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PARP inhibitor
ABT-888(Veliparib) 是一种潜在的抗癌药物,作为 PARP 抑制剂 发挥作用。- Subhajit Chatterjee, .et al. , Cell Signal, 2021, Apr;80:109902 PMID: 33373686
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PARP inhibitor
Olaparib (AZD2281) 是一种抑制剂,针对的是参与 DNA 修复的酶——聚ADP核糖聚合酶(PARP)。- Yuki Yoshino, .et al. , Biochem Biophys Res Commun, 2025, Jan:742:151153 PMID: 39672008
- Saptarshi Sinha, .et al. , Med Oncol, 2024, Jan 6;41(2):49 PMID: 38184505
- Erika Nakatsuka, .et al. , Transl Oncol, 2024, Sep 12:50:102119 PMID: 39270525
- Callum G Jones, .et al. , Cancers (Basel), 2024, Feb 21;16(5):863 PMID: 38473223
- Aurelie Vanderlinden, .et al. , Br J Cancer, 2023, Nov;129(11):1829-1840 PMID: 37777579
- Saptarshi Sinha, .et al. , Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. , J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. , Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. , Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. , Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. , Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. , Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. , Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. , DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. , Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. , Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. , Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. , Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. , J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. , Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. , J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. , SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. , Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. , Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. , Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. , Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. , Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. , Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. , FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. , Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. , BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. , Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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PARP inhibitor
MK-4827 是一种新型的、高效的、口服生物利用度高的 PARP-1 和 PARP-2 抑制剂。- Joseph M Gozgit, .et al. , Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Ann-Katrin Hopp, .et al. , Molecular cell, 2021, Jan 21; 81(2): 340–354 PMID: 33450210
- Bian C, .et al. , Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- Tahira Baloch, .et al. , BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
- Khalid Hilmi, .et al. , Sci Adv, 2017, May; 3(5): e1601898 PMID: 28560323
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PARP inhibitor
BMN-673 是一种口服生物利用度的抑制剂,针对核酶多聚(ADP-核糖)聚合酶(PARP)具有潜在的抗肿瘤活性。- Subhajit Chatterjee, .et al. , J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Charles-André Philip, .et al. , BMC Cancer, 2017, 17: 638 PMID: 28886696
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PARP inhibitor
PJ 34 盐酸盐是一种强效的聚(ADP-核糖)聚合酶(PARP)抑制剂(EC50 = 20 nM)。- Wigle TJ, .et al. , SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Alvin Z.Lu, .et al. , Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
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PARP Inhibitor
BMN-673 (8R,9S) 是 BMN-673 的 (8R,9S) 对映体。BMN 673 是一种新型的 PARP 抑制剂,其 IC50 为 0.58 nM。 -
PARP inhibitor
PJ34 是一种新型的高效特异性 PARP-1/2 抑制剂,其 EC50 为 20 nM。- Tim J Wigle, .et al. , Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
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TNKS2 inhibitor
NVP-TNKS656 是一种高效、选择性强且可口服的 TNKS2 抑制剂,其 IC50 为 6 nM;对 PARP1 和 PARP2 的选择性超过 300 倍。 -
PARP1/PARP2 inhibitor
Niraparib tosylate (MK-4827 tosylate) 是一种高效且可口服吸收的 PARP1 和 PARP2 抑制剂,其 IC50 分别为 3.8 nM 和 2.1 nM。- Laurie B Schenkel, .et al. , Cell Chem Biol, 2021, Mar 2;S2451-9456(21)00095-7 PMID: 33705687
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PARP inhibitor
Rucaparib Camsylate 是一种 PARP 抑制剂,其对 PARP1 的 Ki 值为 1.4 nM,并且还显示出对其他八个 PARP 域的结合亲和力。 -
PARP1 and PARP2 inhibitor
Niraparib hydrochloride (MK-4827 hydrochloride) 是一种高效且可口服吸收的 PARP1 和 PARP2 抑制剂,其 IC50 分别为 3.8 nM 和 2.1 nM。 -
PARP inhibitor
Veliparib dihydrochloride 是一种强效的 PARP 抑制剂,分别以 Kis 值 5.2 和 2.9 nM 抑制 PARP1 和 PARP2。 -
PARP1/PARP2 inhibitor
E7449 是一种强效的 PARP1 和 PARP2 抑制剂,同时也能抑制 TNKS1 和 TNKS2,其半抑制浓度(IC50)分别为 PARP1 2.0 nM、PARP2 1.0 nM、TNKS1 和 TNKS2 约50 nM,使用的底物为 32P-NAD+。 -
PARP1 inhibitor
Niraparib R-enantiomer (MK-4827 R-enantiomer) 是一种优秀的 PARP1 抑制剂,其 IC50 为 2.4 nM。