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Structure-activity relationships of histone deacetylase inhibitors

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Author:: No author available

Journal Title:: ACTA PHARMACEUTICA SINICA

Issue:: 10

DOI:: 10.3321/j.issn:0513-4870.2009.10.003

Key Word:: 组蛋白;HDAC抑制剂;构效关系

Abstract：组蛋白去乙酰化酶(histone deacetylases,HDACs)作为调控基因的关键蛋白酶,其功能异常被证实与肿瘤的发生和发展有直接关系.通过对HDAC功能的抑制调节,可以达到治疗肿瘤的目的.组蛋白去乙酰化酶抑制剂的作用机制已得到广泛研究,已开发出各种组蛋白去乙酰化酶抑制剂.按结构类型,组蛋白去乙酰化酶抑制剂大致可以分为:异羟肟酸类化合物(hydroxamic acid)、环状四肽类化合物、脂肪酸盐类化合物、苯甲酰胺类化合物和亲电酮类化合物等.本文对组蛋白去乙酰化酶抑制剂的各类结构及构效关系作一综述.

Reference

[1]冯娟,解鹏,翁志洁,等.N-取代苯甲酰胺类衍生物的合成与抗肿瘤活性[J].2009,(6).
[2].GCN5 and BCR signalling collaborate to induce pre-mature B cell apoptosis through depletion of ICAD and IAP2 and activation of caspase activities.[J].2008,419(1/2).
[3]Charrier C,Roche J,Gesson JP,etc.Antiproliferative activities of a library of hybrids between indanones and HDAC inhibitor SAHA and MS-275 analogues.[J].2007,17(22).
[4]Jennings AJ,Chi E,Skene RJ,etc.Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases[J].2004,12(7).
[5]Nawrocki ST,Carew JS,Giles FJ.Histone deacetylase inhibitors: mechanisms of cell death and promise in combination cancer therapy.[J].2008,269(1).
[6]Kattar SD,Surdi LM,Zabierek A,etc.Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.[J].2009,19(4).
[7]Weiss TS,Gottlicher M,Lauer UM,etc.Apoptosis on hepatoma cells but not on primary hepatocytes by histone deacetylase inhibitors valproate and ITF2357.[J].2005,42(2).
[8]Eot-Houllier G,Jaulin C,Magnaghi-Jaulin L,etc.Histone deacetylase inhibitors and genomic instability.[J].2009,274(2).
[9]Koustova E,Shults C,Lin T,etc.Histone deacetylase as therapeutic target in a rodent model of hemorrhagic shock: effect of different resuscitation strategies on lung and liver.[J].2007,141(6).
[10]Tini M,Altucci L,Nebbioso A,etc.Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases.[J].2009,19(4).
[11]Vesci L,Barbarino M,Zunino F,etc.Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.[J].2009,44(5).
[12]Yuko Sumida,Tamaki Kato,Shinji Okamura,etc.Cyclic Tetrapeptides Bearing a Sulfhydryl Group Potently Inhibit Histone Deacetylases[J].2003,5(26).
[13]Wenxin Gu,Mercedes Cueto,Paul R. Jensen,etc.Microsporins A and B: new histone deacetylase inhibitors from the marine-derived fungus Microsporum cf. gypseum and the solid-phase synthesis of microsporin A[J].2007,63(28).
[14]Lentzsch S,Hassig CA,Ma H,etc.KD5170, a novel mercaptoketone-based histone deacetylase inhibitor, exerts antimyeloma effects by DNA damage and mitochondrial signaling.[J].2008,7(6).
[15]Ideo A,Kawase M,Kanda Y,etc.Cytotoxic activity of selected trifluoromethyl ketones against oral tumor cells.[J].2006,26(6B).
[16]J. Kell.Mgcd-0103[J].2008,33(4).
[17]Lee JS,Noh EJ,Jeong G,etc.An HDAC inhibitor, trichostatin A, induces a delay at G2/M transition, slippage of spindle checkpoint, and cell death in a transcription-dependent manner.[J].2009,378(3).
[18]Gregoretti I,Lee YM,Goodson HV.Molecular evolution of the histone deacetylase family: functional implications of phylogenetic analysis.[J].2004,338(1).
