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Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).三取代噻唑作为恶性疟原虫蛋白激酶G（PfPKG）的强效和选择性抑制剂。
Bioorg Med Chem Lett. 2018 Oct 15;28(19):3168-3173. doi: 10.1016/j.bmcl.2018.08.028. Epub 2018 Aug 27.
2
Potent inhibitors of malarial P. Falciparum protein kinase G: Improving the cell activity of a series of imidazopyridines.疟原虫 Pf 蛋白激酶 G 的强效抑制剂：提高一系列咪唑并吡啶类化合物的细胞活性。
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3
Characterization of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG): antiparasitic activity of a PKG inhibitor.恶性疟原虫环磷酸鸟苷依赖性蛋白激酶（PfPKG）的特性：PKG抑制剂的抗寄生虫活性
Mol Biochem Parasitol. 2006 Mar;146(1):78-88. doi: 10.1016/j.molbiopara.2005.10.020. Epub 2005 Nov 17.
4
High-throughput screening of the Plasmodium falciparum cGMP-dependent protein kinase identified a thiazole scaffold which kills erythrocytic and sexual stage parasites.高通量筛选恶性疟原虫环鸟苷酸依赖蛋白激酶发现噻唑骨架可杀灭红细胞期和有性期寄生虫。
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Mechanism of allosteric inhibition in the cGMP-dependent protein kinase.别构抑制在 cGMP 依赖性蛋白激酶中的作用机制。
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Potent bicyclic inhibitors of malarial cGMP-dependent protein kinase: approaches to combining improvements in cell potency, selectivity and structural novelty.强效双环疟疾cGMP依赖性蛋白激酶抑制剂：结合提高细胞效力、选择性和结构新颖性的方法
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Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1).取代的咪唑并吡啶类化合物是恶性疟原虫钙依赖蛋白激酶 1（PfCDPK1）的有效和选择性抑制剂。
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8
Imidazopyridazine Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinase 1 Also Target Cyclic GMP-Dependent Protein Kinase and Heat Shock Protein 90 To Kill the Parasite at Different Stages of Intracellular Development.恶性疟原虫钙依赖性蛋白激酶1的咪唑并哒嗪抑制剂还靶向环磷酸鸟苷依赖性蛋白激酶和热休克蛋白90，以在细胞内发育的不同阶段杀死疟原虫。
Antimicrob Agents Chemother. 2015 Dec 28;60(3):1464-75. doi: 10.1128/AAC.01748-15.
9
Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase.恶性疟原虫 cGMP 依赖性蛋白激酶竞争性抑制剂的表征。
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J Med Chem. 2019 Oct 24;62(20):9217-9235. doi: 10.1021/acs.jmedchem.9b01099. Epub 2019 Oct 14.

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A Review on Synthetic Thiazole Derivatives as an Antimalarial Agent.合成噻唑衍生物作为抗疟药物的综述。
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Preparation, biological evaluation and QSAR analysis of urea substituted 2,4-diamino-pyrimidine anti-malarials.尿素取代的2,4-二氨基嘧啶抗疟药的制备、生物学评价及定量构效关系分析
RSC Med Chem. 2022 Oct 20;13(12):1587-1604. doi: 10.1039/d2md00218c. eCollection 2022 Dec 14.
3
Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase.恶性疟原虫 cGMP 依赖性蛋白激酶竞争性抑制剂的表征。
Chembiochem. 2022 Apr 5;23(7):e202100704. doi: 10.1002/cbic.202100704. Epub 2022 Feb 23.
4
Editorial: Heading Against Parasitic Resistance: A Screen for Next Generation Drugs Against Targets of cAMP- or cGMP-regulated Pathways.社论：对抗寄生虫耐药性：筛选针对cAMP或cGMP调节途径靶点的下一代药物
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Physicochemical Profiling and Comparison of Research Antiplasmodials and Advanced Stage Antimalarials with Oral Drugs.研究性抗疟药和晚期抗疟药与口服药物的物理化学特征分析及比较
ACS Omega. 2021 Feb 25;6(9):6424-6437. doi: 10.1021/acsomega.1c00104. eCollection 2021 Mar 9.
6
cGMP-Dependent Protein Kinase - A Novel Chemotherapeutic Target.环磷酸鸟苷依赖性蛋白激酶——一种新型化疗靶点。
Front Microbiol. 2021 Feb 3;11:610408. doi: 10.3389/fmicb.2020.610408. eCollection 2020.
7
Kinases as Potential Drug Targets for Malaria: Challenges and Opportunities.激酶作为疟疾的潜在药物靶点：挑战与机遇
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Discovery of isoxazolyl-based inhibitors of cGMP-dependent protein kinase.基于异恶唑基的环磷酸鸟苷依赖性蛋白激酶抑制剂的发现。
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Targeting the Malaria Parasite cGMP-Dependent Protein Kinase to Develop New Drugs.靶向疟原虫环磷酸鸟苷依赖性蛋白激酶以开发新药。
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Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments.疟原虫激酶抑制剂：最新进展。
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本文引用的文献

