Discovery of a novel SOS1 inhibitor, AIG01012, targeting pan-KRAS mutant cancers

被引:0
|
作者
Kim, Jihye
Park, Sejeong
Kim, Sunkyu
Lee, Sanghoon
Yoo, Kiwoong
Lee, Ho-Jeong
Kang, Jaewoo
Lee, Kwang-Ok
机构
关键词
D O I
10.1158/1538-7445.AM2024-3324
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
3324
引用
收藏
页数:2
相关论文
共 30 条
  • [21] Effective targeting of KRAS-driven tumors by the first-in-class, orally bioavailable SOS1::KRAS inhibitor BI-3406
    Hofmann, Marco H.
    Gmachl, Michael
    Ramharter, Jurgen
    Savarese, Fabio
    Sanderson, Michael P.
    Gerlach, Daniel
    Trapani, Francesca
    Botesteanu, Dana-Adriana
    Kessler, Dirk
    Ettmayer, Peter
    Arnhof, Heribert
    Gerstberger, Thomas
    Schnitzer, Renate
    Kofink, Christiane
    Stadtmueller, Heinz
    Wunberg, Tobias
    O'Connell, Jonathan C.
    Mendes, Rachel L.
    Richard, David
    Saldanha, Adrian S.
    Moll, Juergen
    Pearson, Mark
    McConnell, Darryl B.
    Kraut, Norbert
    MOLECULAR CANCER THERAPEUTICS, 2019, 18 (12)
  • [22] Discovery of Novel Coumarin-quinolinium Derivatives as Pan-KRAS Translation Inhibitors by Targeting 5′-UTR RNA G-Quadruplexes
    Li, Mao-Lin
    Dai, Le-Tian
    Gao, Zhuo-Yu
    Yan, Jia-Tong
    Xu, Shu-Min
    Tan, Jia-Heng
    Huang, Zhi-Shu
    Chen, Shuo-Bin
    Chen, Xiu-Cai
    JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (03) : 1961 - 1981
  • [23] Discovery and Characterization of HH100937, a potent and selective SOS1 inhibitor demonstrates synergistic efficacy in combination with KRAS/MAPK therapies
    Xie, Qing
    Li, Dongsheng
    Jiang, Shujuan
    Zhu, Jie
    Yu, Songda
    Yang, Maozhi
    Cai, Yalei
    Liu, Lei
    Yu, Bing
    Tu, Wangyang
    Zhang, Yixiang
    Li, Leping
    CANCER RESEARCH, 2024, 84 (07)
  • [24] Discovery of novel diaryl urea-oxindole hybrids as BRAF kinase inhibitors targeting BRAF and KRAS mutant cancers
    Ghannam, Iman A. Y.
    El Kerdawy, Ahmed M.
    Mounier, Marwa M.
    Abo-elfadl, Mahmoud T.
    Abdel-Mohsen, Heba T.
    BIOORGANIC CHEMISTRY, 2024, 153
  • [25] HM99462, a novel SOS1 inhibitor, induces tumor regression and synergistic effect with KRAS or EGFR targeted therapy in NSCLC
    Park, W.
    Jung, S. H.
    Choi, J.
    Byun, J.
    Lim, S.
    Jeon, S.
    Lee, Y.
    Ahn, Y. G.
    EUROPEAN JOURNAL OF CANCER, 2024, 211 : S36 - S36
  • [26] Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor
    Huestis, Malcolm P.
    Dela Cruz, Darlene
    DiPasquale, Antonio G.
    Durk, Matthew R.
    Eigenbrot, Charles
    Gibbons, Paul
    Gobbi, Alberto
    Hunsaker, Thomas L.
    La, Hank
    Leung, Dennis H.
    Liu, Wendy
    Malek, Shiva
    Merchant, Mark
    Moffat, John G.
    Muli, Christine S.
    Orr, Christine J.
    Parr, Brendan T.
    Shanahan, Frances
    Sneeringer, Christopher J.
    Wang, Weiru
    Yen, Ivana
    Yin, Jianping
    Siu, Michael
    Rudolph, Joachim
    JOURNAL OF MEDICINAL CHEMISTRY, 2021, 64 (07) : 3940 - 3955
  • [27] Design and Discovery of MRTX0902, a Potent, Selective, Brain- Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction
    Ketcham, John M.
    Haling, Jacob
    Khare, Shilpi
    Bowcut, Vickie
    Briere, David M.
    Burns, Aaron C.
    Gunn, Robin J.
    Ivetac, Anthony
    Kuehler, Jon
    Kulyk, Svitlana
    Laguer, Jade
    Lawson, J. David
    Moya, Krystal
    Nguyen, Natalie
    Rahbaek, Lisa
    Saechao, Barbara
    Smith, Christopher R.
    Sudhakar, Niranjan
    Thomas, Nicole C.
    Vegar, Laura
    Vanderpool, Darin
    Wang, Xiaolun
    Yan, Larry
    Olson, Peter
    Christensen, James G.
    Marx, Matthew A.
    JOURNAL OF MEDICINAL CHEMISTRY, 2022, : 9678 - 9690
  • [28] Evaluation of phosphoprotein- and transcript-based pharmacodynamic biomarkers in pre-linical studies of the novel SOS1::KRAS inhibitor BI-3406
    Gerlach, Daniel
    Savarese, Fabio
    Hofmann, Marco H.
    Trapani, Francesca
    Gmachl, Michael
    Botesteanu, Dana-Adriana
    Ramharter, Juergen
    Arnhof, Heribert
    Schweifer, Norbert
    McConnell, Darryl B.
    Kraut, Norbert
    MOLECULAR CANCER THERAPEUTICS, 2019, 18 (12)
  • [29] Effective preclinical treatment of KRAS mutant lung cancers with a combination of MLN0128, an investigational novel mTORC1/2 inhibitor, and a selective MEK inhibitor
    Fabrey, Robyn
    Atienza, Joy
    Briere, David
    Brake, Rachael
    Vincent, Patrick W.
    MOLECULAR CANCER THERAPEUTICS, 2013, 12 (11)
  • [30] Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers
    Lelais, Gerald
    Epple, Robert
    Marsilje, Thomas H.
    Long, Yun O.
    McNeill, Matthew
    Chen, Bei
    Lu, Wenshuo
    Anumolu, Jaganmohan
    Badiger, Sangamesh
    Bursulaya, Badry
    DiDonato, Michael
    Fong, Rina
    Juarez, Jose
    Li, Jie
    Manuia, Mari
    Mason, Daniel E.
    Gordon, Perry
    Groessl, Todd
    Johnson, Kevin
    Jia, Yong
    Kasibhatla, Shailaja
    Li, Chun
    Isbell, John
    Spraggon, Glen
    Bender, Steven
    Michellys, Pierre-Yves
    JOURNAL OF MEDICINAL CHEMISTRY, 2016, 59 (14) : 6671 - 6689