lindahl, J Yang, W Amiri… - Journal of Biological …, 2022 - ASBMB
… therapies of asciminib+nilotinib and asciminib+dasatinib in inhibiting BCR-Abl1 kinase activity
over … , nilotinib, and dasatinib. As nilotinib and dasatinib bind different Abl1 conformations (…
over … , nilotinib, and dasatinib. As nilotinib and dasatinib bind different Abl1 conformations (…
Research status, synthesis and clinical application of recently marketed and clinical BCR-ABL inhibitors
XL Xu, YJ Cao, W Zhang… - Current Medicinal …, 2022 - ingentaconnect.com
… The second-generation kinase inhibitors dasatinib and nilotinib were able to overcome …
In this review, two new BCRABL inhibitors (flumatinib and radotinib) and five new BCR-ABL …
In this review, two new BCRABL inhibitors (flumatinib and radotinib) and five new BCR-ABL …
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML
Y Pan, S Zeng, R Hao, M Liang, Z Shen… - European Journal of …, 2022 - Elsevier
… activity of BCR-ABL kinase is 10–20 times stronger in comparison with Imatinib. Nilotinib also
… It is prominent that Nilotinib has a lower frequency of CML recurrence and a higher OS rate …
… It is prominent that Nilotinib has a lower frequency of CML recurrence and a higher OS rate …
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
… Nilotinib, though Nilotinib was highly effective for the V299L mutant bearing patients.
Citation19 In summary, CHMFL-ABL-039 was a highly potent and mutants selective BCR-ABL wt/…
Citation19 In summary, CHMFL-ABL-039 was a highly potent and mutants selective BCR-ABL wt/…
Targeting BCL-2 as a therapeutic strategy for primary p210BCR-ABL1-positive B-ALL cells
M Massimino, E Tirro, S Stella, MS Pennisi, SR Vitale… - in vivo, 2020 - iv.iiarjournals.org
… BCR-ABL expression and pharmacological targeting of BCL-2, by venetoclax, alone or in
combination with BCR-ABL1 … -2 and BCR-ABL1 with venetoclax and nilotinib further increases …
combination with BCR-ABL1 … -2 and BCR-ABL1 with venetoclax and nilotinib further increases …
[HTML][HTML] BCR-ABL1 tyrosine kinase complex signaling transduction: challenges to overcome resistance in chronic myeloid leukemia
GP Amarante-Mendes, A Rana, TS Datoguia… - Pharmaceutics, 2022 - mdpi.com
… 12 months, nilotinib was more efficient than imatinib for the treatment of patients with newly
diagnosed CP-BCR-ABL positive CML, where the complete cytogenetic response of nilotinib-…
diagnosed CP-BCR-ABL positive CML, where the complete cytogenetic response of nilotinib-…
Optimal Response in a Patient With CML Expressing BCR–ABL1 E6A2 Fusion Transcript With Nilotinib Therapy: A Case Report
L Manzella, E Tirro, SR Vitale, A Puma, ML Consoli… - in vivo, 2020 - iv.iiarjournals.org
… BCR–ABL1 e6a2 isoform (24, 57) and because of the young age of patient, we employed
nilotinib … of treatment, and after 14 months of nilotinib therapy she is in complete cytogenetic …
nilotinib … of treatment, and after 14 months of nilotinib therapy she is in complete cytogenetic …
[HTML][HTML] The tyrosine kinase c-Abl potentiates interferon-mediated antiviral immunity by STAT1 phosphorylation
H Liu, Y Cui, Y Bai, Y Fang, T Gao, G Wang, L Zhu… - Iscience, 2021 - cell.com
… Compared to vehicle, administration of the c-Abl/Arg selective inhibitor AMN107 resulted
in significantly increased mortality in mice infected with human influenza virus. Our study …
in significantly increased mortality in mice infected with human influenza virus. Our study …
[HTML][HTML] Efficiency of nilotinib to target chronic phase-chronic myeloid leukaemia primary mature CD34− and immature CD34+ cells
MG Berger, B Lebecque, T Tassin, LT Dannus… - Scientific reports, 2021 - nature.com
… Furthermore, we confirmed that BCR-ABL inhibition is … of nilotinib, suggesting a lower
targeting efficacy of nilotinib in this subset through yet unknown mechanisms. However, nilotinib …
targeting efficacy of nilotinib in this subset through yet unknown mechanisms. However, nilotinib …
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