聚腺苷二磷酸核糖聚合酶抑制剂：PARP1 及其他。
PARP inhibition: PARP1 and beyond.
机构信息
Laval University Medical Research Center, Laval University, Québec, Canada.
出版信息
Nat Rev Cancer. 2010 Apr;10(4):293-301. doi: 10.1038/nrc2812. Epub 2010 Mar 4.
Abstract
Recent findings have thrust poly(ADP-ribose) polymerases (PARPs) into the limelight as potential chemotherapeutic targets. To provide a framework for understanding these recent observations, we review what is known about the structures and functions of the family of PARP enzymes, and then outline a series of questions that should be addressed to guide the rational development of PARP inhibitors as anticancer agents.
摘要
最近的研究发现，聚（ADP-核糖）聚合酶（PARPs）成为潜在的化疗靶点。为了为理解这些最新观察结果提供一个框架，我们回顾了 PARP 酶家族的结构和功能的已知知识，然后概述了一系列应该解决的问题，以指导 PARP 抑制剂作为抗癌药物的合理开发。
相似文献
1
PARP inhibition: PARP1 and beyond.聚腺苷二磷酸核糖聚合酶抑制剂：PARP1 及其他。
Nat Rev Cancer. 2010 Apr;10(4):293-301. doi: 10.1038/nrc2812. Epub 2010 Mar 4.
2
PARP inhibitors for cancer therapy.用于癌症治疗的聚（ADP-核糖）聚合酶抑制剂
Expert Rev Mol Med. 2005 Mar 15;7(4):1-20. doi: 10.1017/S146239940500904X.
3
Poly (ADP-ribose) polymerases inhibitor, Zj6413, as a potential therapeutic agent against breast cancer.聚（ADP-核糖）聚合酶抑制剂Zj6413，作为一种潜在的抗乳腺癌治疗药物。
Biochem Pharmacol. 2016 May 1;107:29-40. doi: 10.1016/j.bcp.2016.02.015. Epub 2016 Feb 24.
4
Combinations of PARP Inhibitors with Temozolomide Drive PARP1 Trapping and Apoptosis in Ewing's Sarcoma.聚（ADP-核糖）聚合酶（PARP）抑制剂与替莫唑胺联合使用可促使PARP1捕获并诱导尤因肉瘤细胞凋亡。
PLoS One. 2015 Oct 27;10(10):e0140988. doi: 10.1371/journal.pone.0140988. eCollection 2015.
5
New PARP targets for cancer therapy.用于癌症治疗的新型聚（ADP - 核糖）聚合酶靶点。
Nat Rev Cancer. 2014 Jul;14(7):502-9. doi: 10.1038/nrc3748. Epub 2014 Jun 5.
6
Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361.新型聚（ADP - 核糖）聚合酶 -1抑制剂AG14361的抗癌化学增敏和放射增敏作用
J Natl Cancer Inst. 2004 Jan 7;96(1):56-67. doi: 10.1093/jnci/djh005.
7
Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors in cancer chemotherapy.聚（ADP - 核糖）聚合酶 -1（PARP -1）抑制剂在癌症化疗中的应用
Recent Pat Anticancer Drug Discov. 2006 Jan;1(1):39-53. doi: 10.2174/157489206775246430.
8
9
Temozolomide pharmacodynamics in patients with metastatic melanoma: dna damage and activity of repair enzymes O6-alkylguanine alkyltransferase and poly(ADP-ribose) polymerase-1.替莫唑胺在转移性黑色素瘤患者中的药效学：DNA损伤以及修复酶O6-烷基鸟嘌呤烷基转移酶和聚（ADP-核糖）聚合酶-1的活性
Clin Cancer Res. 2005 May 1;11(9):3402-9. doi: 10.1158/1078-0432.CCR-04-2353.
10
Mitotic functions of poly(ADP-ribose) polymerases.聚（ADP-核糖）聚合酶的有丝分裂功能。
Biochem Pharmacol. 2019 Sep;167:33-43. doi: 10.1016/j.bcp.2019.03.028. Epub 2019 Mar 22.
引用本文的文献
1
Posttranscriptional RNA stabilization of telomeric RNAs FRG2, DBE-T, D4Z4 at human 4q35 in response to genotoxic stress and D4Z4 macrosatellite repeat length.人类4号染色体长臂35区（4q35）端粒RNA FRG2、DBE-T、D4Z4在转录后水平的RNA稳定性对基因毒性应激和D4Z4大卫星重复序列长度的响应
Clin Epigenetics. 2025 May 4;17(1):73. doi: 10.1186/s13148-025-01881-5.
2
Proteome-wide microarray-based screening of PAR-binding proteins.基于蛋白质组芯片的PAR结合蛋白全蛋白质组筛选。
Nucleic Acids Res. 2025 Apr 10;53(7). doi: 10.1093/nar/gkaf300.
3
Novel clinical potential of poly (ADP‑ribose) polymerase inhibitors in triple‑negative breast cancer: Mechanistic insights and clinical applications (Review).聚（ADP-核糖）聚合酶抑制剂在三阴性乳腺癌中的新型临床潜力：机制洞察与临床应用（综述）
Oncol Lett. 2025 Mar 4;29(5):215. doi: 10.3892/ol.2025.14961. eCollection 2025 May.
4
Research for a Common Thread: Insights into the Mechanisms of Six Potential Anticancer Agents.寻找共同线索的研究：六种潜在抗癌药物作用机制的见解
Molecules. 2025 Feb 24;30(5):1031. doi: 10.3390/molecules30051031.
