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具有针对非洲锥虫 Trypanosoma brucei 高活性的人组蛋白去乙酰化酶抑制剂。

Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei.

机构信息

Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK.

出版信息

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1886-90. doi: 10.1016/j.bmcl.2012.01.072. Epub 2012 Jan 28.

DOI:10.1016/j.bmcl.2012.01.072
PMID:22326398
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3314994/
Abstract

A number of hydroxamic acid derivatives which inhibit human histone deacetylases were investigated for efficacy against cultured bloodstream form Trypanosoma brucei. Three out of the four classes tested displayed significant activity. The majority of compounds blocked parasite growth in the submicromolar range. The most potent was a member of the sulphonepiperazine series with an IC(50) of 34nM. These results identify lead compounds with potential for the development of a novel class of trypanocidal agent.

摘要

研究了一些抑制人组蛋白去乙酰化酶的羟肟酸衍生物，以评估其对培养的布鲁氏锥虫血液体形式的疗效。在所测试的四类中的三类显示出显著的活性。大多数化合物以亚微摩尔范围阻止寄生虫生长。最有效的是磺酰哌嗪系列的成员，IC（50）为 34nM。这些结果确定了具有开发新型杀锥虫剂潜力的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/6609754cbecf/fx2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/c303919fbcef/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/dc5cd1cacbcd/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/da9b1a8f2717/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/5923308e3922/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/6609754cbecf/fx2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/c303919fbcef/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/dc5cd1cacbcd/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/da9b1a8f2717/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/5923308e3922/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c93/3314994/6609754cbecf/fx2.jpg

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1
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2
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Am J Transl Res. 2011 Feb;3(2):166-79. Epub 2010 Dec 26.
3
The therapeutic potential of HDAC inhibitors in the treatment of multiple sclerosis.组蛋白去乙酰化酶抑制剂在多发性硬化治疗中的治疗潜力。
Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. doi: 10.1016/j.ijpddr.2017.01.001. Epub 2017 Jan 10.
4
Repurposing strategies for tropical disease drug discovery.热带病药物研发的重新利用策略。
Bioorg Med Chem Lett. 2016 Jun 1;26(11):2569-76. doi: 10.1016/j.bmcl.2016.03.103. Epub 2016 Mar 30.
5
Targeting Lysine Deacetylases (KDACs) in Parasites.靶向寄生虫中的赖氨酸脱乙酰酶（KDACs）。
PLoS Negl Trop Dis. 2015 Sep 24;9(9):e0004026. doi: 10.1371/journal.pntd.0004026. eCollection 2015.
6
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Int J Parasitol Drugs Drug Resist. 2015 Jun 20;5(3):117-26. doi: 10.1016/j.ijpddr.2015.05.004. eCollection 2015 Dec.
7
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PLoS Negl Trop Dis. 2014 Oct 23;8(10):e3253. doi: 10.1371/journal.pntd.0003253. eCollection 2014 Oct.
8
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9
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10
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Mol Med. 2011 May-Jun;17(5-6):442-7. doi: 10.2119/molmed.2011.00077. Epub 2011 Feb 25.
4
Molecular mechanisms underlying the control of antigenic variation in African trypanosomes.控制非洲锥虫抗原变异的分子机制。
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5
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6
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ChemMedChem. 2010 Aug 2;5(8):1232-5. doi: 10.1002/cmdc.201000087.
7
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Expert Rev Mol Med. 2009 Oct 29;11:e31. doi: 10.1017/S1462399409001252.
8
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9
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Genes Dev. 2009 May 1;23(9):1063-76. doi: 10.1101/gad.1790409. Epub 2009 Apr 15.
10
Targeting histone deacetylase inhibitors for anti-malarial therapy.靶向组蛋白去乙酰化酶抑制剂用于抗疟治疗。
Curr Top Med Chem. 2009;9(3):292-308. doi: 10.2174/156802609788085313.