Histone Deacetylase Inhibitors An Attractive Strategy for Cancer Therapy

Histone Deacetylase Inhibitors An Attractive Strategy for Cancer Therapy

ID:40080901

大小:765.90 KB

页数:29页

时间:2019-07-20

Histone Deacetylase Inhibitors An Attractive Strategy for Cancer Therapy_第1页
Histone Deacetylase Inhibitors An Attractive Strategy for Cancer Therapy_第2页
Histone Deacetylase Inhibitors An Attractive Strategy for Cancer Therapy_第3页
Histone Deacetylase Inhibitors An Attractive Strategy for Cancer Therapy_第4页
Histone Deacetylase Inhibitors An Attractive Strategy for Cancer Therapy_第5页
资源描述:

《Histone Deacetylase Inhibitors An Attractive Strategy for Cancer Therapy》由会员上传分享,免费在线阅读,更多相关内容在学术论文-天天文库

1、SendOrdersofReprintsatreprints@benthamscience.net1858CurrentMedicinalChemistry,2013,20,1858-1886HistoneDeacetylaseInhibitors:AnAttractiveStrategyforCancerTherapy*JiyangLi,GuangqiangLiandWenqingXuInstituteofRadiationMedicine,ChineseAcademyofMedicalScience

2、s&PekingUnionMedicalCollege,Tianjin,PeopleRepublicofChinaAbstract:HistonedeacetylasesareabletocatalyzethehydrolysisofN-acetyllysineresiduesofhistoneswhichpackagechromosomalDNA.Thereforetheyplayanimportantroleinmediatinggeneexpressionandcellproliferation.

3、HDACin-hibitorshavenotonlyshownpromiseasantiparasitic,antineurodegenerative,antirheumatologicagentsandimmunosup-pressant,butaspotentanticanceragentsbyinducingcellcyclearrest,differentiationandapoptosis.Thisreviewhighlightsrecentdevelopmentindesign,synthe

4、sisandbiologicalevaluationofHDACinhibitorsforcancertherapy.Keywords:Antitumordrugs,cancertherapy,cyclicpeptide,drugdiscovery,epigeneticregulation,histonedeacetylase,hdacisoforms,histonedeacetylaseinhibitors,hybridcompounds,multi-targetedinhibitor.INTRODU

5、CTIONNH+Nucleosome,whichisthebasicunitofchromatin,com-C3HATCNHOCHOCHprisesaDNAwrappedaroundacorehistoneoctamer,whichiscomposedofaH3–H4tetramerandtwoH2A-H2Bdim-NHHDACNHOmers[1].Thus,DNAiscompactedinasmallersizewhichisrequiredforbeingstoredineukaryoticnucl

6、eus.Butsome-times,thehighdegreeofcompactionwouldbeunnecessary.Forexample,whenDNAreplicationandgenetranscriptionchromatincompactedDNAunfoldedbegan,DNAmustbereleasedandbeloose.Accordingly,aquestionarised.Howwouldthesetwocontraryprocesseshappen?HATs(histone

7、acetyltransferases)andHDACs(his-tonedeacetylases)areonepairofanswers[2].genesilencetranscriptionalactivationInhistoneprotein,themodificationofterminal-aminotranscriptionalinhibitionreplicationactivatedgroupofspecificlysineresidueswasveryimportantfortran

8、-proliferationstimulatedgeneexpressionscriptionalprocesses[3].As(Fig.1)displayed,whenarrowturnedrightwhichmeantlysineresiduewasacetylatedbyFig.(1).TheProcessofHistoneAcetylationandDeacetylation.HATs,theinteractionbetweenhi

当前文档最多预览五页,下载文档查看全文

此文档下载收益归作者所有

当前文档最多预览五页,下载文档查看全文
温馨提示:
1. 部分包含数学公式或PPT动画的文件,查看预览时可能会显示错乱或异常,文件下载后无此问题,请放心下载。
2. 本文档由用户上传,版权归属用户,天天文库负责整理代发布。如果您对本文档版权有争议请及时联系客服。
3. 下载前请仔细阅读文档内容,确认文档内容符合您的需求后进行下载,若出现内容与标题不符可向本站投诉处理。
4. 下载文档时可能由于网络波动等原因无法下载或下载错误,付费完成后未能成功下载的用户请联系客服处理。