Literature DB >> 34036393

ND‑09 inhibits chronic myeloid leukemia K562 cell growth by regulating BCR‑ABL signaling.

Yan-Hong Liu1, Man Zhu1, Pan-Pan Lei1, Xiao-Yan Pan1, Wei-Na Ma1.   

Abstract

Chronic myeloid leukemia (CML) accounts for approximately 15% of new adult leukemia cases. The fusion gene BCRABL is an important biological basis and target for CML. In the present study, a novel compound, ND‑09, was developed and its inhibitory effect and mechanism of action on CML growth were evaluated using RT‑PCR and western blot analysis. The results showed that ND‑09 demonstrated a high level of inhibitory action toward CML cells overexpressing BCRABL and induced K562 cell apoptosis through the mitochondrial pathway. Notably, combined ND‑09 and BCRABL siRNA treatment could better inhibit cell proliferation and induce apoptosis in K562 cells. Furthermore, this growth effect of BCRABL siRNA could be fully rescued by transfection with BCRABL. ND‑09 exhibited a good fit within BCRABL and occupied its ATP‑binding pocket, thus altering BCRABL kinase activity. Therefore, ND‑09 downregulated the phosphorylation of BCRABL and ABL, ultimately inhibiting the downstream signaling pathways in K562 cells. These findings suggest that ND‑09 induces growth arrest in CML cells by targeting BCRABL.

Entities:  

Keywords:  BCR‑ABL; ND‑09; cell apoptosis; cell cycle; chronic myeloid leukemia

Year:  2021        PMID: 34036393     DOI: 10.3892/or.2021.8087

Source DB:  PubMed          Journal:  Oncol Rep        ISSN: 1021-335X            Impact factor:   3.906


  1 in total

1.  miR-let-7c-3p targeting on Egr-1 contributes to the committed differentiation of leukemia cells into monocyte/macrophages.

Authors:  Fu Qi; Xinping Wang; Shouzhen Zhao; Chaozhe Wang; Ruijing Sun; Huan Wang; Pengchao Du; Jing Wang; Xidi Wang; Guosheng Jiang
Journal:  Oncol Lett       Date:  2022-06-22       Impact factor: 3.111

  1 in total

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