首页> Bioorganic & medicinal chemistry letters> From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.

From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.

导出原文传递

翻译打印收藏纠错

第一作者： Jun,Liang

第一单位： Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.

作者： Jun,Liang ^[1] ; Sharada,Labadie ^[2] ; Birong,Zhang ^[2] ; Daniel F,Ortwine ^[2] ; Snahel,Patel ^[2] ; Maia,Vinogradova ^[2] ; James R,Kiefer ^[2] ; Till,Mauer ^[2] ; Victor S,Gehling ^[3] ; Jean-Christophe,Harmange ^[3] ; Richard,Cummings ^[3] ; Tommy,Lai ^[4] ; Jiangpeng,Liao ^[4] ; Xiaoping,Zheng ^[4] ; Yichin,Liu ^[2] ; Amy,Gustafson ^[2] ; Erica,Van der Porten ^[2] ; Weifeng,Mao ^[4] ; Bianca M,Liederer ^[2] ; Gauri,Deshmukh ^[2] ; Le,An ^[2] ; Yingqing,Ran ^[2] ; Marie,Classon ^[2] ; Patrick,Trojer ^[3] ; Peter S,Dragovich ^[2] ; Lesley,Murray ^[2]

作者单位： Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com. ^[1] Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. ^[2] Constellation Pharmaceuticals Inc., 215 First Street, Suite 200, Cambridge, MA 02142, USA. ^[3] WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China. ^[4]

关键词 Epigenetics KDM5 KDM5 inhibitors Overcome cancer resistance Structure-based drug discovery