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Asciminib is a novel inhibitor of ABL1 and ABL2 gene fusions in ALL but requires the ABL SH3 domain for efficacy.

作者信息

Eadie Laura N, Lagonik Elias, Page Elyse C, Schutz Caitlin E, Heatley Susan L, McClure Barbara J, Forgione Michelle O, Yeung David T, Hughes Timothy P, White Deborah L

机构信息

Blood Cancer Program, Precision Cancer Medicine Theme, South Australian Health and Medical Research Institute, Adelaide, Australia.

Faculty of Health and Medical Sciences, The University of Adelaide, Adelaide, Australia.

出版信息

Blood. 2024 Aug 29;144(9):1022-1026. doi: 10.1182/blood.2024024776.

DOI:10.1182/blood.2024024776
PMID:38848536
Abstract
摘要

相似文献

1
Asciminib is a novel inhibitor of ABL1 and ABL2 gene fusions in ALL but requires the ABL SH3 domain for efficacy.阿西替尼是一种针对急性淋巴细胞白血病中ABL1和ABL2基因融合的新型抑制剂,但发挥疗效需要ABL SH3结构域。
Blood. 2024 Aug 29;144(9):1022-1026. doi: 10.1182/blood.2024024776.
2
Absence of ABL1 exon 2-encoded SH3 residues in BCR::ABL1 destabilizes the autoinhibited kinase conformation and confers resistance to asciminib.BCR::ABL1中缺乏ABL1外显子2编码的SH3结构域会破坏自身抑制激酶构象,并赋予对阿斯科利尼布的抗性。
Leukemia. 2024 Sep;38(9):2046-2050. doi: 10.1038/s41375-024-02353-0. Epub 2024 Jul 31.
3
Asciminib antagonizes transplantable BCR::ABL1-positive lymphoid blast crisis in vivo by targeting malignant stem cells.ASCiminib 通过靶向恶性干细胞在体内拮抗可移植的 BCR::ABL1 阳性淋巴母细胞危象。
Leukemia. 2024 Aug;38(8):1825-1830. doi: 10.1038/s41375-024-02320-9. Epub 2024 Jun 21.
4
Tyrosine kinase inhibitor response of ABL-class acute lymphoblastic leukemia: the role of kinase type and SH3 domain.ABL 类急性淋巴细胞白血病的酪氨酸激酶抑制剂反应:激酶类型和 SH3 结构域的作用。
Blood. 2024 May 23;143(21):2178-2189. doi: 10.1182/blood.2023023120.
5
The e13a3 (b2a3) and e14a3 (b3a3) BCR::ABL1 isoforms are resistant to asciminib.e13a3(b2a3)和e14a3(b3a3)BCR::ABL1亚型对阿斯科利尼布耐药。
Leukemia. 2024 Sep;38(9):2041-2045. doi: 10.1038/s41375-024-02314-7. Epub 2024 Jun 15.
6
BCR::ABL1 kinase N-lobe mutants confer moderate to high degrees of resistance to asciminib.BCR::ABL1 激酶 N 端结构域突变体赋予 ASCIMIB 中等到高度的耐药性。
Blood. 2024 Aug 8;144(6):639-645. doi: 10.1182/blood.2023022538.
7
Crizotinib acts as ABL1 inhibitor combining ATP-binding with allosteric inhibition and is active against native BCR-ABL1 and its resistance and compound mutants BCR-ABL1 and BCR-ABL1.克唑替尼作为一种ABL1抑制剂,兼具ATP结合和变构抑制作用,对天然BCR-ABL1及其耐药和复合突变体BCR-ABL1均有活性。
Ann Hematol. 2021 Aug;100(8):2023-2029. doi: 10.1007/s00277-020-04357-z. Epub 2021 Jun 10.
8
The specificity of asciminib, a potential treatment for chronic myeloid leukemia, as a myristate-pocket binding ABL inhibitor and analysis of its interactions with mutant forms of BCR-ABL1 kinase.ASCIMINIB 的特异性,一种治疗慢性髓性白血病的潜在药物,作为一种豆蔻酰口袋结合的 ABL 抑制剂,并分析其与 BCR-ABL1 激酶突变形式的相互作用。
Leuk Res. 2020 Nov;98:106458. doi: 10.1016/j.leukres.2020.106458. Epub 2020 Sep 29.
9
Thinking outside of ABL1 for resistance to tyrosine kinase inhibitors: a perspective of the SEPT9-ABL1 fusion protein.跳出ABL1思考酪氨酸激酶抑制剂耐药性:SEPT9-ABL1融合蛋白的视角
Leuk Res. 2014 Dec;38(12):1399-400. doi: 10.1016/j.leukres.2014.09.015. Epub 2014 Oct 16.
10
Asciminib and ponatinib combination in Philadelphia chromosome-positive acute lymphoblastic leukemia.阿西替尼与波纳替尼联合用于费城染色体阳性急性淋巴细胞白血病的治疗
Leuk Lymphoma. 2021 Dec;62(14):3558-3560. doi: 10.1080/10428194.2021.1966787. Epub 2021 Aug 18.

引用本文的文献

1
Activity of STAMP inhibitors in rearranged acute lymphoblastic leukemia is dependent on the Abl2 SH3 domain.STAMP抑制剂在重排急性淋巴细胞白血病中的活性依赖于Abl2 SH3结构域。
Blood Neoplasia. 2025 Apr 25;2(3):100109. doi: 10.1016/j.bneo.2025.100109. eCollection 2025 Aug.
2
T-cell acute lymphoblastic leukaemia: subtype prevalence, clinical outcome, and emerging targeted treatments.T细胞急性淋巴细胞白血病:亚型患病率、临床结局及新兴靶向治疗
Leukemia. 2025 Apr 17. doi: 10.1038/s41375-025-02599-2.
3
Absence of ABL1 exon 2-encoded SH3 residues in BCR::ABL1 destabilizes the autoinhibited kinase conformation and confers resistance to asciminib.
BCR::ABL1中缺乏ABL1外显子2编码的SH3结构域会破坏自身抑制激酶构象,并赋予对阿斯科利尼布的抗性。
Leukemia. 2024 Sep;38(9):2046-2050. doi: 10.1038/s41375-024-02353-0. Epub 2024 Jul 31.