Potent and orally efficacious PROTAC degraders of estrogen receptor α (ER α )

被引：0
|
作者：
Rej, Rohan K.
Chen, Zhixiang
Acharyya, Ranjan K.
Wu, Dimin
Hu, Biao
Xu, Guozhang
Nagilla, Rakesh
Metwally, Hoda
Wang, Yu
Wen, Bo
Sun, Duxin
Bai, Longchuan
Wang, Shaomeng
机构：
来源：
CANCER RESEARCH | 2024年 / 84卷 / 06期
关键词：
D O I：
10.1158/1538-7445.AM2024-4510
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
4510
引用
收藏
页数：2
相关论文
共 50 条
  • [31] Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor
    Liu, K
    Xu, LB
    Szalkowski, D
    Li, ZH
    Ding, V
    Kwei, G
    Huskey, S
    Moller, DE
    Heck, JV
    Zhang, BB
    Jones, AB
    JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (19) : 3487 - 3494
  • [32] KRAS-targeted PROTAC degraders are broadly efficacious against KRAS-dependent tumor models
    Smith, Kathryn
    Lopez-Arroyo, Andrea
    Berk, Jason
    Hegan, Peter
    Nower, Peter
    Tice, Samantha
    Moutran, Aurelie
    Pizzano, Jennifer
    Dowtin, Amanda
    Bookbinder, Mark
    Bortolon, Elizabeth
    Cadelina, Greg
    Karim, Fazlul
    Digianantonio, Katie
    Bekes, Miklos
    Medina, Jesus
    MOLECULAR CANCER RESEARCH, 2023, 21 (05)
  • [33] Discovery of potent PROTAC degraders of Pin1 for the treatment of acute myeloid leukemia
    Shi, Yunkai
    Liu, Minmin
    Li, Mengna
    Mao, Yiwen
    Ma, Jingkun
    Long, Ruikai
    Xu, Miaomiao
    Yang, Yaxi
    Wang, Wenlong
    Zhou, Yubo
    Li, Jia
    Zhou, Bing
    CHEMICAL SCIENCE, 2024, 15 (13) : 5027 - 5035
  • [34] Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression
    Chen, Zhixiang
    Wang, Mi
    Wu, Dimin
    Bai, Longchuan
    Xu, Tianfeng
    Metwally, Hoda
    Wang, Yu
    Mceachern, Donna
    Zhao, Lijie
    Li, Ruiting
    Takyi-Williams, John
    Wang, Meilin
    Wang, Lu
    Li, Qiuxia
    Wen, Bo
    Sun, Duxin
    Wang, Shaomeng
    JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (07) : 5275 - 5304
  • [35] Development of a Commercial Manufacturing Process for Vepdegestrant, an Orally Bioavailable PROTAC Estrogen Receptor Degrader for the Treatment of Breast Cancer
    Avery, Steve
    Buske, Jamie M.
    Chen, Doris
    Chen, Herman
    Chen, Xin
    Davidson, Andrew R.
    Desrosiers, Jean-Nicolas
    Dong, Hanqing
    Fellah, Noalle
    Fernandez, David F.
    Grosso, John
    Han, Lu
    Hochdorfer, Teri
    Johnson, Amber M.
    Jones, Brian P.
    Kalinowski, Maciej
    Launer-Felty, Katherine D.
    Lopez, Jorge
    Makowski, Teresa
    Mastriano, Carolyn
    Nguyen, Truong N.
    Patel, Nitinchandra D.
    Peng, Zhihui
    Potter, Tyler
    Pritchard, Robert P.
    Rane, Anil M.
    Reeve, Max
    Richins, Margaret C.
    Salazar, Chase A.
    Salisbury, John J.
    Simpson, Robert
    Tabshey, Liza
    Tweed, Erin J.
    Wahome, Paul G.
    Walsh-Sayles, Nancy
    Willie, Jordan A.
    Wood, Ethan
    ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2024, 28 (11) : 4079 - 4090
  • [36] A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase
    Kaller, Matthew R.
    Harried, Scott S.
    Albrecht, Brian
    Amarante, Patricia
    Babu-Khan, Safura
    Bartberger, Michael D.
    Brown, James
    Brown, Ryan
    Chen, Kui
    Cheng, Yuan
    Citron, Martin
    Croghan, Michael D.
    Graceffa, Russell
    Hickman, Dean
    Judd, Ted
    Kriemen, Chuck
    La, Daniel
    Li, Vivian
    Lopez, Patricia
    Luo, Yi
    Masse, Craig
    Monenschein, Holger
    Nguyen, Thomas
    Pennington, Lewis D.
    Miguel, Tisha San
    Sickmier, E. Allen
    Wahl, Robert C.
    Weiss, Matthew M.
    Wen, Paul H.
    Williamson, Toni
    Wood, Stephen
    Xue, May
    Yang, Bryant
    Zhang, Jianhua
    Patel, Vinod
    Zhong, Wenge
    Hitchcock, Stephen
    ACS MEDICINAL CHEMISTRY LETTERS, 2012, 3 (11): : 886 - 891
  • [37] Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors
    Coburn, CA
    Rush, DM
    Williams, PD
    Homnick, C
    Lyle, EA
    Lewis, SD
    Lucas, BJ
    Di Muzio-Mower, JM
    Juliano, M
    Krueger, JA
    Vastag, K
    Chen, IW
    Vacca, JP
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (10) : 1069 - 1072
  • [38] Identification of the highly potent and orally available ER-targeting PROTAC degrader HP568 for the treatment of breast cancer
    Du, Wu
    Tu, Zhilin
    Qin, Dekun
    Li, Haibo
    Duan, Jingyi
    Liu, Shijuan
    Zhang, Meng
    Nie, Zhenyan
    Yuan, Zhihui
    Li, Jing
    Li, Xinghai
    CANCER RESEARCH, 2024, 84 (07)
  • [39] ERα-Targeting PROTAC as a Chemical Knockdown Tool to Investigate the Estrogen Receptor Function in Rat Menopausal Arthritis
    Duan, Li
    Xu, Xiao
    Xu, Limei
    Wen, Caining
    Ouyang, Kan
    Li, Zigang
    Liang, Yujie
    FRONTIERS IN PHARMACOLOGY, 2021, 12
  • [40] Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119
    Semple, Graeme
    Fioravanti, Beatriz
    Pereira, Guillherme
    Calderon, Imelda
    Uy, Jane
    Choi, Karoline
    Xiong, Yifeng
    Ren, Albert
    Morgan, Michael
    Dave, Vibha
    Thomsen, William
    Unett, David J.
    Xing, Charles
    Bossie, Stuart
    Carroll, Chris
    Chu, Zhi-Liang
    Grottick, Andrew J.
    Hauser, Erin K.
    Leonard, James
    Jones, Robert M.
    JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (17) : 5172 - 5175
12345