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The ProTides Boom.前药核苷的热潮。
ChemMedChem. 2016 Jun 6;11(11):1114-6. doi: 10.1002/cmdc.201600156. Epub 2016 May 9.
2
Could 5'-N and S ProTide analogues work as prodrugs of antiviral agents?5'-N 和 S 核苷类似物能否作为抗病毒药物的前药？
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Phosphorodiamides as prodrugs for antiviral nucleosides.磷二酰胺作为抗病毒核苷的前药。
Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):963-6. doi: 10.1081/NCN-120022696.
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Nucleoside, nucleotide, and non-nucleoside inhibitors of hepatitis C virus NS5B RNA-dependent RNA-polymerase.丙型肝炎病毒NS5B RNA依赖性RNA聚合酶的核苷、核苷酸及非核苷抑制剂。
J Med Chem. 2012 Mar 22;55(6):2481-531. doi: 10.1021/jm201384j. Epub 2012 Jan 23.
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An overview of ProTide technology and its implications to drug discovery.ProTide 技术概述及其对药物发现的影响。
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Nucleotide prodrugs for HCV therapy.用于丙型肝炎病毒治疗的核苷酸前药。
Antivir Chem Chemother. 2011 Aug 23;22(1):23-49. doi: 10.3851/IMP1797.
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Advanced Prodrug Strategies in Nucleoside and Non-Nucleoside Antiviral Agents: A Review of the Recent Five Years.核苷类和非核苷类抗病毒药物的高级前药策略：对最近五年的综述。
Molecules. 2017 Oct 16;22(10):1736. doi: 10.3390/molecules22101736.
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Antivir Chem Chemother. 2018 Jan-Dec;26:2040206618775243. doi: 10.1177/2040206618775243.
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Progress in the development of anti-hepatitis C virus nucleoside and nucleotide prodrugs.抗丙型肝炎病毒核苷和核苷酸前药的研究进展。
Future Med Chem. 2012 Apr;4(5):625-50. doi: 10.4155/fmc.12.10.
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Current and future use of nucleo(s)tide prodrugs in the treatment of hepatitis C virus infection.核苷酸前药在丙型肝炎病毒感染治疗中的当前及未来应用。
Antivir Chem Chemother. 2018 Jan-Dec;26:2040206618756430. doi: 10.1177/2040206618756430.

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Phosphonodiamidate prodrugs of phosphoantigens (ProPAgens) exhibit potent Vγ9/Vδ2 T cell activation and eradication of cancer cells.磷酸抗原的膦酸二酰胺前药（ProPAgens）表现出强大的Vγ9/Vδ2 T细胞激活作用并能根除癌细胞。
RSC Med Chem. 2024 Jun 3;15(7):2462-2473. doi: 10.1039/d4md00208c. eCollection 2024 Jul 17.
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Advanced prodrug strategies in nucleoside analogues targeting the treatment of gastrointestinal malignancies.靶向胃肠道恶性肿瘤治疗的核苷类似物中的先进前药策略。
Front Cell Dev Biol. 2023 Apr 18;11:1173432. doi: 10.3389/fcell.2023.1173432. eCollection 2023.
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Prodrugs of Nucleoside 5'-Monophosphate Analogues: Overview of the Recent Literature Concerning their Synthesis and Applications.核苷 5'-单磷酸类似物前药：关于其合成和应用的近期文献综述。
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J Med Chem. 2020 Oct 8;63(19):11258-11270. doi: 10.1021/acs.jmedchem.0c01232. Epub 2020 Sep 29.
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A Subcutaneous Implant of Tenofovir Alafenamide Fumarate Causes Local Inflammation and Tissue Necrosis in Rabbits and Macaques.富马酸替诺福韦艾拉酚胺的皮下植入物可引起兔和猕猴的局部炎症和组织坏死。
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本文引用的文献

