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PARP 抑制剂
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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Bcl-2 抑制剂
ABT-737 是一种广谱 Bcl-2 抑制剂。IC50 值从 192 nM（前B细胞系 Hal-01）到小于 10 μM（Nalm-6、K562 和 HL-60）。- Jung Mo Lee, .et al. , Yonsei Med J, 2022, Jan;63(1):16-25 PMID: 34913280
- AidaVarela-Moreira, .et al. , Int J Pharm, 2022, Apr 25;618:121638 PMID: 35257802
- Daniel F R Boehmer, .et al. , Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Shivani Arora, .et al. , Med, 2021, 2,1-13
- Ying Ji, .et al. , Nat Commun, 2020, Aug 25;11(1):4249 PMID: 32843618
- Birgit Ritschka, .et al. , Genes Dev, 2020, Apr 1;34(7-8):489-494 PMID: 32139422
- Hiroki Akiyama, .et al. , Cancers, 2020, 12 (2) PMID: 32050632
- Hsu CC, .et al. , Arch Oral Biol, 2020, Mar;111:104653 PMID: 31935534
- Gupta VK, .et al. , Apoptosis, 2020, Feb;25(1-2):135-150 PMID: 31867678
- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Jose Mario Gonzalez-Meljem, .et al. , Nat Commun, 2017, 8: 1819 PMID: 29180744
- Zhang C, .et al. , J Biol Chem, 2017, Sep 8;292(36):15105-15120 PMID: 28673964
- Eun Young Kim, .et al. , Neoplasia, 2017, Apr; 19(4): 354-363 PMID: 28319809
- Masayoshi Toge, .et al. , Int J Oncol., 2015, Apr;46(4):1844-8 PMID: 25647738
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Topoisomerase II 抑制剂
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
- 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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HMG-CoA reductase 抑制剂
Pitavastatin Calcium 是一种与酶 HMGCR (HMG-CoA reductase) 竞争的抑制剂，能够减少 LDL cholesterol 的合成。- Weizhen Chen, .et al. , Biomaterials, 2021, 280:121260 PMID: 34823885
- Karis Tutuska, .et al. , Cell Death Dis, 2020, Apr; 11(4): 274 PMID: 32332697
- D Jarmuzek, .et al. , J Photochem Photobiol A Chem, 2019, November
- Marwan Ibrahim Abdullah, .et al. , Sci Rep, 2017, 7: 8090 PMID: 28808351
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PLA 抑制剂
Polydatin 通过改善微循环和抑制血小板聚集，保护脑细胞免受缺血性损伤。此外，polydatin 抑制内皮细胞在脂多糖刺激下的 ICAM-1 表达；它还减轻了白细胞与内皮细胞之间的粘附。- Darshika Pathiraja, .et al. , Food Chem, 2023, May 1;407:135145 PMID: 36521391
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mTOR 抑制剂
PP242 是一种强效且选择性的 mTOR 抑制剂，能够抑制 mTORC1 和 mTORC2。- Nobuyuki Kondo, .et al. , JCI Insight, 2023, Dec 22;8(24):e173688 PMID: 37917191
- Hiroshi Fukamachi, .et al. , J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Fuse MJ, .et al. , Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
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MAO-B 抑制剂
Quercetin 抑制多种酶系统，包括酪氨酸蛋白激酶、磷脂酶A2、磷酸二酯酶、线粒体ATP酶、PI 3-激酶和蛋白激酶C。 -
HDAC 抑制剂
Valproic acid sodium salt (Sodium Valproate) 是一种 HDAC 抑制剂，其 IC50 在 0.5 至 2 mM 范围内，同时抑制 HDAC1（IC50，400 μM），并诱导 HDAC2 的蛋白酶体降解。 -
RTK 抑制剂
舒尼替尼是一种口服的小分子多靶点受体酪氨酸激酶（RTK）抑制剂，用于治疗肾细胞癌（RCC）和对伊马替尼耐药的胃肠间质瘤（GIST）。- Sophie J. Bakri, .et al. , PLoS One, 2024, 19(6): e0304782 PMID: 38833447
- Chern Ein Oon, .et al. , World J Gastrointest Oncol, 2023, May 15;15(5):810-827 PMID: 37275453
- Rachel K Toth, .et al. , Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Thibaut Fourniols, .et al. , Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
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MEK 抑制剂
U0126-EtOH 是一种同时抑制 MEK1 和 MEK2 的抑制剂，其半抑制浓度（IC50）分别为 72 nM 和 58 nM。- Ji Wang, .et al. , Acta Pharmacol Sin, 2024, Nov 20 PMID: 39567750
- Hanna Galganska, .et al. , Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Choe YJ, .et al. , Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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HDAC 抑制剂
