Table 1. Exemplary Proteins Successfully Targeted for E3 Ligase Degradation.
| targeted protein | E3 ligase/subunit recruited | degrader | year |
|---|---|---|---|
| MetAP217 | βTRCP | PROTAC | 2001 |
| androgen receptor34 | βTRCP | PROTAC | 2003 |
| estrogen receptor34 | βTRCP | PROTAC | 2003 |
| androgen receptor18 | VHL | PROTAC | 2004 |
| aryl hydrocarbon receptor35 | VHL | PROTAC | 2007 |
| androgen receptor19 | MDM2 | PROTAC | 2008 |
| estrogen receptor36 | VHL | PROTAC | 2008 |
| FRS2α37 | VHL | PROTAC | 2008 |
| PI3K37 | VHL | PROTAC | 2008 |
| CRABPI and CRABPII23 | cIAP | PROTAC | 2010 |
| RAR23 | cIAP | PROTAC | 2010 |
| androgen receptor38 | cIAP | SNIPER | 2011 |
| estrogen receptor38 | cIAP | SNIPER | 2011 |
| TACC339 | cIAP | SNIPER | 2014 |
| BET (BRD2, BRD3, and BRD4)22,40 | VHL | PROTAC | 2015 |
| BET (BRD2, BRD3, and BRD4)41,42 | CRBN | PROTAC | 2015 |
| ERRα21 | VHL | PROTAC | 2015 |
| FKBP1241 | CRBN | molecular glue, PROTAC | 2015 |
| RIPK221 | VHL | PROTAC | 2015 |
| AKT43 | VHL | PROTAC | 2016 |
| BCR–ABL44 | VHL | PROTAC | 2016 |
| BCR–ABL44 | CRBN | PROTAC | 2016 |
| tau45 | VHL | PROTAC | 2016 |
| RBM3946 | DCAF15 | molecular glue | 2017 |
| RBM2347,48 | DCAF15 | molecular glue | 2019 |