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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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Protein Synthesis Inhibitor
环己酰胺（又称为放线菌酮）被用作一种选择性抗生素。它通过与80S核糖体结合，抑制腐生真菌真核生物的蛋白质合成（依赖DNA的RNA），而对皮肤癣菌和系统性真菌无效。- Tianfeng Huang, .et al. , Mol Neurobiol, 2024, Sep 13 PMID: 39271624
- Han Xiao, .et al. , JPA, 2023, Apr 19
- Shuanghui Lu, .et al. , Chem Biol Interact, 2022, Dec 1;368:110219 PMID: 36243147
- Ke Chen, .et al. , Cancer Commun (Lond), 2021, Apr; 41(4): 316-332 PMID: 33591636
- Zhiyuan Qin, .et al. , Cancers (Basel), 2021, Feb 4;13(4):618 PMID: 33557163
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
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topoisomerase II inhibitor
Adriamycin 是一种蒽环类抗生素，它通过插入 DNA 来发挥作用，而最严重的副作用是可能危及生命的心脏损伤。它常用于治疗多种癌症，包括血液恶性肿瘤、多种类型的癌症和软组织肉瘤。- Sanaz Naghibi, .et al. , Biosensors (Basel), 2022, May 29;12(6):373 PMID: 35735521
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DNA and RNA synthesis inhibitor
氟尿嘧啶（Adrucil）是一种自杀抑制剂，其作用机制是通过不可逆地抑制胸苷酸合成酶来发挥作用。- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Adi Jacob Berger, .et al. , Nat Cancer, 2021, 2, 1055-1070 PMID: 35121883
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PARP inhibitor
AG-014699（Rucaparib）是一种PARP抑制剂，它抑制多聚（ADP-核糖）聚合酶（PARP），这是DNA修复中的关键酶。- Ali Divan, .et al. , Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Tahira Baloch, .et al. , BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
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PARP1 inhibitor
AG14361 是一种强效的 PARP 抑制剂，在 MMR（错配修复） -完好/缺陷细胞中增强了 TMZ 的细胞毒性。- Vimal Pandey, .et al. , Scientific Reports, 2019, 9, Article number: 5012 PMID: 30899038
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Topoisomerase inhibitor
Amonafide 是一种用于治疗肿瘤性疾病的 DNA 插入剂 和 拓扑异构酶 II 抑制剂，是抗肿瘤药物之一。- Veronica Rendo, .et al. , Nat Commun, 2020, 11: 1308 PMID: 32161261
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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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HDAC inhibitor
Belinostat (PXD101) 是一种 HDAC 抑制剂，在 HeLa 细胞提取物中抑制 HDAC 活性，其 IC50 为 27 nM。- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
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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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Telomerase Inhibitor
BIBR 1532 是一种选择性的端粒酶抑制剂（IC50 值分别为 93, > 100000 和 > 100000 nM，针对人类端粒酶、人类 RNA 聚合酶 I 和人类 RNA 聚合酶 II + III）。- Hosoi T, .et al. , Neurosci Lett, 2016, Aug 26;629:241-244 PMID: 27443785
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DNA/RNA Synthesis inhibitor
硫酸亚叶霉素是从链霉菌Streptomyces verticillus分离出的基本糖肽类抗肿瘤抗生素硫酸盐的混合物。- Arina Morozan, .et al. , Sci Rep, 2023, Nov 23;13(1):20577 PMID: 37996447
- Mai Kanemaru, .et al. , J Dermatol Sci, 2018, Jan;93(1):41-49 PMID: 30655107
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PARP1 inhibitor
BSI-201 是一种强效的 PARP-1 抑制剂，并已显示能够穿越 血脑屏障。- Jianwei Dou, .et al. , J Sep Sci, 2020, Dec 4 PMID: 33275824
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Topoisomerase I inhibitor
Camptothecin 是一种具有细胞毒性的喹啉生物碱，它抑制 DNA 酶 拓扑异构酶 I（topo I）。- Kengo Takeda, .et al. , Int J Mol Sci, 2024, Mar 26;25(7):3693 PMID: 38612503
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Topoisomerase inhibitor
Cerubidine (Daunorubicin HCl, Rubidomycin HCl) interacts with DNA by intercalation and inhibition of macromolecular biosynthesis. This inhibits the progression of the enzyme topoisomerase II, which relaxes supercoils in DNA for transcription. It stabilizes the topoisomerase II complex after it has broken the DNA chain for replication, preventing the DNA double helix from being resealed and thereby stopping the process of replication. -
DNA/RNA Synthesis inhibitor
