Discovery of I-0436650, a potent and selective SHP2 allosteric inhibitor for the treatment of RAS driven solid tumors

被引:0
|
作者
Puca, F. [1 ]
Fodale, V. [1 ]
Randazzo, P. [2 ]
Fabbrini, D. [2 ]
Missineo, A. [1 ]
Bisbocci, M. [3 ]
Esposito, S. [4 ]
Nibbio, M. [4 ]
Amaudrut, J. [2 ]
Colaceci, F. [5 ]
Sasso, R. [5 ]
Scalabri, F. [1 ]
Loponte, S. [1 ]
Alli, C. [3 ]
Pucci, V. [4 ]
Montalbetti, C. [2 ]
Di Fabio, R. [2 ]
Petrocchi, A. [2 ]
Carugo, A. [1 ]
Toniatti, C. [1 ]
机构
[1] IRBM SpA, Biol, Rome, Italy
[2] IRBM SpA, Small Mol R&D, Rome, Italy
[3] IRBM SpA, Translat Res, Rome, Italy
[4] IRBM SpA, Expt Pharmacol, Rome, Italy
[5] IRBM SpA, Vivo Pharmacol, Rome, Italy
关键词
D O I
暂无
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
77
引用
收藏
页码:S26 / S26
页数:1
相关论文
共 50 条
  • [21] Selective inhibition of leukemia-associated SHP2E69K mutant by the allosteric SHP2 inhibitor SHP099
    Sun, X.
    Ren, Y.
    Gunawan, S.
    Teng, P.
    Chen, Z.
    Lawrence, H. R.
    Cai, J.
    Lawrence, N. J.
    Wu, J.
    LEUKEMIA, 2018, 32 (05) : 1246 - 1249
  • [22] Selective inhibition of leukemia-associated SHP2E69K mutant by the allosteric SHP2 inhibitor SHP099
    X Sun
    Y Ren
    S Gunawan
    P Teng
    Z Chen
    HR Lawrence
    J Cai
    NJ Lawrence
    J Wu
    Leukemia, 2018, 32 : 1246 - 1249
  • [23] Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors
    Taylor, Alexander M.
    Williams, Bret R.
    Giordanetto, Fabrizio
    Kelley, Elizabeth H.
    Lescarbeau, Andre
    Shortsleeves, Kelley
    Tang, Yong
    Walters, W. Patrick
    Arrazate, Alfonso
    Bowman, Christine
    Brophy, Erin
    Chan, Emily W.
    Deshmukh, Gauri
    Greisman, Jack B.
    Hunsaker, Thomas L.
    Kipp, D. Randal
    Lopez-Larrocha, Pablo Saenz
    Maddalo, Danilo
    Martin, Iain J.
    Maragakis, Paul
    Merchant, Mark
    Murcko, Mark
    Nisonoff, Hunter
    Nguyen, Vi
    Nguyen, Vy
    Orozco, Olivia
    Owen, Christopher
    Pierce, Levi
    Schmidt, Molly
    Shaw, David E.
    Smith, Sherri
    Therrien, Eric
    Tran, John C.
    Watters, Jim
    Waters, Nigel J.
    Wilbur, Jeremy
    Willmore, Lindsay
    JOURNAL OF MEDICINAL CHEMISTRY, 2023, 66 (19) : 13384 - 13399
  • [24] Discovery of a novel SHP2 allosteric inhibitor using virtual screening, FMO calculation, and molecular dynamic simulation
    Yuan, Zhen
    Zhang, Manzhan
    Chang, Longfeng
    Chen, Xingyu
    Ruan, Shanshan
    Shi, Shanshan
    Zhang, Yiqing
    Zhu, Lili
    Li, Honglin
    Li, Shiliang
    JOURNAL OF MOLECULAR MODELING, 2024, 30 (05)
  • [25] Discovery of IACS-13909, an allosteric SHP2 inhibitor that overcomes multiple mechanisms underlying osimertinib resistance
    Sun, Yuting
    Meyers, Brooke A.
