Discovery of potent, selective, and orally bioavailable GSPT1 degraders and their preclinical anti-tumor activity in acute myeloid leukemia and solid tumors

被引：0
|
作者：
Joo, Min Sung
Lee, JaeYung
Kim, Eun-Jung
Ki, Dong Hyuk
Choi, Hunmi
Nam, Joonwoo
Park, Jaewoo
Kang, Keon Wook
Han, Wooseok
机构：
来源：
CANCER RESEARCH | 2023年 / 83卷 / 07期
关键词：
D O I：
10.1158/1538-7445.AM2023-1673
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
1673
引用
收藏
页数：2
相关论文
共 50 条
  • [1] Discovery of new Lenalidomide derivatives as potent and selective GSPT1 degraders
    Wei, Yiying
    Xu, Xinxin
    Jiang, Minchuan
    Wang, Yongxing
    Zhou, Yang
    Wang, Zhen
    Zhang, Zhang
    Zhou, Fengtao
    Ding, Ke
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 258
  • [2] Design and Discovery of Preclinical Candidate LYG-409 as a Highly Potent and Selective GSPT1 Molecular Glue Degraders
    Zhang, Yanqing
    Liu, Wenjing
    Tong, Chao
    Wang, Xinhong
    Chang, Xiujin
    Qu, Fangui
    Zhang, Zhiming
    Fan, Zhongpen
    Zhao, Monong
    Tang, Cheng
    Song, Beichen
    Ding, Ming
    Qiu, Zhixia
    Wang, Jubo
    Bian, Jinlei
    Li, Zhiyu
    Wu, Hongxi
    Xu, Xi
    JOURNAL OF MEDICINAL CHEMISTRY, 2025, 68 (03) : 2608 - 2638
  • [3] Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators
    Nishiguchi, Gisele
    Keramatnia, Fatemeh
    Min, Jaeki
    Chang, Yunchao
    Jonchere, Barbara
    Das, Sourav
    Actis, Marisa
    Price, Jeanine
    Chepyala, Divyabharathi
    Young, Brandon
    McGowan, Kevin
    Slavish, P. Jake
    Mayasundari, Anand
    Jarusiewicz, Jamie A.
    Yang, Lei
    Li, Yong
    Fu, Xiang
    Garrett, Shalandus H.
    Papizan, James B.
    Kodali, Kiran
    Peng, Junmin
    Miller, Shondra M. Pruett
    Roussel, Martine F.
    Mullighan, Charles
    Fischer, Marcus
    Rankovic, Zoran
    JOURNAL OF MEDICINAL CHEMISTRY, 2021, 64 (11) : 7296 - 7311
  • [4] Discovery of highly potent dual GSPT1/BRD4 degraders with anti-AML activity
    Xu, Yue
    Yang, Hang
    Li, Yunxuan
    Qi, Yuying
    Zhao, Fangling
    Hong, Yun
    Cheng, Binbin
    Lu, Zebei
    Zhang, Jiaming
    Guo, Chunyi
    Fu, Jie
    Lin, Qinrong
    Chen, Chunhong
    Shi, Ningning
    Cai, Jianping
    Li, Ke
    Wang, Shuanghu
    Gao, Ruijuan
    Dai, Dapeng
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2025, 288
  • [5] The orally bioavailable GSPT1/2 degrader SJ6986 exhibits in vivo efficacy in acute lymphoblastic leukemia
    Chang, Yunchao
    Keramatnia, Fatemeh
    Ghate, Pankaj S.
    Nishiguchi, Gisele
    Gao, Qingsong
    Iacobucci, Ilaria
    Yang, Lei
    Chepyala, Divyabharathi
    Mishra, Ashutosh
    High, Anthony A.
    Goto, Hiroaki
    Akahane, Koshi
    Peng, Junmin
    Yang, Jun J.
    Fischer, Marcus
    Rankovic, Zoran
    Mullighan, Charles G.
    BLOOD, 2023, 142 (07) : 629 - 642
  • [6] Discovery of orally bioavailable SMARCA2/4 dual degraders for treatment of acute myeloid leukemia
    Abbineni, Chandrasekhar
    Khare, Leena
    Kuila, Bilash
    Khaji, Abdul Rawoof
    Mahadeo, Dhaytadak Bhagwan
    Dukare, Sandeep Vitthal
    Kumar, Bhagya M. S.
    Gore, Suraj T.
    Ahuja, Vijay Kamal
    Dhudashiya, Amit A.
    Raghavendra, N. R.
    Gowda, Nagesh
    Charamanna, K. B.
    Aithal, Kiran B.
    Samiulla, D. S.
    Mukherjee, Subhendu
    Antony, Thomas
    Giri, Sanjeev
    Chelur, Shekar
    Nellore, Kavitha
    Daginakatte, Girish
    Ramachandra, Murali
    Samajdar, Susanta
    CANCER RESEARCH, 2022, 82 (12)
  • [7] Potent anti-tumor activity of a selective and orally bioavailable reversible covalent CDK12 inhibitor
    Khare, Leena
    Poddutoori, Ramulu
    Mukherjee, Subhendu
    Samiulla, D. S.
    Devaraja, T. S.
    Marappan, Sivapriya
    Nayak, Shilpa
    Sivakumar, Sasirekha
    Kaza, Lakshmi
    Tgore, Suraj
    Dhudashiya, Amit
    Raghavendra, N. R.
    Gunnepalli, Bhargav
    Aravind, A. B.
    Amith, A.
    Charamanna, K. B.
    Antony, Thomas
    Nellore, Kavitha
    Daginakatte, Girish
    Chelur, Shekar
    Giri, Sanjeev
    Ramachandra, Murali
    Samajdar, Susanta
    MOLECULAR CANCER THERAPEUTICS, 2023, 22 (12)
  • [8] Discovery of highly potent, selective, and orally bioavailable IKZF2 degrader and its anti-tumor activity in syngeneic mouse models
    Park, Seulki
    Moon, Jeong Hee
    Lee, Gaseul
    Kim, Hyun Jin
    Kim, Jeong-Hoon
    Hwang, Jong Yeon
    CANCER RESEARCH, 2024, 84 (06)
  • [9] 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
  • [10] Discovery and preclinical evaluation of AMG 397, a potent, selective and orally bioavailable MCL1 inhibitor
    Caenepeel, Sean
    Karen, Rex
    Belmontes, Brian
    Verlinsky, Alla
    Tan, Hong
    Yang, Yajing
    Chen, Xiaoyue
    Li, Kexue
    Allen, Jennifer
    Wahlstrom, Jan
    Canon, Jude
    Coxon, Angela
    Hughes, Paul
    CANCER RESEARCH, 2020, 80 (16)
12345