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Table 2 The structures of PROTAC molecules targeting cell proliferation in cancers. (red: POI ligand; yellow: E3 ligand)

From: Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Target

PROTAC

PROTAC structure

Cancer

Ref

Target

PROTAC

PROTAC structure

Cancer

Ref

BRD4

ARV-825

BL

[39]

BRD4

SNIPER(BRD4)-1

BC

[89]

BRD4

dBET1

AML

[12]

BRD4

A1874

CRC, M, BL, et al.

[90]

BRD4

MZ1

CC

[33, 91]

BRD4

CLIPTAC-BRD4

CC, M, CRC

[26]

BRD4

dBET6

T-ALL

[92]

BRD4

opto-dBE

T1

MM, PC, ALCL, et al.

[22]

BRD4

ZXH-3-26

MM

[93]

BRD4

PROTAC4

BC, PC

[23]

BRD4

ARV-771

PC

[76]

BRD4

pc-PROTAC1

BL, HCC

[25]

BRD4

macroPROTAC-1

PC, AML

[94]

BRD4

PHOTAC-I-3

ALL

[21]

BRD4

BETd-246

TNBC

[95]

BRD4

photoPROTAC-1

BL

[20]

BRD4

BETd-260

AML, ALL

[96]

BRD4

PROTAC3

CC

[24]

BRD4

KB02-JQ1

/

[97]

EGFR

compound 1

OC, CC

[79]

BRD4

XH2

BC

[98]

EGFR

compound 14o

NSCLC

[99]

BRD4

DP1

DLBCL

[100]

EGFR

compound P3

LC

[101]

CDK4/6

BSJ-03-123

AML

[102]

EGFR

MS154

LC

[103]

CDK4/6

pal-pom

TNBC

[104]

EGFR

DDC-01-163

LC

[80]

CDK4/6

BSJ-02-162

MCL

[77]

AURORA-A

JB170

AML, OS, NB, HCC

[81]

CDK4/6

BSJ-04-132

T-ALL

[77]

Raf

P4B

M, CRC

[60]

CDK4/6

YX-2-107

ALL

[78]

AR

PROTAC 14

CC

[7]

CDK4/6

compound 11

M

[105]

AR

ARCC-4

PC

[106]

CDK4/6

PROTAC 34

ALL, AML, MM, TNBC

[107]

AR

TD-802

PC

[108]

AR

MTX-23

PC

[109]

BRD7/9

ACBI1

AML, M, NSCLC

[83]

AR

ARD-69

PC

[110]

CDK2/5

TMX-2172

OC

[84]

AR

SNIPER(AR)-51

PC

[111]

CDK8

JH-XI-10-02

T-ALL

[112]

ALK

MS4077

NSCLC, ALCL

[113]

CDK9

PROTAC 3

CRC

[114]

ALK

TL13–12

ALCL, NB, NSCLC

[52]

CDK9

THAL-SNS-032

T-ALL

[38]

ALK

opto-dALK

NSCLC, ALCL

[22]

CDK9

B03

AML

[115]

ALK

SIAIS117

NSCLC, ALCL

[116]

CDK9

compound F3

PC

[117]

BLK

PROTAC 7

CML

[118]

Cdc20

CP5V

BC

[119]

BRD7/9

dBRD9

AML

[82]

c-Met

PROTAC 7

TNBC, GC

[79]

BRD7/9

VZ185

MRT

[120]

CREPT

PRTC

PaC

[121]

CYP1B1

compound 6C

PC

[122]

MEK1/2

MS432

CRC, M

[86]

DHODH

probe 10

PaC

[123]

Ras

LC-2

NSCLC, PaC

[87]

ER

ERD-308

BC

[124]

GSPT1

CC-885

AML

[125]

ER

compound I-6

BC

[126]

PLK1

HBL-4

AML

[127]

ER

TD-PROTAC

BC

[128]

SLC9A1

d9A-2

CML

[129]

ER

SNIPER(ER)-87

BC

[89]

TACC3

SNIPER(TACC3)-1

FS, OS, CRC

[130]

ERK1/2

ERK-CLIPTAC

CC, M, CRC

[26]

TRIM 24

dTRIM24

AML

[131]

FLT-3

FLT-3 PROTAC

AML

[132]

TRKA/C

CG416

CRC, AML

[133]

HER2

PROTAC 1

OC, BC

[79]

Wee1

ZNL-02-096

OC, T-ALL

[88]

MEK1/2

compound 3

M

[85]

α1A-AR

α1A-AR

PC

[134]