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Antioxidant, antiangiogenic, antitumor agent
(-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea.- Grace Northrop, .et al. , Food Funct, 2022, Apr 4;13(7):3894-3904 PMID: 35285840
- Wafa Dridi, .et al. , Carbohydr Polym, 2021, 274:118670 PMID: 34702486
- A S D'Costa, .et al. , Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Fenteany G, .et al. , Sci Rep, 2019, Sep 5;9(1):12801 PMID: 31488855
- LiliSun, .et al. , Nutrition, 2019, pii:S0899-9007(18)31140-7
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Fluoroquinolone antibiotic
ABT-492 is a new fluoroquinolone against 155 aerobic and 171 anaerobic pathogens. -
PARP inhibitor
ABT-888(Veliparib) is a potential anti-cancer drug acting as a PARP inhibitor.- Subhajit Chatterjee, .et al. , Cell Signal, 2021, Apr;80:109902 PMID: 33373686
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Protein Synthesis Inhibitor
Cycloheximide (also known as actidione) is used as an selective antibiotic. It inhibits the protein synthesis (DNA-dependent RNA) of saprobic fungi eukaryotes. by binding with the 80S ribosome, while inactive against dermatophytes and systemic fungi.- 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 is an anthracycline antibiotic, it works by intercalating DNA, while most serious adverse effect being life-threatening heart damage. It is commonly used in the treatment of a wide range of cancers, including hematological malignancies, many types of carcinoma, and soft tissue sarcomas.
- Sanaz Naghibi, .et al. , Biosensors (Basel), 2022, May 29;12(6):373 PMID: 35735521
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DNA and RNA synthesis inhibitor
Fluorouracil (Adrucil) is a suicide inhibitor and works through irreversible inhibition of thymidylate synthase.- 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) is a PARP inhibitor that inhibits poly(ADP-ribose) polymerase (PARP) is a key enzyme in DNA repair.- 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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PARP inhibitor
AG14361 is a potent PARP inhibitor, enhanced TMZ cytotoxicity in MMR(mismatch repair)-proficient / deficient cells.- Vimal Pandey, .et al. , Scientific Reports, 2019, 9, Article number: 5012 PMID: 30899038
- Alendronate is a nitrogen-containing bisphosphonate that is commonly used in the treatment of osteoporosis and other metabolic bone diseases.
- Altretamine is classified as an alkylating antineoplastic agent.This unique structure is believed to damage tumor cells through the production of the weakly alkylating species formaldehyde, a product of CYP450-mediated N-demethylation.
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Topoisomerase inhibitor
Amonafide is a DNA intercalator and topoisomerase II inhibitor for the treatment of neoplastic diseases, one of Antitumor agent.
- Veronica Rendo, .et al. , Nat Commun, 2020, 11: 1308 PMID: 32161261
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PARP inhibitor
Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.- Saptarshi Sinha, .et al. , Med Oncol, 2024, Jan 6;41(2):49 PMID: 38184505
- 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) is a HDAC inhibitor that inhibits HDAC activity in HeLa cell extracts with an IC50 of 27 nM.- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
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Bendamustine Hydrochloride is a small molecule bifunctional DNA alkylating agent, combining a nitrogen mustard functionality with a purine-analog structure. The dense DNA-damaging functionality of Bendamustine differentiates it from other compounds used as antiproliferative agents, and these functionalities are thought to promote cell death through a variety of different pathways including apoptosis and mitotic catastrophe.
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Berberine hydrochloride was novelly found that it has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities. Berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD activity.
- 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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PI3K/mTOR Inhibitor
BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.- 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 is a selective telomerase inhibitor (IC50 values are 93, > 100000 and > 100000 nM for human telomerase, human RNA polymerase I and human RNA polymerase II + III respectively).
- Hosoi T, .et al. , Neurosci Lett, 2016, Aug 26;629:241-244 PMID: 27443785
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DNA/RNA Synthesis inhibitor
Bleomycin sulfate is a mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus.- 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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PARP inhibitor
BSI-201 is a potent inhibitor of PARP-1 and has been shown to cross the blood-brain barrier.- Jianwei Dou, .et al. , J Sep Sci, 2020, Dec 4 PMID: 33275824
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Topoisomerase I inhibitor
Camptothecin is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I).- Kengo Takeda, .et al. , Int J Mol Sci, 2024, Mar 26;25(7):3693 PMID: 38612503
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Carboplatin is a chemotherapy drug used against some forms of cancer (mainly ovarian carcinoma, lung, head and neck cancers). Cisplatin and carboplatin, as well as oxaliplatin, interact with DNA, akin to the mechanism of alkylating agents.
- Hye Ryeong Jun, .et al. , Biomaterials, 2023, May;296:122087 PMID: 36924663
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Jianwei Dou, .et al. , J Sep Sci, 2020, Dec 4 PMID: 33275824
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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.
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DNA/RNA Synthesis inhibitor
Cidofovir (Vistide) is an antiviral used for the treatment of cytomegalovirus (CMV) infection (ie: retinitis).- Adhikary A, .et al. , J Phys Chem B, 2015, Sep 3;119(35):11496-505 PMID: 26237072
- Cisplatin was the first member of a class of platinum-containing anti-cancer drugs, which now also includes carboplatin and oxaliplatin. These platinum complexes react in vivo, binding to and causing crosslinking of DNA, which ultimately triggers apoptosis (programmed cell death).
- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Ping Tian, .et al. , Chem Biol Drug Des, 2024, Jan;103(1):e14424 PMID: 38230774
- Jintian Song, .et al. , J Cancer, 2023, May 21;14(9):1515-1530 PMID: 37325046
- Huan Li, Srinivas Chatla, .et al. , Res Sq, 2023, Apr 6;rs.3.rs-2688694 PMID: 37066268
- Min-Yung Kuo, .et al. , Int J Mol Sci, 2022, Dec 21;24(1):138 PMID: 36613579
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- RUI-NING LIANG, .et al. , Research Square, 2022, July 6th
- Wei Zeng, .et al. , Exp Ther Med, 2021, May; 21(5): 424 PMID: 33747163
- Yi-Ru Pan, .et al. , Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
- Amnah Alshangiti, .et al. , Neuronal Signal, 2019, 2019
- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
- Pi-Lin Sung, .et al. , Oncotarget, 2016, Jan 26; 7(4): 4036-4047 PMID: 26716408
- Clafen (Cyclophosphamide) is a nitrogen mustard alkylating agent. An alkylating agent adds an alkyl group (CnH2n+1) to DNA. It attaches the alkyl group to the guanine base of DNA, at the number 7 nitrogen atom of the imidazole ring.
- 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/RNA Synthesis inhibitor
Clofarabine is a second generation purine nucleoside analog with antineoplastic activity- Xie J, .et al. , Pediatr Blood Cancer, 2019, Dec 25:e28133 PMID: 31876116
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Telomerase inhibitor
Costunolide is an Inhibitor of human telomerase activity (IC50 = 65 μM in MCF-7 breast cancer cells). It is described to act as an antioxidant, anti-mycobacterial, anti-inflammatory, and anti-viral, with cytotoxic activity. - Dacarbazine is an antineoplastic chemotherapy drug used in the treatment of various cancers.Dacarbazine is a member of the class of alkylating agents, which destroy cancer cells by adding an alkyl group (CnH2n+1) to its DNA.
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DNA/RNA Synthesis inhibitor
Daptomycin is a lipopeptide antibiotic used in the treatment of certain infections caused by Gram-positive organisms.- 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 is a selective inhibitor of HDAC3, HDAC6, and HDAC8 that shows comparable inhibition of HDAC6 and HDAC8 with IC50 = 2.47 and 1.46 μmol/L, respectively. -
Topoisomerase II inhibitor
Epirubicin is a cell-permeable anthracycline antitumor antibiotic. It is a stereoisomer(4?€?-epi-isomer) of doxorubicin that exhibits reduced cardiotoxicity. It is used to inhibit topoisomerase II and DNA helicase activity. -
DNA/RNA Synthesis inhibitor
Oxaliplatin is a platinum-based antineoplastic agent that is used in cancer chemotherapy. In vivo studies showed that Oxaliplatin has anti-tumor activity against colon carcinoma through its (non-targeted) cytotoxic effects.- 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
Etoposide forms a ternary complex with DNA and the topoisomerase II enzyme (which aids in DNA unwinding), prevents re-ligation of the DNA strands, and by doing so causes DNA strands to break. Therefore, this causes errors in DNA synthesis and promotes apoptosis of the cancer cell.- 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 is a potent and selective SIRT1 class III histone deacetylase enzyme inhibitor with IC50 of 38 nM in a cell-free assay.- 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
- Fisetin is a flavonol, a structurally distinct chemical substance that belongs to the flavonoid group of polyphenols. It can be found in many plants, where it serves as a colouring agent. Possible anti-aging, anti-inflammatory, anti-cancer, and anti-viral properties of fisetin are under active scientific investigation.
- Bih-Cheng Chen, .et al. , Phytomedicine, 2019, Apr; 57:1-8
- Jeng LB, .et al. , J Cell Physiol, 2018, Sep;233(9):7134-7142 PMID: 29574877
- Kuan-Ho Lin, .et al. , Journal of Functional Foods, 2018, 52: 212-218
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DNA/RNA Synthesis inhibitor
Floxuridine is an oncology drug that belongs to the class known as antimetabolites. - Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.
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DNA/RNA Synthesis inhibitor
Tegafur is a chemotherapeutic 5-FU prodrug used in the treatment of cancers. It is a component of tegafur-uracil.- 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
Gatifloxacin is a fluoroquinolone antibiotic which inhibits bacterial DNA gyrase (IC50 = 0.109 ng/ml) and topoisomerase IV (IC50 = 13.8 ng/ml). -
DNA/RNA Synthesis inhibitor
Gemcitabine (Gemzar) is a newer chemotherapy drug acting by replacing one of the building blocks of nucleic acids during DNA replication in cancer cells, preventing tumor growth.- Chiao-Ping Chen, .et al. , Biomed Pharmacother, 2023, Oct:166:115389 PMID: 37659202
- G. R. Iglesias, .et al. , Polymers, 2018, 10(3), 269
- Genistin is an isoflavone found in a number of dietary plants like soy and kudzu. It was shown to stimulate estrogen-dependent breast cancer cell growth in vivo.
- 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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Topoisomerase inhibitor
Idarubicin is an anthracycline antibiotic that is an anti-leukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin.- Wei Y, .et al. , Mol Cell, 2017, Jun 1;66(5):581-596.e6 PMID: 28552615
- Ifosfamide is a cytostatic agent that is structurally related to cyclophosphamide.
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PARP Inhibitor
3-Aminobenzamide is a novel PARP inhibitor, known to sensitize cells to radiation in vitro by inhibiting the repair of DNA damage.- Kamada Y, .et al. , Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
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Topoisomerase I inhibitor
Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.- 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
Irinotecan (CPT 11), a compound within the camptothecin family, is an inhibitor of topoisomerase 1 involved in cellular DNA replication and transcription. -
HDAC inhibitor
ITF2357 (Givinostat) is a HDACs inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities.- 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) is a pan-HDAC inhibitor with marked potency toward HDAC1 (IC(50), 0.16 nmol/L).- Minoru Ueda, .et al. , Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096