Description
JQ-1isatriazolothienodiazepinecompoundthatinhibitstheBETbromodomain(BRD)familyofproteins.Althoughitisadiazepine-likecompound,JQ-1exhibitsnosedativeoranxiolyticefficacy.JQ-1wasinitiallyindevelopmentasanon-hormonalmalecontraceptive,inhibitingbromodomaintestis-specificproteinBRDTandchromatinremodelingduringspermatogenesis,thereforepreventingspermproduction.ThiscompoundalsoactivateslatentHIV-1invitroandinhibitsTcellproliferationthroughdownregulationofTcellactivationsignalsCD3,CD28,andCXCR4;JQ-1iscurrentlyusedasanexperimentaltoolforexaminingmechanismsofHIV-1latency.Additionally,JQ-1exhibitsanticancerchemotherapeuticactivityinvitroandinvivo;throughitsinhibitionofBRD4,JQ-1suppressesMycexpression,IL-7Rexpression,andreducesJAK/STATphosphorylation,inducingcellcyclearrestandalteringsurvivalinavarietyofcelllines.BIOLOGicalbromodomainbindingactivitycomesprimarilyfrom(+)-JQ-1;the(-)-JQ-1stereoisomerdoesnotbindBETbromodomains.
References
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