Cidofovir (Vistide) 是一种抗病毒药物，用于治疗巨细胞病毒（CMV）感染（例如：视网膜炎）。- Adhikary A, .et al. , J Phys Chem B, 2015, Sep 3;119(35):11496-505 PMID: 26237072
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DNA/RNA Synthesis inhibitor
Clofarabine 是一种第二代 嘌呤核苷类似物，具有 抗肿瘤活性。- Xie J, .et al. , Pediatr Blood Cancer, 2019, Dec 25:e28133 PMID: 31876116
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Telomerase inhibitor
Costunolide 是一种抑制人类端粒酶活性的抑制剂（在 MCF-7 乳腺癌细胞中的 IC50 为 65 μM）。它被描述为具有抗氧化、抗结核、抗炎和抗病毒作用，并具有细胞毒性活性。 -
DNA/RNA Synthesis inhibitor
达托霉素是一种脂肽类抗生素，用于治疗由革兰氏阳性菌引起的某些感染。- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
- Shigeru Fujimura, .et al. , J Infect Chemother., 2015, Oct;21(10):756-9 PMID: 26162777
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HDAC inhibitor
Droxinostat 是一种选择性的 HDAC3、HDAC6 和 HDAC8 抑制剂，对 HDAC6 和 HDAC8 的抑制作用相当，其半抑制浓度（IC50）分别为 2.47 和 1.46 微摩尔/升。 -
Topoisomerase II inhibitor
Epirubicin 是一种可渗透细胞的蒽环类抗肿瘤抗生素。它是多柔比星的立体异构体（4'epi-异构体），显示出较低的心脏毒性。它用于抑制拓扑异构酶II和DNA解旋酶活性。 -
DNA/RNA Synthesis inhibitor
奥沙利铂是一种基于铂的抗肿瘤药物，用于癌症化疗。体内研究表明，奥沙利铂通过其（非靶向的）细胞毒性效应对结肠癌具有抗肿瘤活性。- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
- Mohamed Elbadawy, .et al. , Biomed Pharmacother, 2021, Oct;142:112043 PMID: 34411919
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Shimokawa M, .et al. , Nature, 2017, May 11;545(7653):187-192 PMID: 28355176
- Eri Takiguchi, .et al. , Exp Ther Med, 2017, Nov; 14(5): 4293-4299 PMID: 29067110
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Topoisomerase II inhibitor
依托泊苷与DNA和拓扑异构酶II（帮助DNA解旋）形成三元复合物，阻止DNA链的重新连接，并因此导致DNA链断裂。因此，这会导致DNA合成出错，并促进癌细胞的凋亡。- Bageshri Naimish Nanavati, .et al. , Curr Biol, 2024, Sep 9;34(17):4081-4090 PMID: 39153481
- Wan J Gan, .et al. , Cytoskeleton (Hoboken), 2024, Jul 10 PMID: 38984538
- Wan J. Gan, .et al. , bioRxiv, 2024, March 10
- Zoya Mann, .et al. , Mol Biol Cell, 2024, Jan 1; 35(1) PMID: 37903230
- Bageshri Naimish Nanavati, .et al. , bioRxiv, 2023, Feb 23 PMID: 36865131
- Sibei Wang, .et al. , Molecules, 2023, Jan 19;28(3):1016 PMID: 36770683
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Chen JC, .et al. , Biomolecules, 2019, Sep 9;9(9) PMID: 31505885
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
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SIRT1 inhibitor
EX 527 是一种强效且选择性的 SIRT1 类 III 组蛋白去乙酰化酶 抑制剂，在无细胞试验中的 IC50 为 38 nM。- Yue He, .et al. , FASEB J, 2024, Oct 15;38(19):e70095 PMID: 39373984
- Qiang Chen, .et al. , J Bioenerg Biomembr, 2022, Feb;55(1):33-42 PMID: 36525212
- Flavien Bizot, .et al. , Mol Ther Nucleic Acids, 2022, Nov 21;30:606-620 PMID: 36514350
- Takeshi Nakamura, .et al. , Shimane Journal of Medical Science, 2022, 38 (2), 59-66
- Bugga Paramesha, .et al. , Antioxidants (Basel), 2021, Feb 24;10(3):338 PMID: 33668369
- Wenhui Yao, .et al. , J Cell Physiol, 2020, 07 August
- Guang Bai, .et al. , Epigenetics of Chronic Pain, 2019, Pages 1-48
- Yoshikawa A, .et al. , J Neurochem, 2015, Feb;132(3):342-53 PMID: 25351847
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DNA/RNA Synthesis inhibitor
Tegafur 是一种用于治疗癌症的化疗 5-FU 前药。它是 tegafur-uracil 的一个组成部分。- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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DNA gyrase/topoisomerase IV inhibitor
加替沙星是一种氟喹诺酮类抗生素，它抑制细菌DNA回旋酶（IC50 = 0.109 ng/ml）和拓扑异构酶IV（IC50 = 13.8 ng/ml）。 -
DNA/RNA Synthesis inhibitor
Gemcitabine（Gemzar）是一种较新的化疗药物，其作用机制是在癌细胞的DNA复制过程中替换核酸的一种构建模块，从而阻止肿瘤生长。- Chiao-Ping Chen, .et al. , Biomed Pharmacother, 2023, Oct:166:115389 PMID: 37659202
- G. R. Iglesias, .et al. , Polymers, 2018, 10(3), 269
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Topoisomerase inhibitor
伊达比星是一种蒽环类抗生素，它是一种抗白血病药物，具有比多柔比星更高的DNA结合能力和更强的细胞毒性。- Wei Y, .et al. , Mol Cell, 2017, Jun 1;66(5):581-596.e6 PMID: 28552615
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PARP Inhibitor
3-氨基苯甲酰胺是一种新型的 PARP 抑制剂，已知通过抑制 DNA 损伤的修复，能够在体外使细胞对辐射敏感化。- Kamada Y, .et al. , Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