Vorinostat 是一种 HDACs 抑制剂，它抑制去乙酰化作用，导致 高乙酰化组蛋白 和转录因子的积累。- Masahiro Yamada, .et al. , Int J Hematol, 2024, Sep;120(3):325-336 PMID: 38954186
- Amy E Neely, .et al. , Commun Biol, 2023, Jun 23;6(1):664 PMID: 37353594
- Ting-Yu Chang, .et al. , Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- David Diaz-Carballo, .et al. , Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Arshdeep Singh, .et al. , Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14
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JAK1/2 抑制剂
INCB018424 是一种强效且选择性的 Janus-associated kinase (JAK) 1 和 2 抑制剂，其半抑制浓度（IC50）分别为 JAK1 2.7 nM、JAK2 4.5 nM 和 JAK3 332 nM。- Meenu Kesarwani, .et al. , Blood Adv, 2024, Jun 11;8(11):2765-2776 PMID: 38531054
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Rasmus Siersbek, .et al. , Cancer cell, 2020, Jul 6;S1535-6108(20)30311-1 PMID: 32679107
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Kagoya Y, .et al. , Blood., 2014, Nov 6;124(19):2996-3006 PMID: 25217696
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PDGFR/FLT3 抑制剂
Crenolanib (CP-868596) 是一种口服生物利用度高的选择性小分子抑制剂，针对 PDGFR 酪氨酸激酶 进行抑制，能在皮克摩尔浓度下同时抑制 PDGFRA 和 PDGFRB。- N Naganna, .et al. , EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
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Autophagy/PI3K 抑制剂
3-甲基腺嘌呤是III类磷脂酰肌醇3激酶（PI 3-激酶）的抑制剂。- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
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JAK1/2 抑制剂
Ruxolitinib sulfate（INCB018424 sulfate）是首个进入临床的强效、选择性 JAK1/2 抑制剂，其 IC50 值分别为 3.3 nM/2.8 nM，并且对 JAK1/2 比 JAK3 的选择性高出 130 倍以上。 -
JAK 抑制剂
磷酸鲁索替尼是鲁索替尼的磷酸盐形式，这是一种口服生物可用的Janus相关激酶（JAK）抑制剂，具有潜在的抗肿瘤和免疫调节活性。 -
Mitochondrial respiratory chain 抑制剂
Sulfosuccinimidyl oleate（Sulfo-N-succinimidyl oleate）是一种长链脂肪酸，能够抑制脂肪酸进入细胞。Sulfosuccinimidyl oleate 是一种强效且不可逆的线粒体呼吸链抑制剂。 -
HMG-CoA reductase 抑制剂
Pitavastatin Lactone 是一种 HMG-CoA reductase inhibitor。 -
DRP1 抑制剂
Mdivi-1 是一种选择性的、细胞渗透性的线粒体分裂抑制剂，针对线粒体分裂 DRP1（与动力蛋白相关的 GTP酶）和线粒体分裂 Dynamin I (Dnm1)，其半抑制浓度（IC50）为 1-10 微摩尔。- Umut Kerem Kolac, .et al. , Mol Biol Rep, 2023, Jan;50(1):493-506 PMID: 36352179
- KOLAC UK, .et al. , Research Square, 2022, 03 Jun
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Topoisomerase II 抑制剂
多柔比星是一种抗生素药物，它抑制DNA拓扑异构酶II并诱导DNA损伤和凋亡。- Laura Wiggins, .et al. , Nat Commun, 2023, 14: 1854
- Stefania Scialla, .et al. , Int J Pharm, 2023, Feb 5;632:122575 PMID: 36603672
- Fernando Espinola-Portilla, .et al. , Mol. Pharmaceutics, 2023, 20(3): 1490-1499
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- R Mahalakshmi, .et al. , Mol Biol Rep, 2022, Jan;49(1):463-476 PMID: 34739690
- J Priyanga, .et al. , Chem Biol Interact, 2020, Nov 1;331:109250 PMID: 32956706
- Abdelrehim A, .et al. , PLoS One, 2019, Feb 22;14(2):e0212701 PMID: 30794671
- J Wei, .et al. , bioRxiv, 2018, 2018
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JAK 抑制剂
S-Ruxolitinib 是 INCB018424 的手性形式，是一种强效且选择性的小分子 Janus kinase 1 (JAK1) 和 JAK2 抑制剂。 -
HDAC 抑制剂
Valproic acid 是一种 HDAC 抑制剂，其 IC50 在 0.5 至 2 mM 范围内，同时抑制 HDAC1（IC50，400 μM），并诱导 HDAC2 的蛋白酶体降解；Valproic acid sodium salt 用于治疗癫痫、双相情感障碍以及预防偏头痛。- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
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multi-targeted receptor tyrosine kinase 抑制剂
Sunitinib（SU 11248）是一种多靶点受体酪氨酸激酶抑制剂，其对VEGFR2和PDGFRβ的IC50分别为80 nM和2 nM。- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Wei Kang Cheng, .et al. , Microvasc Res, 2022, Feb 11;142:104341 PMID: 35157839
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autophagy/mitophagy 抑制剂
Liensinine 是一种自噬/线粒体自噬抑制剂。Liensinine 是从莲子（Nelumbo nucifera Gaertn）种胚提取的主要异喹啉生物碱，具有广泛的生物活性，包括抗心律失常、抗高血压、抗肺纤维化、放松血管平滑肌等。
