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. 2022 Apr 11;21:99. doi: 10.1186/s12943-021-01434-3

Table 2.

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

Target PROTAC PROTAC structure Cancer Ref Target PROTAC PROTAC structure Cancer Ref
BRD4 ARV-825 graphic file with name 12943_2021_1434_Figa_HTML.gif BL [39] BRD4 SNIPER(BRD4)-1 graphic file with name 12943_2021_1434_Figb_HTML.gif BC [89]
BRD4 dBET1 graphic file with name 12943_2021_1434_Figc_HTML.gif AML [12] BRD4 A1874 graphic file with name 12943_2021_1434_Figd_HTML.gif CRC, M, BL, et al. [90]
BRD4 MZ1 graphic file with name 12943_2021_1434_Fige_HTML.gif CC [33, 91] BRD4 CLIPTAC-BRD4 graphic file with name 12943_2021_1434_Figf_HTML.gif CC, M, CRC [26]
BRD4 dBET6 graphic file with name 12943_2021_1434_Figg_HTML.gif T-ALL [92] BRD4

opto-dBE

T1

graphic file with name 12943_2021_1434_Figh_HTML.gif MM, PC, ALCL, et al. [22]
BRD4 ZXH-3-26 graphic file with name 12943_2021_1434_Figi_HTML.gif MM [93] BRD4 PROTAC4 graphic file with name 12943_2021_1434_Figj_HTML.gif BC, PC [23]
BRD4 ARV-771 graphic file with name 12943_2021_1434_Figk_HTML.gif PC [76] BRD4 pc-PROTAC1 graphic file with name 12943_2021_1434_Figl_HTML.gif BL, HCC [25]
BRD4 macroPROTAC-1 graphic file with name 12943_2021_1434_Figm_HTML.gif PC, AML [94] BRD4 PHOTAC-I-3 graphic file with name 12943_2021_1434_Fign_HTML.gif ALL [21]
BRD4 BETd-246 graphic file with name 12943_2021_1434_Figo_HTML.gif TNBC [95] BRD4 photoPROTAC-1 graphic file with name 12943_2021_1434_Figp_HTML.gif BL [20]
BRD4 BETd-260 graphic file with name 12943_2021_1434_Figq_HTML.gif AML, ALL [96] BRD4 PROTAC3 graphic file with name 12943_2021_1434_Figr_HTML.gif CC [24]
BRD4 KB02-JQ1 graphic file with name 12943_2021_1434_Figs_HTML.gif / [97] EGFR compound 1 graphic file with name 12943_2021_1434_Figt_HTML.gif OC, CC [79]
BRD4 XH2 graphic file with name 12943_2021_1434_Figu_HTML.gif BC [98] EGFR compound 14o graphic file with name 12943_2021_1434_Figv_HTML.gif NSCLC [99]
BRD4 DP1 graphic file with name 12943_2021_1434_Figw_HTML.gif DLBCL [100] EGFR compound P3 graphic file with name 12943_2021_1434_Figx_HTML.gif LC [101]
CDK4/6 BSJ-03-123 graphic file with name 12943_2021_1434_Figy_HTML.gif AML [102] EGFR MS154 graphic file with name 12943_2021_1434_Figz_HTML.gif LC [103]
CDK4/6 pal-pom graphic file with name 12943_2021_1434_Figaa_HTML.gif TNBC [104] EGFR DDC-01-163 graphic file with name 12943_2021_1434_Figab_HTML.gif LC [80]
CDK4/6 BSJ-02-162 graphic file with name 12943_2021_1434_Figac_HTML.gif MCL [77] AURORA-A JB170 graphic file with name 12943_2021_1434_Figad_HTML.gif AML, OS, NB, HCC [81]
CDK4/6 BSJ-04-132 graphic file with name 12943_2021_1434_Figae_HTML.gif T-ALL [77] Raf P4B graphic file with name 12943_2021_1434_Figaf_HTML.gif M, CRC [60]
