Nason-Burchenal K, Maerz W, Albanell J, Allopenna J, Martin P, Moore M A, Dmitrovsky E
Laboratory of Molecular Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY 10021, USA.
Differentiation. 1997 Aug;61(5):321-31. doi: 10.1046/j.1432-0436.1997.6150321.x.
The acute promyelocytic leukemia (APL) t(15;17) rearrangement fuses the promyelocytic leukemia (PML) gene to the retinoic acid receptor-alpha (RAR alpha). There is expression of the chimeric transcript, PML/RAR alpha, in these APL cells. These clinical APL cases respond to the differentiation agent all-trans retinoic acid (ATRA) with complete but not durable remissions because ATRA resistance develops. The NB4 APL cell line expresses PML/RAR alpha and responds to the growth inhibitory and differentiation-inducing signals of ATRA. To identify mechanisms responsible for ATRA resistance in APL, ATRA-resistant NB4 cell lines were derived from parental NB4 cells using different strategies. These lines were resistant to the growth inhibition and differentiation effects of ATRA. ATRA-resistant cells were isolated as a de novo resistant line from parental NB4 cells (NB4-R1), following chemical mutagenization and selection in ATRA (NB4-R2), or after chronic selection in ATRA (NB4-R3). Common defects linked to this ATRA resistance were found. When cultured in ATRA, these resistant cells still express PML, RAR alpha, and PML/RAR alpha proteins. Sequence abnormalities were not detected in the RAR alpha DNA binding domains cloned from a representative RA-resistant NB4 line. In ATRA-sensitive but not ATRA-resistant NB4 cells, ATRA down-regulated retinoid X receptor-alpha (RXR alpha) expression, a known marker of ATRA response in parental NB4 cells. Notably, engineered overexpression of RXR alpha in ATRA-sensitive NB4 cells did not block ATRA-mediated growth suppression. ATRA treatment of these resistant NB4 lines did not signal a decline in telomerase activity or reorganization of PML-associated nuclear bodies, but both events occurred in ATRA-sensitive NB4 cells. These ATRA-resistant NB4 lines are not fully differentiation-defective, since monocytic maturation was induced following treatment with phorbol 12-myristate 13-acetate (PMA) and 1,25 dihydroxy vitamin D3 (vitamin D3). Notably, induced monocytic differentiation of these distinct ATRA-resistant APL lines markedly repressed telomerase activity. Thus, this study suggests that persistent telomerase activity and nuclear body disorganization are linked to ATRA resistance in APL.
急性早幼粒细胞白血病(APL)的t(15;17)重排使早幼粒细胞白血病(PML)基因与维甲酸受体α(RARα)融合。在这些APL细胞中存在嵌合转录本PML/RARα的表达。这些临床APL病例对分化剂全反式维甲酸(ATRA)有反应,可实现完全但不持久的缓解,因为会产生ATRA耐药性。NB4 APL细胞系表达PML/RARα,并对ATRA的生长抑制和分化诱导信号有反应。为了确定APL中ATRA耐药的机制,采用不同策略从亲本NB4细胞中获得了对ATRA耐药的NB4细胞系。这些细胞系对ATRA的生长抑制和分化作用具有抗性。ATRA耐药细胞可作为从亲本NB4细胞中分离出的全新耐药系(NB4-R1),或经化学诱变并在ATRA中筛选后获得(NB4-R2),或经长期在ATRA中筛选后获得(NB4-R3)。发现了与这种ATRA耐药相关的常见缺陷。当在ATRA中培养时,这些耐药细胞仍表达PML、RARα和PML/RARα蛋白。从一个具有代表性的对维甲酸耐药的NB4细胞系克隆的RARα DNA结合域中未检测到序列异常。在对ATRA敏感而非耐药的NB4细胞中,ATRA下调了维甲酸X受体α(RXRα)的表达,这是亲本NB4细胞中ATRA反应的已知标志物。值得注意的是,在对ATRA敏感的NB4细胞中过表达RXRα并不能阻断ATRA介导的生长抑制。用ATRA处理这些耐药的NB4细胞系并未使端粒酶活性下降或PML相关核体发生重组,但这两个事件在对ATRA敏感的NB4细胞中均会发生。这些对ATRA耐药的NB4细胞系并非完全存在分化缺陷,因为在用佛波醇12-肉豆蔻酸酯13-乙酸酯(PMA)和1,25-二羟基维生素D3(维生素D3)处理后可诱导单核细胞成熟。值得注意的是,这些不同的对ATRA耐药的APL细胞系诱导的单核细胞分化显著抑制了端粒酶活性。因此,本研究表明持续的端粒酶活性和核体紊乱与APL中的ATRA耐药有关。