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文献引用
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PI3K/mTOR Inhibitor
BEZ235（NVP-BEZ235）通过结合到这些酶的ATP结合裂隙，抑制PI3K和mTOR激酶活性。- Lijuan Chen, .et al. , Behav Neurol, 2023, May 9;2023:6991826 PMID: 37200987
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Tzeng SF, .et al. , FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Dominik Schulz, .et al. , Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
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ATM inhibitor
KU-55933 是一种 ATM 抑制剂，通过抑制细胞增殖并通过阻断在癌细胞中过度激活的 Akt 来诱导凋亡。- Ryo Sakasai, .et al. , Biochem Biophys Res Commun, 2023, Aug 6;668:42-48 PMID: 37244033
- Atsushi Saito, .et al. , Cell Rep, 2023, May 30;42(5):112479 PMID: 37178686
- Mariko Shikata, .et al. , Chem Res Toxicol, 2021, Dec 20;34(12):2512-2521 PMID: 34784199
- Masaya Igase, .et al. , Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- Hayakawa K, .et al. , Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
- Chwastek J, .et al. , Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
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ATM Inhibitor
KU-60019 是一种效力强大且特异性的 ATM 抑制剂，其 IC50 为 6.3 nM。- Erika Nakatsuka, .et al. , Transl Oncol, 2024, Sep 12:50:102119 PMID: 39270525
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Yuri Tozaki, .et al. , Cancers (Basel), 2023, Jan 25;15(3):735 PMID: 36765693
- Fu-Xing Gong, .et al. , Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
- Hegedus C, .et al. , Cancers (Basel), 2019, Dec 18;12(1) PMID: 31861350
- Masaya Igase, .et al. , Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- CHENGHUA LOU, .et al. , Oncol Lett, 2016, Jul; 12(1): 295-300 PMID: 27347141
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PI3K inhibitor
Wortmannin 是一种强效、选择性、细胞渗透性和不可逆的磷脂酰肌醇3激酶（PI 3-kinase）抑制剂（IC50 = 2 - 4 nM），同时也强效抑制polo样激酶1（PLK1）（IC50 = 5.8 nM）。- Weili Chen, .et al. , Communications Biology, 2024, 7:488
- Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938
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mTOR inhibitor
Torin 2 是一种强效且选择性的 mTOR 抑制剂（IC50 = 2.1 nM）。在细胞内对 mTOR 比 PI3K 有800倍的选择性（mTOR 和 PI3K 的细胞 EC50 值分别为 0.25 nM 和 200 nM）。- Diane Yang, .et al. , Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
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ATM/ATR inhibitor
VE-821 是一种强效且选择性的 蛋白激酶 ATR 抑制剂。- Atsushi Saito, .et al. , Cell Rep, 2023, May 30;42(5):112479 PMID: 37178686
- Mitsuru Sasaki-Honda, .et al. , Hum Mol Genet, 2018, Dec 1; 27(23): 4024-4035 PMID: 30107443
- Kim J, .et al. , Mol Cell, 2018, Jan 4;69(1):36-47.e7 PMID: 29249653
- Antonio Postigo, .et al. , Cell Rep, 2017, May 2; 19(5): 1022-1032 PMID: 28467896
- Nnennaya Kanu, .et al. , Genome Biol, 2016, 17: 185 PMID: 27634334
- Carolyn Botting, .et al. , Virol J, 2016, 13: 15 PMID: 26817608
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ATR inhibitor
ETP-46464 是一种强效且选择性的 ATR 抑制剂，其 IC50 为 25 nM。- Fu-Xing Gong, .et al. , Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
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ATR inhibitor
AZD6738 是一种强效的 ATR激酶 抑制剂，其对分离酶的 IC50 为1 nM，对细胞中 ATR激酶 依赖的 CHK1磷酸化 的 IC50 为74 nM。- Erika Nakatsuka, .et al. , Transl Oncol, 2024, Sep 12:50:102119 PMID: 39270525
- Zhiyan Silvia Liu, .et al. , Cancer Res, 2024, Feb 15;84(4):577-597 PMID: 37967363
- Yang Lim, .et al. , Science, 2023, Sep 22;381(6664) PMID: 37590370
- Brian F Kiesel, .et al. , Cancer Chemother Pharmacol, 2022, Feb;89(2):231-242 PMID: 35066692
- Albert Job, .et al. , Sci Rep, 2020, Nov 3;10(1):18924 PMID: 33144657
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ATM inhibitor
AZD0156 是一种强效且选择性的 ATM激酶 抑制剂，具有潜在的化疗/放疗增敏和抗肿瘤活性。- Yi-Ru Pan, .et al. , Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