    Johnson, Sarah B.
    Harris, Angela L.
    Czako, Barbara
    Cross, Jason B.
    Leonard, Paul G.
    Mseeh, Faika
    Di Francesco, Maria E.
    Parker, Connor A.
    Wu, Qi
    Bristow, Christopher A.
    Burke, Jason P.
    Carrillo, Caroline C.
    Carroll, Christopher L.
    Chang, Qing
    Feng, Ningping
    Gera, Sonal
    Guang, Gao
    Huang, Justin Kwang-Lay
    Jiang, Yongying
    Kang, Zhijun
    Kovacs, Jeffrey J.
    Ma, Xiaoyan
    Mandal, Pijus K.
    McAfoos, Timothy
    Mullinax, Robert A.
    Peoples, Michael D.
    Ramamoorthy, Vandhana
    Seth, Sahil
    Suzuki, Erika
    Williams, Christopher Conrad
    Yu, Simon S.
    Zuniga, Andy M.
    Draetta, Giulio F.
    Marszalek, Joseph R.
    Heffernan, Timothy P.
    Kohl, Nancy E.
    Jones, Philip
    MOLECULAR CANCER THERAPEUTICS, 2019, 18 (12)
  • [26] Off-target autophagy inhibition by SHP2 allosteric inhibitors contributes to their antitumor activity in RAS-driven cancers
    Miao, Yiming
    Bai, Yunpeng
    Miao, Jinmin
    Murray, Allison A.
    Lin, Jianping
    Dong, Jiajun
    Qu, Zihan
    Zhang, Ruo-Yu
    Nguyen, Quyen D.
    Wang, Shaomeng
    Yu, Jingmei
    Meke, Frederick Nguele
    Zhang, Zhong-Yin
    JOURNAL OF CLINICAL INVESTIGATION, 2024, 134 (15):
  • [27] Off-target autophagy inhibition by SHP2 allosteric inhibitors and therapeutic implications for aberrant RAS-driven cancers
    Miao, Yiming
    Bai, Yunpeng
    Miao, Jinmin
    Murray, Allison A.
    Lin, Jianping
    Dong, Jiajun
    Qu, Zihan
    Zhang, Ruo-Yu
    Nguyen, Quyen
    Wang, Shaomeng
    Zhang, Zhong-Yin
    CANCER RESEARCH, 2024, 84 (06)
  • [28] Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer
    Dong, Qing
    Dougan, Douglas R.
    Gong, Xianchang
    Halkowycz, Petro
    Jin, Bohan
    Kanouni, Toufike
    O'Connell, Shawn M.
    Scorah, Nicholas
    Shi, Lihong
    Wallace, Michael B.
    Zhou, Feng
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (05) : 1315 - 1319
  • [29] PCC0208023, a potent SHP2 allosteric inhibitor, imparts an antitumor effect against KRAS mutant colorectal cancer
    Chen, Xiao
    Zou, Fangxia
    Hu, Zhengping
    Du, Guangying
    Yu, Pengfei
    Wang, Wenyan
    Wang, Hongbo
    Ye, Liang
    Tian, Jingwei
    TOXICOLOGY AND APPLIED PHARMACOLOGY, 2020, 398
  • [30] Discovery of BPI460372, a potent and selective inhibitor of TEAD for the treatment of solid tumors harboring Hippo pathway aberrations
    Shen, Hongling
    Xu, Xiaofeng
    Rong, Hongfei
    Song, Xizhen
    Gao, Jinheng
    Chen, Jie
    Zhu, Di
    Zhao, Xiangdong
    Tong, Jun
    Zou, Zhengyao
    Liu, Xiaoyun
    Guo, Jin
    Xu, Yan
    Li, Yabin
    Liu, Xiangyong
    Chen, Hong
    Zhao, Jiayu
    Liu, Yanju
    Ju, Xuepeng
    Chen, Haibo
    Lan, Hong
    Ding, Lieming
    Wang, Jiabing
    CANCER RESEARCH, 2023, 83 (07)