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BIOMARKER:

BCR-ABL1 M351T

i
Other names: BCR, BCR Activator Of RhoGEF And GTPase, BCR, RhoGEF And GTPase Activating Protein, Breakpoint Cluster Region Protein, Renal Carcinoma Antigen NY-REN-26, Breakpoint Cluster Region, D22S11, BCR1, BCR/FGFR1 Chimera Protein, FGFR1/BCR Chimera Protein, D22S662, ALL, CML, PHL, ABL proto-oncogene 1, ABL, c-ABL, JTK7, p150, ABL1
Entrez ID:
1m
Occurrence of Existing BCR-ABL Baseline Mutations and Associated Haplotype (NmR) Among CML Patients with Diverse IM Response: A Hospital-based Study from North-East India. (PubMed, Biochem Genet)
Highly polymorphic BCR-ABL kinase domains have been reported to harbor more than a hundred mutations, and among these, 40-60% have been identified as influencers of imatinib mesylate (IM) resistance...A haplotype frequency distribution pattern analysis of ABL1 loci further identified the CGC haplotype as an independent predictor for IM resistance. As such the study highlights the importance of patient characteristics, genotype distribution, and haplotype frequency distribution in predicting the response to IM treatment and clinical outcomes of CML patients.
Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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BCR-ABL1 E255K • BCR-ABL1 Y253H • BCR-ABL1 M351T • ABL1 E255K • ABL1 M351T • ABL1 Y253H
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imatinib
4ms
Asciminib Enhances Its Treatment Efficacy Synergistically in the Treatment of Chronic Myeloid Leukemia Harboring ABL1 Kinase Domain Mutation When Combined with a Reduced Dose of Ponatinib, Dasatinib, or Bosutinib, but Not with Nilotinib or Imatinib (ASH 2023)
The present study demonstrated that a half of baseline conc ABPIs in combination with ASC is as effective as other ABPIs not just in WT but also in other ABL1 KDM CML cell lines. Different CML cell lines harboring different ABL KDM has different treatment spectrum on optimal ABPI drug as well as optimal drug conc. This result will be useful to design future clinical trial of dual blockade of ASC with other ABPIs considering the ABL KDM profiles.
Clinical
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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BCR-ABL1 E255K • BCR-ABL1 F317L • BCR-ABL1 G250E • BCR-ABL1 M244V • ABL1 T315I • BCR-ABL1 M351T • BCR-ABL1 H396P • BCR-ABL1 Y253F • BCR-ABL1 F317V • ABL1 E255K • BCR-ABL1 T315A • ABL1 F317L • ABL1 G250E • ABL1 M351T
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dasatinib • imatinib • Iclusig (ponatinib) • Tasigna (nilotinib) • Bosulif (bosutinib) • Scemblix (asciminib)
over1year
In Vitro Evidence of Double Blockade of Asciminib with Reduced Dose of ATP-Binding Pocket Inhibitors in the Treatment of Chronic Myeloid Leukemia Harboring ABL1 Kinase Domain Mutation (ASH 2022)
ASCEMBL trial showed superior efficacy of ASC to Bosutinib (BOS) with a higher molecular response rate, and a lower rate of discontinuation due to lack of efficacy (24.2% vs 35.5% at week 96)...A phase 1 study attempted to determine appropriate dose of ASC in combination with fixed dose of ABPIs including Imatinib (IMA), Dasatinib (DAS) and Nilotinib (NIL)...Each cell lines does have its inherent resistance level to double blockades, which needs to be further explored. A phase 1 study with reduced dose of ABPI in combination with fixed dose ASC is strongly warranted to define an optimal dose for combination.
Preclinical
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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BCR-ABL1 E255K • BCR-ABL1 Y253H • BCR-ABL1 G250E • BCR-ABL1 M244V • BCR-ABL1 M351T • BCR-ABL1 Y253F • BCR-ABL1 F317V • ABL1 E255K • ABL1 G250E • ABL1 M351T • ABL1 Y253H
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dasatinib • imatinib • Tasigna (nilotinib) • Bosulif (bosutinib) • Scemblix (asciminib)
over2years
Tyrosine kinase domain mutations in chronic myelogenous leukemia patients: A single center experience. (PubMed, J Postgrad Med)
Y253F mutation was not seen in the present study sample. In the present cohort of 83 patients, 29 (35%) cases were positive for single mutation, 12 (14%) had two mutations and 3 (4%) had three mutations.
Clinical • Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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BCR-ABL1 E255K • BCR-ABL1 G250E • BCR-ABL1 M244V • ABL1 T315I • BCR-ABL1 M351T • BCR-ABL1 Y253F • ABL1 E255K • ABL1 G250E • ABL1 M351T
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imatinib
3years
Discovery of a highly potent kinase inhibitor capable of overcoming multiple imatinib-resistant ABL mutants for chronic myeloid leukemia (CML). (PubMed, Eur J Pharmacol)
Although dasatinib and nilotinib have been approved as second-line therapies that could overcome some of these mutants, the most prevalent gatekeeper T315I mutant remains unconquered. CHMFL-48 also exhibited great anti-leukemic efficacies in vivo in K562 cells and p210-T315I-transformed BaF3 cell-inoculated murine models. This discovery extended the pharmacological diversity of BCR-ABL kinase inhibitors and provided more potential options for anti-CML therapies.
Journal
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CRKL (CRK Like Proto-Oncogene, Adaptor Protein)
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BCR-ABL1 E255K • BCR-ABL1 F317L • BCR-ABL1 M351T • BCR-ABL1 Y253F
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dasatinib • imatinib • Tasigna (nilotinib)
over3years
Clinical • New trial
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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BCR-ABL1 V299L • BCR-ABL1 F317L • BCR-ABL1 M244V • BCR-ABL1 M351T • BCR-ABL1 H396R • BCR-ABL1 Q252H • BCR-ABL1 mutation • BCR-ABL1 E355G • BCR-ABL1 L387M • ABL1 F317L • ABL1 L387M • ABL1 M351T
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dasatinib • imatinib • Tasigna (nilotinib) • Hansoh Xinfu (flumatinib)
over3years
[VIRTUAL] Clonal Hematopoiesis with Somatic Mutations in „AYA“ Generation of Patients with Chronic Myeloid Leukemia (ASH 2020)
In patient #6, G645delinsGWfs was found at the diagnosis and on the 3rd line nilotinib treatment...In patient #3, the CSF3R mutation A593V was found at diagnosis and confirmed 14 months after the imatinib initiation...Despite the clonal hematopoiesis with somatic mutations is considered as age-related phenomenon, in AYA CML patients, it may represent a critical problem in achieving sustained molecular response on solo TKI therapy, or even worse, it may result in higher risk of therapy failure and disease progression. Supported by MZCR 00023736
Clinical
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ABL1 (ABL proto-oncogene 1) • RUNX1 (RUNX Family Transcription Factor 1) • ASXL1 (ASXL Transcriptional Regulator 1) • TET2 (Tet Methylcytosine Dioxygenase 2) • ATRX (ATRX Chromatin Remodeler) • CSF3R (Colony Stimulating Factor 3 Receptor) • SIRT1 (Sirtuin 1)
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BCR-ABL1 T315I • ASXL1 mutation • BCR-ABL1 E255K • BCR-ABL1 F317L • BCR-ABL1 M244V • ABL1 T315I • BCR-ABL1 M351T • BCR-ABL1 Q252H • BCR-ABL1 V379I • ABL1 E255K • ABL1 F317L • ABL1 M351T
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imatinib • Tasigna (nilotinib)