多发性骨髓瘤
癌症研究
有丝分裂
医学
体内
微核试验
硼替佐米
细胞
不利影响
生物
免疫学
脆弱性(计算)
细胞生长
细胞周期
酪氨酸激酶
血液学
细胞培养
移植
程序性细胞死亡
肿瘤科
肿瘤细胞
突变
激酶
内科学
干细胞
体外
作者
Anaïs Schavgoulidze,Jian Cui,Jessica Encinas,Vanessa Favasuli,Srikanth Talluri,Sabrina Mahéo,Chloé Cerutti,Masood A. Shammas,Daniel Primo,Carmen de Vicente,Marta Larráyoz,José A. Martinez‐Climent,K S Anderson,Anıl Aktaş Samur,Mehmet K. Samur,Herve Avet-Loiseau,Jill Corre,Nikhil C. Munshi,Mariateresa Fulciniti
出处
期刊:Blood
[Elsevier BV]
日期:2026-06-03
标识
DOI:10.1182/blood.2026033819
摘要
Deletion of 17p is among the most adverse cytogenetic abnormalities in multiple myeloma (MM). By integrating RNA-seq data from patient MM cells with genetic dependency data from MM cell lines, we identified the protein kinase membrane-associated tyrosine/threonine 1 (PKMYT1) kinase, a member of the Wee family, as a potential therapeutic target in MM cells harboring del(17p). Genetic suppression or pharmacological inhibition of PKMYT1 activity with the selective inhibitor RP-6306 triggered accumulation of DNA damage, micronucleus formation and mitotic catastrophe, resulting in preferential cell death in del(17p) MM cells while largely sparing del(17p)-negative MM cells and healthy cells. RP-6306 also reduced tumor burden and extended survival in vivo in both xenograft and TP53-deficient syngeneic models. Collectively, our findings nominate PKMYT1 as an actionable target and support PKMYT1 inhibition as a biomarker-driven therapeutic strategy for patients with del(17p)/TP53-deficient MM.
科研通智能强力驱动
Strongly Powered by AbleSci AI