medRxiv Oncology· Sfeir, A., Rosen, E., Mathieu, M.-C., Ferraro, G. B., Mochirian, P., Godbout, C., Poirier, H., Fournier, S., Henry, D. A., Kim, H., Papp, R., Yin, S. Y., Leclaire, M.-E., Houle, R., Nejad, P., Schonhoft, J. D., Zahn, K., Black, W. C., Gallant, M., Kim, I., Ulanet, D., Basciano, P., Veloso, A., Rimkunas, V., Yap, T. A., Guo, R., Mai, N., Koehler, M., Zinda, M., Roulston, A., Zimmermann, M., Morris, S. J. ·· 10 天前精选评分59
Polθ抑制剂RP-3467临床前验证及在携带TP53BP1耐药突变的gBRCA1卵巢癌患者中显示临床应答
Targeting Polθ Helicase with RP-3467: Preclinical Validation and Clinical Response in a gBRCA1 ovarian cancer patient with an acquired PARPi resistance mutation in TP53BP1
导读
RP-3467是一种靶向DNA聚合酶θ（Polθ）ATP酶结构域的新型小分子抑制剂，临床前研究显示其在HR缺陷模型中诱导合成致死并与PARP抑制剂（奥拉帕利、鲁卡帕利）协同，在多个人源肿瘤异种移植模型中实现持续肿瘤消退。
来源：medRxiv Oncology · medrxiv.org