1
A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.针对疟疾环磷酸鸟苷依赖性蛋白激酶的强效系列药物可清除感染并阻断传播。
Nat Commun. 2017 Sep 5;8(1):430. doi: 10.1038/s41467-017-00572-x.
2
Invasion of hepatocytes by Plasmodium sporozoites requires cGMP-dependent protein kinase and calcium dependent protein kinase 4.疟原虫子孢子侵入肝细胞需要环磷酸鸟苷依赖性蛋白激酶和钙依赖性蛋白激酶4。
Mol Microbiol. 2016 Oct;102(2):349-363. doi: 10.1111/mmi.13466. Epub 2016 Aug 9.
3
Phosphoproteomics reveals malaria parasite Protein Kinase G as a signalling hub regulating egress and invasion.磷酸化蛋白质组学揭示疟原虫蛋白激酶G作为调控出芽和入侵的信号枢纽。
Nat Commun. 2015 Jul 7;6:7285. doi: 10.1038/ncomms8285.
4
The threat of artemisinin-resistant malaria.耐青蒿素疟疾的威胁。
N Engl J Med. 2011 Sep 22;365(12):1073-5. doi: 10.1056/NEJMp1108322.
5
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.开发含有芳基磺酰胺头基的强效 B-RafV600E 抑制剂。
Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436-40. doi: 10.1016/j.bmcl.2011.06.021. Epub 2011 Jun 16.
6
Kinase selectivity potential for inhibitors targeting the ATP binding site: a network analysis.靶向 ATP 结合位点的抑制剂的激酶选择性潜力：网络分析。
Bioinformatics. 2010 Jan 15;26(2):198-204. doi: 10.1093/bioinformatics/btp650. Epub 2009 Nov 26.
7
Role of Plasmodium berghei cGMP-dependent protein kinase in late liver stage development.疟原虫 cGMP 依赖蛋白激酶在肝脏晚期发育阶段的作用。
J Biol Chem. 2010 Jan 29;285(5):3282-8. doi: 10.1074/jbc.M109.070367. Epub 2009 Nov 24.
8
The malaria parasite cyclic GMP-dependent protein kinase plays a central role in blood-stage schizogony.疟原虫环磷酸鸟苷依赖性蛋白激酶在血液阶段裂体生殖中起核心作用。
Eukaryot Cell. 2010 Jan;9(1):37-45. doi: 10.1128/EC.00186-09. Epub 2009 Nov 13.
9
A cyclic GMP signalling module that regulates gliding motility in a malaria parasite.一个调节疟原虫滑行运动的环鸟苷酸信号模块。
PLoS Pathog. 2009 Sep;5(9):e1000599. doi: 10.1371/journal.ppat.1000599. Epub 2009 Sep 25.
10
Gametogenesis in malaria parasites is mediated by the cGMP-dependent protein kinase.疟原虫的配子发生由依赖环磷酸鸟苷的蛋白激酶介导。
PLoS Biol. 2008 Jun 3;6(6):e139. doi: 10.1371/journal.pbio.0060139.

三取代噻唑作为恶性疟原虫蛋白激酶G（PfPKG）的强效和选择性抑制剂。

Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).

作者信息

Tsagris Denise J, Birchall Kristian, Bouloc Nathalie, Large Jonathan M, Merritt Andy, Smiljanic-Hurley Ela, Wheldon Mary, Ansell Keith H, Kettleborough Catherine, Whalley David, Stewart Lindsay B, Bowyer Paul W, Baker David A, Osborne Simon A

机构信息

LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.

LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.

出版信息

Bioorg Med Chem Lett. 2018 Oct 15;28(19):3168-3173. doi: 10.1016/j.bmcl.2018.08.028. Epub 2018 Aug 27.

DOI:10.1016/j.bmcl.2018.08.028
PMID:30174152
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6193536/
Abstract

A series of trisubstituted thiazoles have been identified as potent inhibitors of Plasmodium falciparum (Pf) cGMP-dependent protein kinase (PfPKG) through template hopping from known Eimeria PKG (EtPKG) inhibitors. The thiazole series has yielded compounds with improved potency, kinase selectivity and good in vitro ADME properties. These compounds could be useful tools in the development of new anti-malarial drugs in the fight against drug resistant malaria.

摘要

通过从已知的艾美球虫PKG（EtPKG）抑制剂进行模板跳跃，一系列三取代噻唑已被鉴定为恶性疟原虫（Pf）环鸟苷酸依赖性蛋白激酶（PfPKG）的有效抑制剂。噻唑系列已产生了具有提高的效力、激酶选择性和良好体外吸收、分布、代谢和排泄（ADME）特性的化合物。这些化合物可能是开发新型抗疟药物以对抗耐药性疟疾的有用工具。