2020
DOI: 10.1111/cbdd.13801
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Recent advances in Bcr‐Abl tyrosine kinase inhibitors for overriding T315I mutation

Abstract: BCR-ABL is a gene produced by the fusion of the bcr gene and the c-abl protooncogene and is considered to be the main cause of chronic myelogenous leukemia (CML) production. Therefore, the development of selective Bcr-Abl kinase inhibitors is an attractive strategy for the treatment of CML. However, in the treatment of CML with a Bcr-Abl kinase inhibitor, the T315I gatekeeper mutant disrupts the important contact interaction between the inhibitor and the enzyme, resistant to the first-and second-generation dru… Show more

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Cited by 41 publications
(26 citation statements)
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“…Novel drugs targeting the mutant form of the protein, such as dasatinib and nilotinib are the only inhibitors that can block the activity of the T315I BCR-ABL mutation. These drugs have been developed to treat relapsed CML patients who have developed resistance to imatinib [40,41]. The acquisition of secondary mutations that prevent drug binding to the target kinase catalytic site, which has been shown for a range of oncogeneaddicted cancers, including EGFR in NSCLC, has been highlighted as a recurrent theme in the landscape of targeted therapy [42].…”
Section: Salient Features Of Oncogene Addictionmentioning
confidence: 99%
“…Novel drugs targeting the mutant form of the protein, such as dasatinib and nilotinib are the only inhibitors that can block the activity of the T315I BCR-ABL mutation. These drugs have been developed to treat relapsed CML patients who have developed resistance to imatinib [40,41]. The acquisition of secondary mutations that prevent drug binding to the target kinase catalytic site, which has been shown for a range of oncogeneaddicted cancers, including EGFR in NSCLC, has been highlighted as a recurrent theme in the landscape of targeted therapy [42].…”
Section: Salient Features Of Oncogene Addictionmentioning
confidence: 99%
“…Some molecules prepared are in the preclinical stage, where many others are employed in the clinical research. Ponatinib is an IMPcontaining drug used in these researches (see Figure 2, compound 2) (2). Another review article states that Ponatinib is approved as an auxilary treatment molecule for chronic myelogenous leukemia (CML) and Philadelphia chromosomepositive acute lymphoblastic leukemia (ALL).…”
Section: Inhibitory Properties Of Imp On Many Enzymes Inhibition Of Bcr-abl Kinase Of Substituted Imidazopyridazine Scaffold As a Trustedmentioning
confidence: 99%
“…For the site-selective sp 2 C−H silylation of azines, Gu et al have devised a base-mediated synthetic method. Authors report that the conditions are mild, the protocol is simple, and for a diverse set of azines, the site selectivity is excellent.…”
Section: Site-selective C-h Silylation Of Azinesmentioning
confidence: 99%
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“…Zeta chain of T-cell receptor-associated protein kinase 70 (ZAP-70), B lymphocyte kinase (BLK), JAK2, tyrosine-protein kinase (LYN) and neurotrophic Receptor Tyrosine Kinase 3 (NTRK3) are found to be the most commonly mutated kinases in CLL [ 24 ]. The abelson tyrosine-protein kinase 1 (ABL1) mutants and their therapeutic inhibitors have been extensively reported to play a critical role in leukaemia and discussed in detail in recent reviews [ 25 , 26 , 27 ].…”
Section: Introductionmentioning
confidence: 99%