Protein Information

Name histone deacetylase (protein family or complex)
Synonyms Histone deacetylase; Histone deacetylases

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
20217840 Chakrabarty S, Jasmine, Bhadaliya C, Sinha BN, Mahesh A, Bai H, Blond SY, Jayaprakash V: Inhibitors of human histone deacetylase: synthesis and enzyme assay of hydroxamates with piperazine linker. Arch Pharm. 2010 Mar;343(3):167-72.
114(1,2,2,4) Details
17827005 Anandan SK, Ward JS, Brokx RD, Denny T, Bray MR, Patel DV, Xiao XY: Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5995-9. Epub 2007 Aug 19.

The thiazole ring connects to a piperazine spacer, which is capped with a sulfonamide group.
2(0,0,0,2) Details
19111466 Smil DV, Manku S, Chantigny YA, Leit S, Wahhab A, Yan TP, Fournel M, Maroun C, Li Z, Lemieux AM, Nicolescu A, Rahil J, Lefebvre S, Panetta A, Besterman JM, Deziel R: Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors. Bioorg Med Chem Lett. 2009 Feb 1;19(3):688-92. Epub 2008 Dec 14.

In an effort to identify HDAC isoform selective inhibitors, we designed and synthesized novel, chiral 3,4-dihydroquinoxalin-2 (1H)-one and piperazine-2,5-dione aryl hydroxamates showing selectivity (up to 40-fold) for human HDAC6 over other class I/IIa HDACs.
1(0,0,0,1) Details
16670375 Cassel S, Carouge D, Gensburger C, Anglard P, Burgun C, Dietrich JB, Aunis D, Zwiller J: Fluoxetine and cocaine induce the epigenetic factors MeCP2 and MBD1 in adult rat brain. Mol Pharmacol. 2006 Aug;70(2):487-92. Epub 2006 May 2.

Once bound to methylated CpG sites, methyl-CpG-binding protein 2 (MeCP2) is thought to silence transcription of downstream genes by recruiting a histone deacetylase (HDAC).
Mecp2 was not induced by repeated injections of 1-(2-bis (4-fluorphenyl)-methoxy)-ethyl)-4-(3-phenyl-propyl) piperazine (GBR-12909) or nortriptyline.
1(0,0,0,1) Details