eLife (2017)
Update date:2022-08-15
Topics:
Raj, Ganesh V.
Sareddy, Gangadhara Reddy
Ma, Shihong
Lee, Tae-Kyung
Viswanadhapalli, Suryavathi
Li, Rui
Liu, Xihui
Murakami, Shino
Chen, Chien-Cheng
Lee, Wan-Ru
Mann, Monica
Krishnan, Samaya Rajeshwari
Manandhar, Bikash
Gonugunta, Vijay K.
Strand, Douglas
Tekmal, Rajeshwar Rao
Ahn, Jung-Mo
Vadlamudi, Ratna K.
The majority of human breast cancer is estrogen receptor alpha (ER) positive. While anti-estrogens/aromatase inhibitors are initially effective, resistance to these drugs commonly develops. Therapy-resistant tumors often retain ER signaling, via interaction with critical oncogenic coregulator proteins. To address these mechanisms of resistance, we have developed a novel ER coregulator binding modulator, ERX-11. ERX-11 interacts directly wiTheR and blocks the interaction between a subset of coregulators with both native and mutant forms of ER. ERX-11 effectively blocks ER-mediated oncogenic signaling and has potent anti-proliferative activity against therapy-sensitive and therapy-resistant human breast cancer cells. ERX-11 is orally bioavailable, with no overt signs of toxicity and potent activity in both murine xenograft and patient-derived breast tumor explant models. This first-in-class agent, with its novel mechanism of action of disrupting critical protein-protein interactions, overcomes the limitations of current therapies and may be clinically translatable for patients with therapy-sensitive and therapy-resistant breast cancers.
View MoreFusilin chemical science & technology co., ltd.
Contact:532-80698166/86057573, +86-400-669-7885
Address:School of Material Science & Engineering, Shandong Uinversity of Science & Technology, Huangdao Zone, Qindao, Shandong
Hefei Highzone Fine Chemical S&T CO.,LTD
Contact:86-0551-63663560
Address:room 1801 NO. 24 Shuguang RD.
Rugao Jinling Chemical Co., Ltd.
Contact:0086-513-68005586
Address:Lianluo new village huangshi town Rugao city Jiangsu Province.
Hangzhou Maytime Bio-Tech Co.,Ltd.
website:http://www.maytime.com.cn
Contact:+86-571-88925295 88920965
Address:NO.2-1701 Ganghui Central Ningwei Street, Xiaoshan Hangzhou Zhejiang China
Nanjing distinctions Medical Technology Co., Ltd.
Contact:+86-15996203785 13914714059
Address:nanjing,jiangsu , China
Doi:10.1039/c2tb00155a
(2013)Doi:10.1016/j.ica.2011.03.007
(2011)Doi:10.1071/CH12440
(2013)Doi:10.1021/ja00002a040
(1991)Doi:10.1021/jo00001a050
(1991)Doi:10.1139/v98-147
(1998)