[19]Jarak I,Zinic M,Suman L,etc.Novel Cyano- and N-Isopropylamidino-Substituted Derivatives of Benzo(b)thiophene-2-carboxanilides and Benzo(b)thieno(2,3-c)quinolones: Synthesis, Photochemical Synthesis, Crystal Structure Determination, and Antitumor Evaluation. 2.[J].2005,48(7).
[20]Krennhrubec K,Marshall BL,Hedglin M,etc.Design and evaluation of 'Linkerless' hydroxamic acids as selective HDAC8 inhibitors.[J].2007,17(10).
[21]Wenxin Gu,Curt M. Horvath,Inna Nusinzon,etc.Carbonyl- and sulfur-containing analogs of suberoylanilide hydroxamic acid: Potent inhibition of histone deacetylases[J].2006,14(10).
[22]Minucci S,Botrugno OA,Santoro F.Histone deacetylase inhibitors as a new weapon in the arsenal of differentiation therapies of cancer.[J].2009,280(2).
[23]Bottoni P,Brosch G,Mai A,etc.Exploring the connection unit in the HDAC inhibitor pharmacophore model: Novel uracil-based hydroxamates.[J].2005,15(21).
[24]MacDonald JL,Roskams AJ.Epigenetic regulation of nervous system development by DNA methylation and histone deacetylation.[J].2009,88(3).
[25]Christiane Riedinger,Jane A. Endicott,Stuart J. Kemp,etc.Analysis of Chemical Shift Changes Reveals the Binding Modes of Isoindolinone Inhibitors of the MDM2-p53 Interaction[J].2008,130(47).
[26]Ines Bruno,Elena Cini,Luigi Gomez-Paloma.Design and Synthesis of Cyclopeptide Analogues of the Potent Histone Deacetylase Inhibitor FR235222[J].2007,2(10).
[27]Watanabe S.,Takahashi Y.,Hiratsuka R.,etc.Caged compounds with a steroid skeleton: synthesis, liposome-formation and photolysis[J].2002,58(9).
[28]Smith EJ,Li Y,Shuja F,etc.Acetylation: a novel method for modulation of the immune response following trauma/hemorrhage and inflammatory second hit in animals and humans.[J].2008,144(2).
[29]Nishino N,Kato T,Watanabe LA,etc.Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand.[J].2004,14(10).
[30]Paul Helquist,Difei Wang,Olaf Wiest.Zinc Binding in HDAC Inhibitors: A DFT Study[J].2007,72(14).
[31]Perrino E,Sparatore A,Cappelletti G,etc.New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity.[J].2008,18(6).
[32]Marks PA,Breslow R.Dimethyl sulfoxide to vorinostat: Development of this histone deacetylase inhibitor as an anticancer drug[J].2007,25.
[33]Eikel D,Nau H,Ronndahl G,etc.Novel valproic acid derivatives with potent differentiation-inducing activity in myeloid leukemia cells.[J].2006,30(9).
[34]Methot JL,Hamblett CL,Mampreian DM,etc.SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).[J].2008,18(23).
[35]Blackwell L,Norris J,Suto CM,etc.The use of diversity profiling to characterize chemical modulators of the histone deacetylases.[J].2008,82(21).
[36]Jose A.Restituyo,Rebeccah J.Katzenberger,Jared R.Mays.Cyclic disulfides as functional mimics of the histone deacetylase inhibitor FK-228[J].2007,48(26).
[37]Spanjaard RA,Chen JS,Faller DV.Short-chain fatty acid inhibitors of histone deacetylases: promising anticancer therapeutics?[J].2003,3(3).
[38]Burkhardt C,Weinbrenner S,Dehmel F,etc.Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles[J].2008,51(13).
[39]Wang JF,Young LT,Shao L,etc.Mood stabilizing drug lithium increases expression of endoplasmic reticulum stress proteins in primary cultured rat cerebral cortical cells.[J].2006,78(12).