Skip to main content

Table 3 Comparison of strategies that selectively target proteins for degradation

From: Epigenetic modifications of histones in cancer

MethodRate of action (t1/2)Customized or universal ligandReversibilityGenetic manipulation requiredReal-time visualizationToxicity in mouse modelDegradation mediator
Thalidomide-targeted degradation< 1 hCustomizedYesNoNoNoCRL4aCRBN RING E3 ubiquitin ligase complex
PROTACs< 2 hCustomizedYesNoNoNoCRL4aCRBN and CRL2VHL E3 ligase
HaloPROTACs4–8 h/1 hUniversal HaloPROTAC3/bestatin 1bYesYes, HaloTag7 / HaloTag fusionYesN/ACRL2VHL E3 ligase and IAP E3 ligase
SMAShN/AUniversal asunaprevirYesYes, self-cleaving NS3pro-NS4A fusionN/ANoNS3 protease from hepatitis C virus
dTAG< 1 hUniversal dTAG ligandYesYes, FKBP12 (F36 V) fusionNoNoCRBN-dependent E3 ligase
AID< 1 hUniversal auxin (IAA)YesYes, AID tag fusion and Tir1 F-box protein expressionYesYesCRL1Tir1