Novel pyrazolo [3, 4-d] pyrimidines as dual Src/Bcr-Abl kinase inhibitors: synthesis and biological evaluation for chronic myeloid leukemia treatment

S Di Maria, F Picarazzi, M Mori, A Cianciusi… - Bioorganic …, 2022 - Elsevier
… Dasatinib resulted active against all the imatinib resistant Bcr-Abl point mutations, except
for the T315I one (substitution of the amino acid threonine 315 with isoleucine) [16]. This …

First-line second generation tyrosine kinase inhibitors in patients with newly diagnosed accelerated phase chronic myeloid leukemia

M Balsat, V Alcazer, G Etienne, F Huguet, M Berger… - Leukemia Research, 2023 - Elsevier
… in imatinib-resistant patients: 96.84 % for OS, 93.73 % for PFS here, compared to 82 % for
OS and 66 % for PFS for dasatinib second-line [9]; and 70 % for and 33 % for PFS for nilotinib …

CXCR2, a novel target to overcome tyrosine kinase inhibitor resistance in chronic myelogenous leukemia cells

JH Kim, SJ Lee, KW Kang, BH Lee, Y Park… - Biochemical …, 2021 - Elsevier
… A cytokine array analysis was performed on K562, K562 imatinib-resistant cells (K562/IR),
and … downregulating BCR-ABL and c-Myc expression after SB225002 treatment induced cell …

[HTML][HTML] Management of chronic myeloid leukemia in 2023–common ground and common sense

J Senapati, K Sasaki, GC Issa, JH Lipton… - Blood cancer …, 2023 - nature.com
… -generation BCR::ABL1 tyrosine kinase inhibitors (TKIs) in Philadelphia chromosome (Ph)-positive
chronic myeloid … on treatment options in frontline and subsequent-line CML therapy, …

BCR-ABL1 compound mutants: prevalence, spectrum and correlation with tyrosine kinase inhibitor resistance in a consecutive series of Philadelphia chromosome …

S Soverini, M Martelli, L Bavaro, C De Benedittis… - Leukemia, 2021 - nature.com
second-generation tyrosine kinase inhibitors (TKIs) used for the treatment of chronic myeloid
… They invariably paired one of the most frequent imatinib-resistant mutation hotspots with …

[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
… This led to the development of second generation TKIs. … in the treatment of imatinib-resistant
CML. The advantage of this … portion of BCR-ABL, but rather works as an allosteric inhibitor of …

Genetic alterations in the BCR-ABL1 fusion gene related to imatinib resistance in chronic myeloid leukemia

M Martínez-Castillo, L Gómez-Romero, H Tovar… - Leukemia Research, 2023 - Elsevier
… tyrosine kinase inhibitor imatinib as the first-line treatment in chronic myeloid leukemia (CML…
BCR-ABL mutated chronic myeloid leukemia patients who failed to tyrosine kinase inhibitors

[HTML][HTML] Resistance to tyrosine kinase inhibitors in chronic myeloid leukemia—from molecular mechanisms to clinical relevance

R Alves, AC Gonçalves, S Rutella, AM Almeida… - Cancers, 2021 - mdpi.com
… a critical role in CML by amplifying BCR-ABL signaling [112]. … resistant to TKIs and
Imatinib-resistant cell lines show higher … inhibition of autophagy using second generation

[HTML][HTML] Differentiation of imatinib-resistant chronic myeloid leukemia cells with BCR-ABL-T315I mutation induced by Jiyuan Oridonin A

Y Xu, Z Wang, L Zhang, C Gao, F Li, X Li, Y Ke… - Journal of …, 2023 - ncbi.nlm.nih.gov
… by imatinib and second generation BCR-ABL inhibitor. CML with … but also imatinib -resistant
cells with BCR-ABL mutation, which … the imatinib -resistant induced by inhibitors of BCR-ABL

Molecular mechanisms of tyrosine kinase inhibitor resistance in chronic myeloid leukemia

M Kaehler, I Cascorbi - Precision Medicine, 2023 - Springer
treated using tyrosine kinase inhibitors (TKIs) such as imatinib, which prevent phosphorylation
of downstream targets by blockade of the BCR-ABL kinase… Further, imatinib-resistant CML …