Summary of small molecules which target the polyamine synthesis and downstream hypusination pathways

MoleculeaTargetbEffect(s) on polyamine levelsReference(s)
DFMOODC1Inhibition of putrescine synthesis, reduced levels of all polyamines 87
MGBGSAMDCInhibition of spermidine and spermine synthesis 88
SAM486aSAMDCInhibition of spermidine and spermine synthesis 89
MDL-72527PAOXInhibition of polyamine interconversion 90
DENSpmSAT1Acetylation of spermidine and spermine, interconversion and removal of polyamines 91
GC7DHPSReduction in eIF5A-deoxyhypusine and -hypusine levels 79
CPXDOHHReduction in eIF5A-hypusine levels 92, 93
DEFDOHHReduction in eIF5A-hypusine levels 92
  • a DFMO, difluoromethylornithine; MGBG, methylglyoxal (bis)guanylhydrazone; SAM486a, sardomozide; DENSpm, N1,N11-diethylnorspermine; GC7, N1-guanyl-1,7-diamine-heptane; CPX, ciclopirox; DEF, deferiprone.

  • b ODC1, ornithine decarboxylase 1; SAMDC, S-adenosylmethionine decarboxylase; PAOX, polyamine oxidase; SAT1, spermidine/spermine acetyltransferase 1; DHPS, deoxyhypusine synthase; DOHH, deoxyhypusine hydroxylase.