The chemotherapeutic CX-5461 primarily targets TOP2B and exhibits selective activity in high-risk neuroblastoma

The chemotherapeutic CX-5461 primarily targets TOP2B and exhibits selective activity in high-risk neuroblastoma

CX-5461 recently progressed through phase I clinical trial as a first-inhuman inhibitor of RNA-POL I. Here, the authors demonstrate that CX-5461 synergizes with topoisomerase I inhibitors to inhibit neuroblastoma cells and that its primary target in this disease is topoisomerase II beta and not RNA-...

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Autores principales: Min Pan, William C. Wright, Richard H. Chapple, Asif Zubair, Manbir Sandhu, Jake E. Batchelder, Brandt C. Huddle, Jonathan Low, Kaley B. Blankenship, Yingzhe Wang, Brittney Gordon, Payton Archer, Samuel W. Brady, Sivaraman Natarajan, Matthew J. Posgai, John Schuetz, Darcie Miller, Ravi Kalathur, Siquan Chen, Jon Patrick Connelly, M. Madan Babu, Michael A. Dyer, Shondra M. Pruett-Miller, Burgess B. Freeman, Taosheng Chen, Lucy A. Godley, Scott C. Blanchard, Elizabeth Stewart, John Easton, Paul Geeleher
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2021
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Science
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Acceso en línea:https://doaj.org/article/eab356ebc3d24e3c88297e4fc7fbc176
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Sumario:CX-5461 recently progressed through phase I clinical trial as a first-inhuman inhibitor of RNA-POL I. Here, the authors demonstrate that CX-5461 synergizes with topoisomerase I inhibitors to inhibit neuroblastoma cells and that its primary target in this disease is topoisomerase II beta and not RNA-POL I.

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