1
Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys.小分子GS-5734对恒河猴体内埃博拉病毒的治疗效果。
Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2.
2
Discontinued drugs in 2012 - 2013: hepatitis C virus infection.2012 - 2013年停用的药物：丙型肝炎病毒感染
Expert Opin Investig Drugs. 2015 Feb;24(2):239-51. doi: 10.1517/13543784.2015.982274. Epub 2014 Nov 11.
3
Discovery of PSI-353661, a Novel Purine Nucleotide Prodrug for the Treatment of HCV Infection.PSI-353661的发现，一种用于治疗丙型肝炎病毒感染的新型嘌呤核苷酸前药。
ACS Med Chem Lett. 2010 Dec 17;2(2):130-5. doi: 10.1021/ml100209f. eCollection 2011 Feb 10.
4
Application of ProTide technology to gemcitabine: a successful approach to overcome the key cancer resistance mechanisms leads to a new agent (NUC-1031) in clinical development.ProTide 技术在吉西他滨中的应用：克服关键癌症耐药机制的成功方法导致一种新的药物（NUC-1031）进入临床开发。
J Med Chem. 2014 Feb 27;57(4):1531-42. doi: 10.1021/jm401853a. Epub 2014 Feb 14.
5
Advances in the development of nucleoside and nucleotide analogues for cancer and viral diseases.核苷和核苷酸类似物在癌症和病毒疾病方面的研发进展。
Nat Rev Drug Discov. 2013 Jun;12(6):447-64. doi: 10.1038/nrd4010.
6
Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside.抗癌剂氟达拉滨的磷酰胺酯前药在细胞内成功传递预先形成的生物活性单磷酸盐，并优于亲本核苷。
J Med Chem. 2011 Oct 27;54(20):7247-58. doi: 10.1021/jm200815w. Epub 2011 Sep 27.
7
INX-08189, a phosphoramidate prodrug of 6-O-methyl-2'-C-methyl guanosine, is a potent inhibitor of hepatitis C virus replication with excellent pharmacokinetic and pharmacodynamic properties.INX-08189 是一种 6-O-甲基-2'-C-甲基鸟苷的磷酰胺酯前药，是一种有效的丙型肝炎病毒复制抑制剂，具有良好的药代动力学和药效学特性。
Antimicrob Agents Chemother. 2011 May;55(5):1843-51. doi: 10.1128/AAC.01335-10. Epub 2011 Feb 28.
8
Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus.发现一种β-d-2'-脱氧-2'-α-氟-2'-β-C-甲基尿苷核苷酸前药（PSI-7977），用于治疗丙型肝炎病毒。
J Med Chem. 2010 Oct 14;53(19):7202-18. doi: 10.1021/jm100863x.
9
Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus.设计、合成及评价新型双重前药 INX-08189：一种新型丙型肝炎病毒临床候选药物。
Bioorg Med Chem Lett. 2010 Aug 15;20(16):4850-4. doi: 10.1016/j.bmcl.2010.06.094. Epub 2010 Jun 20.
10
Aryloxy phosphoramidate triesters: a technology for delivering monophosphorylated nucleosides and sugars into cells.芳氧基磷酰胺酸酯三酯：将单磷酸化核苷和糖递送到细胞内的技术。
ChemMedChem. 2009 Nov;4(11):1779-91. doi: 10.1002/cmdc.200900289.

前药核苷的热潮。

The ProTides Boom.

作者信息

Mehellou Youcef

机构信息

School of Pharmacy, College of Medical and Dental Sciences, University of Birmingham, Edgbaston, B15 2TT, UK.

出版信息

ChemMedChem. 2016 Jun 6;11(11):1114-6. doi: 10.1002/cmdc.201600156. Epub 2016 May 9.

DOI:10.1002/cmdc.201600156
PMID:27159529
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7162417/
Abstract

The masking of nucleoside phosphate and phosphonate groups by an aryl motif and an amino acid ester, nowadays known as the 'ProTide' technology, has proven to be effective in the discovery of nucleotide therapeutics. Indeed, this technology, which was invented by Chris McGuigan in the early 1990s, has inspired the discovery of two FDA-approved antiviral nucleotide drugs, and many more are currently undergoing (pre)clinical development. The usefulness of this technology in the discovery of nucleotide therapeutics is showcased in this Highlight by discussing the ProTides development and the various ProTides that have reached clinical trials.

摘要

如今被称为“前药核苷酸”技术的，通过芳基基序和氨基酸酯对核苷磷酸酯和膦酸酯基团进行的掩蔽，已被证明在核苷酸疗法的发现中是有效的。事实上，这项由克里斯·麦奎根在20世纪90年代初发明的技术，激发了两种获美国食品药品监督管理局批准的抗病毒核苷酸药物的发现，目前还有更多药物正在进行（前）临床开发。本综述通过讨论前药核苷酸的研发情况以及已进入临床试验的各种前药核苷酸，展示了该技术在核苷酸疗法发现中的实用性。