Table 1.
Proteins Successfully Targeted for Degradation
| Target | Mechanism | Year |
|---|---|---|
| Akt | VHL (polypeptidic)129 | 2016 |
| Androgen Receptor | β-TrCP (polypeptidic)122 | 2003 |
| VHL (polypeptidic)125 | 2004 | |
| MDM2 (nutlin-3)134 | 2008 | |
| cIAP (small-molecule)145 | 2011 | |
| HyT (adamantane)116 | 2015 | |
| Aryl Hydrocarbon Receptor | VHL (polypeptidic)214 | 2007 |
| BCR-ABL | VHL (small-molecule)71 | 2016 |
| CRBN (small-molecule)71 | 2016 | |
| BET (BRD2/3/4) | VHL (small-molecule)162,163 | 2015 |
| CRBN (small-molecule)72,160 | 2015 | |
| CRABP-I and -II | cIAP (small-molecule)138 | 2010 |
| DHFR | HyT (Arg-Boc3)107 | 2012 |
| ERRα | VHL (small-molecule)70 | 2015 |
| ErbB3 | HyT (adamantane)114 | 2014 |
| Estrogen Receptor | Fulvestrant78 | 1991 |
| β-TrCP (polypeptidic)122 | 2003 | |
| VHL (polypeptidic)127 | 2008 | |
| cIAP (small-molecule)145 | 2011 | |
| FKBP12 | CRBN (small-molecule)72 | 2015 |
| FRS2α | VHL (polypeptidic)131 | 2013 |
| GST | HyT (Arg-Boc3)107 | 2012 |
| HaloTag | HyT (adamantane)110 | 2011 |
| VHL (small-molecule)177 | 2015 | |
| cIAP (small-molecule)215 | 2015 | |
| MetAP-2 | β-TrCP (polypeptidic)118 | 2001 |
| PI3K | VHL (polypeptidic)131 | 2013 |
| RAR | cIAP (small-molecule) 138 | 2010 |
| RIPK2 | VHL (small-molecule)70 | 2015 |
| TACC3 | cIAP (small-molecule)146 | 2014 |
| Tau | VHL (polypeptidic)130 | 2016 |
BCR-ABL, breakpoint cluster region-Abelson tyrosine kinase fusion protein; BET, bromodomain and extra-terminal; BRD4, bromodomain containing protein 4; CRABP, Cellular retinoic acid-binding protein; DHFR, dihydrofolate reductase; ErbB3, erythroblastosis oncogene B3; ERRα, estrogen-related receptor α; FKBP12, FK506 binding protein 12; FRS2α, fibroblast growth factor receptor substrate 2α; GST, glutathione-S-transferase; MetAP-2, methionine aminopeptidase-2; PI3K, phosphatidylinositol-3-kinase; RAR, retinoic acid receptor; RIPK2, receptor-interacting serine-threonine kinase 2; TACC3, transforming, acidic coiled-coil containing protein 3.