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Topoisomerase I inhibitor
伊立替康通过抑制拓扑异构酶1，阻止DNA解旋。- Gils Jose, .et al. , Cancers (Basel), 2020, Oct 31;12(11):E3211 PMID: 33142721
- T Kannathasan, .et al. , Cancers (Basel), 2020, May; 12(5): 1231 PMID: 32422901
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Topoisomerase inhibitor
伊立替康（CPT 11），一种来源于喜树碱家族的化合物，是拓扑异构酶 1的抑制剂，参与细胞 DNA 的复制和转录。- Jingyao Gan, .et al. , Int J Pharm, 2025, Jan 25:669:125000 PMID: 39608586
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HDAC inhibitor
ITF2357（Givinostat）是一种 HDACs 抑制剂，具有潜在的 抗炎、抗血管生成 和 抗肿瘤 活性。- Flavien Bizot, .et al. , Mol Ther Nucleic Acids, 2022, Nov 21;30:606-620 PMID: 36514350
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HDAC inhibitor
JNJ-26481585（Quisinostat）是一种全面的HDAC抑制剂，对HDAC1具有显著的效力（IC(50)，0.16 nmol/L）。- Minoru Ueda, .et al. , Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096
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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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HDAC Inhibitor
LAQ824（NVP-LAQ824）是一种强效的新型组蛋白去乙酰化酶抑制剂，对多发性骨髓瘤具有显著的活性。- De-Run Chen, .et al. , Appl Mater Today, 2022, 26: 101363
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HDAC Inhibitor
LBH589 是一种羟胺酸，作为非选择性 HDAC 抑制剂，其对 HDAC1 的 IC50 为 0.23 nM。- Jalila Chagraoui, .et al. , Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Gils Jose, .et al. , Cancers (Basel), 2020, Oct 31;12(11):E3211 PMID: 33142721
- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14
- Justin Kale, .et al. , EMBO Rep, 2018, Sep; 19(9): e45235 PMID: 29987135
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HDAC Inhibitor
MC1568 是 HDAC 抑制剂的一种，它通过改变细胞周期中大多数处于 G1 阶段的各种重要基因的遗传表达，抑制组蛋白去乙酰化酶 II 类，从而导致乳腺癌细胞通过凋亡死亡。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Vivek Bora, .et al. , Can J Physiol Pharmacol, 2021, 6 October
- Minoru Ueda, .et al. , Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096
- S Ishikawa, .et al. , Int J Cancer., 2014, 135(11): 2528-2536 PMID: 24346863
- Usui T, .et al. , Hypertension., 2014, Feb;63(2):397-403 PMID: 24166750
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HDAC Inhibitor
MGCD0103（Mocetinostat）是一种苯甲酰胺类组蛋白去乙酰化酶抑制剂，主要通过抑制组蛋白去乙酰化酶1（HDAC1），同时也能抑制HDAC2、HDAC3和HDAC11。- Mari Ishigami-Yuasa, .et al. , Biol Pharm Bull, 2019, 42, 448-452 PMID: 30828077
- Guang Bai, .et al. , Epigenetics of Chronic Pain, 2019, Pages 1-48
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Topoisomerase inhibitor
Moxifloxacin 是一种喹诺酮/氟喹诺酮类抗生素。- Hiroshi Arakawa, .et al. , Biopharm Drug Dispos, 2016, Jan;37(1):39-45 PMID: 26590007
- Arisa Higa, .et al. , Fundam. Toxicol. Sci, 2016, 3(2): 47-53
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HDAC inhibitor
MS-275（Entinostat）是一种强效的HDAC抑制剂，其IC50分别为HDAC1的0.3uM和HDAC3的8uM。- Wenguang Liu, .et al. , Biochem Biophys Res Commun, 2024, Dec 20:739:150970 PMID: 39550862
- Vivek Bora, .et al. , Can J Physiol Pharmacol, 2021, 6 October
- Taito Kashio, .et al. , Tissue Barriers, 2021, May 6;1911195 PMID: 33955828
- Ting-Yu Chang, .et al. , Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- Arshdeep Singh, .et al. , Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Minoru Ueda, .et al. , Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096
- Parthenolide（(-)-Parthenolide）是一种天然存在于小白菊（Tanacetum parthenium）中的倍半萜内酯。
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HDAC Inhibitor
PCI-24781 是一种广谱的苯基羟胺酸 HDAC 抑制剂。- Kazuya Tsumagari, .et al. , Biochem Biophys Res Commun, 2021, Jul 23;563:60-65 PMID: 34062387
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PI3K Inhibitor
PI-103 是一种强效的、细胞渗透性的、ATP竞争性抑制剂，针对磷脂酰肌醇3激酶（PI3K）家族成员具有选择性，特别是对 DNA-PK、PI3K (p110α) 和 mTOR。- Diane Yang, .et al. , Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
