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    BIOMARKER:

    BCR-ABL1 Y253H + BCR-ABL1 T315I

    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:
    25; 613
    Related biomarkers:
    Expression
    Mutation
    CNA
    Fusion
    Others
    15d
    Fluorescence Quantitative PCR Detection of ABL1 Kinase Region Mutations (PubMed, Zhongguo Shi Yan Xue Ye Xue Za Zhi)
    Compared with Sanger sequencing, fluorescence quantitative PCR has higher sensitivity and can screen for low-frequency ABL1 kinase mutations in the early stage. Moreover, it can also perform relative quantitative analysis, so the method has good clinical application prospects for detecting ABL1 mutation.
    Journal
    |
    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
    |
    BCR-ABL1 E255K • BCR-ABL1 Y253H • ABL1 T315I • ABL1 E255K • BCR-ABL1 T315A • ABL1 Y253H • BCR-ABL1 Y253H + BCR-ABL1 T315I
    1year
    Tgrx-678, a Novel Allosteric Inhibitor of BCR-ABL1, Demonstrates Preclinical Anti-Leukemia Activity, High Oral Bioavailability and Synergism with Ponatinib to Suppress the Highly Resistant Compound Mutations (ASH 2023)
    ABL1 is subject to auto-inhibition mediated by myristoylation-triggered conformational change, which can be exploited to overcome resistance, as validated by allosteric inhibitors such as GNF2, GNF5 and asciminib. Furthermore, TGRX-678 and ponatinib synergize to overcome the clinically challenging resistance conferred by T315M or T315I-inclusive compound mutations. This data warrant further clinical investigation of TGRX-678 for the treatment of resistant or refractory CML patients.
    Preclinical
    |
    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
    |
    BCR-ABL1 T315I • BCR-ABL1 E255K • BCR-ABL1 Y253H • BCR-ABL1 E255V • BCR-ABL1 G250E • ABL1 T315I • BCR-ABL1 Q252H • ABL1 E255K • ABL1 G250E • ABL1 Y253H • BCR-ABL1 T315M • BCR-ABL1 Y253H + BCR-ABL1 T315I
    |
    Iclusig (ponatinib) • Scemblix (asciminib) • TGRX-678