Table 2 The summary and comparison of PROTACs targeting EGFR

From: PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

No.

PROTAC

Warhead

E3 ligase

1

MS39(22)

Gefitinib

VHL

2

MS154(23)

Gefitinib

CRBN

3

24

Osimertinib

CRBN

4

25

Gefitinib

VHL

5

26

Pyrido[3,4-d] pyrimidine moiety

CRBN

6

27

Pyrido[3,4-d] pyrimidine moiety

VHL

7

P3(28)

Purine-containing derivative

VHL

8

29

XTF-262

VHL

9

SIAI125(30)

Canertinib

CRBN

10

SIAI126(31)

Canertinib

CRBN