Article
BRD4 Inhibition Is Synthetic Lethal with PARP Inhibitors through the Induction of Homologous Recombination Deficiency.
Cancer cell - 12 Mar 2018
Sun Chaoyang, Yin Jun, Fang Yong, Chen Jian, Jeong Kang Jin, Chen Xiaohua, Vellano Christopher P, Ju Zhenlin, Zhao Wei, Zhang Dong, Lu Yiling, Meric-Bernstam Funda, Yap Timothy A, Hattersley Maureen, O'Connor Mark J, Chen Huawei, Fawell Stephen, Lin Shiaw-Yih, Peng Guang, Mills Gordon B
Abstract excerpt
Poly(ADP-ribose) polymerase inhibitors (PARPi) are selectively active in cells with homologous recombination (HR) deficiency (HRD) caused by mutations in BRCA1, BRCA2, and other pathway members. We sought small molecules that induce HRD in HR-competent cells to induce synthetic lethality with PARPi and extend the utility of PARPi. We demonstrated that inhibition of bromodomain containing 4 (BRD4) induced HRD and...
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