5
Early Detection of the Pathogenetic Variants of Homologous Recombination Repair Genes in Prostate Cancer: Critical Analysis and Experimental Design.前列腺癌中同源重组修复基因致病变异的早期检测：批判性分析与实验设计
Biology (Basel). 2025 Jan 23;14(2):117. doi: 10.3390/biology14020117.
6
Impact of a Cancer-Associated Mutation on Poly(ADP-ribose) Polymerase1 Inhibition.一种癌症相关突变对聚（ADP - 核糖）聚合酶1抑制作用的影响。
J Phys Chem B. 2025 Feb 27;129(8):2175-2186. doi: 10.1021/acs.jpcb.4c07960. Epub 2025 Feb 17.
7
RECQL4 requires PARP1 for recruitment to DNA damage, and PARG dePARylation facilitates its associated role in end joining.RECQL4招募至DNA损伤处需要PARP1，而PARG去聚腺苷酸化促进其在末端连接中的相关作用。
Exp Mol Med. 2025 Feb;57(1):264-280. doi: 10.1038/s12276-024-01383-z. Epub 2025 Jan 28.
8
Drug repurposing screen targeting PARP identifies cytotoxic activity of efavirenz in high-grade serous ovarian cancer.针对聚（ADP-核糖）聚合酶（PARP）的药物重新利用筛选确定了依非韦伦在高级别浆液性卵巢癌中的细胞毒性活性。
Mol Ther Oncol. 2024 Nov 23;32(4):200911. doi: 10.1016/j.omton.2024.200911. eCollection 2024 Dec 19.
9
Colon-Targeted Poly(ADP-ribose) Polymerase Inhibitors Synergize Therapeutic Effects of Mesalazine Against Rat Colitis Induced by 2,4-Dinitrobenzenesulfonic Acid.结肠靶向聚（ADP - 核糖）聚合酶抑制剂增强美沙拉嗪对2,4 - 二硝基苯磺酸诱导的大鼠结肠炎的治疗效果。
Pharmaceutics. 2024 Dec 2;16(12):1546. doi: 10.3390/pharmaceutics16121546.
10
Novel inhibitors of PARP1 and PARP14: design, synthesis, and potentiation of cisplatin efficacy in cancer.PARP1和PARP14的新型抑制剂：设计、合成及增强顺铂在癌症治疗中的疗效
Future Med Chem. 2025 Jan;17(1):35-58. doi: 10.1080/17568919.2024.2437972. Epub 2024 Dec 18.
本文引用的文献
1
Crystal structure of the catalytic domain of human PARP2 in complex with PARP inhibitor ABT-888.人 PARP2 催化结构域与 PARP 抑制剂 ABT-888 复合物的晶体结构
Biochemistry. 2010 Feb 16;49(6):1056-8. doi: 10.1021/bi902079y.
2
PARP-3 is a mono-ADP-ribosylase that activates PARP-1 in the absence of DNA.PARP-3 是一种单 ADP-ribosylase，在没有 DNA 的情况下激活 PARP-1。
J Biol Chem. 2010 Mar 12;285(11):8054-60. doi: 10.1074/jbc.M109.077834. Epub 2010 Jan 11.
3
Synthetic lethal targeting of PTEN mutant cells with PARP inhibitors.聚腺苷二磷酸核糖聚合酶抑制剂靶向 PTEN 突变细胞的合成致死作用。
EMBO Mol Med. 2009 Sep;1(6-7):315-22. doi: 10.1002/emmm.200900041.
4
Structural and biophysical studies of human PARP-1 in complex with damaged DNA.人源 PARP-1 与损伤 DNA 复合物的结构和生物物理研究。
J Mol Biol. 2010 Feb 5;395(5):983-94. doi: 10.1016/j.jmb.2009.11.062. Epub 2009 Dec 4.
5
Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.2-{4-[(3S)-哌啶-3-基]苯基}-2H-吲唑-7-甲酰胺（MK-4827）的发现：一种新型口服聚（ADP-核糖）聚合酶（PARP）抑制剂，对BRCA-1和-2突变肿瘤有效。
J Med Chem. 2009 Nov 26;52(22):7170-85. doi: 10.1021/jm901188v.
6
Global analysis of transcriptional regulation by poly(ADP-ribose) polymerase-1 and poly(ADP-ribose) glycohydrolase in MCF-7 human breast cancer cells.聚（ADP-核糖）聚合酶-1和聚（ADP-核糖）糖苷水解酶对MCF-7人乳腺癌细胞转录调控的全局分析
J Biol Chem. 2009 Dec 4;284(49):33926-38. doi: 10.1074/jbc.M109.023879. Epub 2009 Oct 7.
7
Identification of the ADP-ribosylation sites in the PARP-1 automodification domain: analysis and implications.聚（ADP-核糖）聚合酶-1（PARP-1）自身修饰结构域中ADP-核糖基化位点的鉴定：分析及其意义
J Am Chem Soc. 2009 Oct 14;131(40):14258-60. doi: 10.1021/ja906135d.
8
Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling.端锚聚合酶抑制可使轴蛋白稳定并拮抗Wnt信号通路。
Nature. 2009 Oct 1;461(7264):614-20. doi: 10.1038/nature08356. Epub 2009 Sep 16.
9
New functions for an ancient domain.古老结构域的新功能。
Nat Struct Mol Biol. 2009 Sep;16(9):904-7. doi: 10.1038/nsmb0909-904.
10
A macrodomain-containing histone rearranges chromatin upon sensing PARP1 activation.一种含宏结构域的组蛋白在感知PARP1激活后会重新排列染色质。
Nat Struct Mol Biol. 2009 Sep;16(9):923-9. doi: 10.1038/nsmb.1664. Epub 2009 Aug 13.
Zotero 插件