Faculty of Pharmacy, Meijo University, Nagoya, Japan.
Department of Hematology and Oncology, Nagoya University Graduate School of Medicine, Nagoya, Japan.
Int J Hematol. 2011 Feb;93(2):237-242. doi: 10.1007/s12185-011-0766-2. Epub 2011 Jan 25.
BCR-ABL kinase domain mutations were sequentially analyzed in a patient with chronic myeloid leukemia (CML) who exhibited repeated B-lymphoid blast crisis (CML-BC) during treatment with imatinib and dasatinib. We first identified five mutant BCR-ABL clones: Y253H, G250E, F311L, F317L and K294RGG, which was generated by two-nucleotide mutations and six-nucleotide insertion, at the third BC during the imatinib treatment, and retrospectively found that three of them (Y253H, G250E, K294RGG) were already present at the second BC. The in vitro analysis using K294RGG mutant BCR-ABL-expressing 32D cells revealed that K294RGG mutation was imatinib resistant but dasatinib sensitive. Consistent with the in vitro data, the clone with K294RGG mutation was eliminated by the dasatinib treatment in this patient. During the imatinib treatment, several mutant clones emerged and expanded, while additional mutations on the same allele were not acquired. However, after the dasatinib treatment, wild-type BCR-ABL clone disappeared and T315I or F317L mutation was acquired in G250E and Y253H mutant clones on the same allele without the emergence of each sole mutant clone. Cytogenetic and immunoglobulin heavy chain gene rearrangement analysis revealed that all mutant clones that appeared in this patient might be derived from the same CML clone.
BCR-ABL 激酶结构域突变在接受伊马替尼和达沙替尼治疗的慢性髓系白血病(CML)患者中反复发生 B 淋巴细胞样急变期(CML-BC)时进行了连续分析。我们首先在伊马替尼治疗的第三次急变期时鉴定了五个突变 BCR-ABL 克隆:Y253H、G250E、F311L、F317L 和 K294RGG,其由两个核苷酸突变和六个核苷酸插入产生,同时回顾性发现其中三个(Y253H、G250E、K294RGG)在第二次急变期时已经存在。使用 K294RGG 突变 BCR-ABL 表达 32D 细胞的体外分析表明,K294RGG 突变对伊马替尼耐药但对达沙替尼敏感。与体外数据一致,该患者中 K294RGG 突变克隆被达沙替尼治疗消除。在伊马替尼治疗期间,出现了几个突变克隆并不断扩增,而同一等位基因上没有获得其他额外突变。然而,在达沙替尼治疗后,野生型 BCR-ABL 克隆消失,并且在 G250E 和 Y253H 突变克隆上获得了 T315I 或 F317L 突变,而没有单独出现每个突变克隆。细胞遗传学和免疫球蛋白重链基因重排分析表明,该患者中出现的所有突变克隆可能均源自同一 CML 克隆。