CDK4/6 YX-2-107 graphic file with name 12943_2021_1434_Figag_HTML.gif ALL [78] AR PROTAC 14 graphic file with name 12943_2021_1434_Figah_HTML.gif CC [7]
CDK4/6 compound 11 graphic file with name 12943_2021_1434_Figai_HTML.gif M [105] AR ARCC-4 graphic file with name 12943_2021_1434_Figaj_HTML.gif PC [106]
CDK4/6 PROTAC 34 graphic file with name 12943_2021_1434_Figak_HTML.gif ALL, AML, MM, TNBC [107] AR TD-802 graphic file with name 12943_2021_1434_Figal_HTML.gif PC [108]
AR MTX-23 graphic file with name 12943_2021_1434_Figam_HTML.gif PC [109] BRD7/9 ACBI1 graphic file with name 12943_2021_1434_Figan_HTML.gif AML, M, NSCLC [83]
AR ARD-69 graphic file with name 12943_2021_1434_Figao_HTML.gif PC [110] CDK2/5 TMX-2172 graphic file with name 12943_2021_1434_Figap_HTML.gif OC [84]
AR SNIPER(AR)-51 graphic file with name 12943_2021_1434_Figaq_HTML.gif PC [111] CDK8 JH-XI-10-02 graphic file with name 12943_2021_1434_Figar_HTML.gif T-ALL [112]
ALK MS4077 graphic file with name 12943_2021_1434_Figas_HTML.gif NSCLC, ALCL [113] CDK9 PROTAC 3 graphic file with name 12943_2021_1434_Figat_HTML.gif CRC [114]
ALK TL13–12 graphic file with name 12943_2021_1434_Figau_HTML.gif ALCL, NB, NSCLC [52] CDK9 THAL-SNS-032 graphic file with name 12943_2021_1434_Figav_HTML.gif T-ALL [38]
ALK opto-dALK graphic file with name 12943_2021_1434_Figaw_HTML.gif NSCLC, ALCL [22] CDK9 B03 graphic file with name 12943_2021_1434_Figax_HTML.gif AML [115]
ALK SIAIS117 graphic file with name 12943_2021_1434_Figay_HTML.gif NSCLC, ALCL [116] CDK9 compound F3 graphic file with name 12943_2021_1434_Figaz_HTML.gif PC [117]
BLK PROTAC 7 graphic file with name 12943_2021_1434_Figba_HTML.gif CML [118] Cdc20 CP5V graphic file with name 12943_2021_1434_Figbb_HTML.gif BC [119]
BRD7/9 dBRD9 graphic file with name 12943_2021_1434_Figbc_HTML.gif AML [82] c-Met PROTAC 7 graphic file with name 12943_2021_1434_Figbd_HTML.gif TNBC, GC [79]
BRD7/9 VZ185 graphic file with name 12943_2021_1434_Figbe_HTML.gif MRT [120] CREPT PRTC graphic file with name 12943_2021_1434_Figbf_HTML.gif PaC [121]
CYP1B1 compound 6C graphic file with name 12943_2021_1434_Figbg_HTML.gif PC [122] MEK1/2 MS432 graphic file with name 12943_2021_1434_Figbh_HTML.gif CRC, M [86]
DHODH probe 10 graphic file with name 12943_2021_1434_Figbi_HTML.gif PaC [123] Ras LC-2 graphic file with name 12943_2021_1434_Figbj_HTML.gif NSCLC, PaC [87]
ER ERD-308 graphic file with name 12943_2021_1434_Figbk_HTML.gif BC [124] GSPT1 CC-885 graphic file with name 12943_2021_1434_Figbl_HTML.gif AML [125]
ER compound I-6 graphic file with name 12943_2021_1434_Figbm_HTML.gif BC [126] PLK1 HBL-4 graphic file with name 12943_2021_1434_Figbn_HTML.gif AML [127]
ER TD-PROTAC graphic file with name 12943_2021_1434_Figbo_HTML.gif BC [128] SLC9A1 d9A-2 graphic file with name 12943_2021_1434_Figbp_HTML.gif CML [129]
ER SNIPER(ER)-87 graphic file with name 12943_2021_1434_Figbq_HTML.gif BC [89] TACC3 SNIPER(TACC3)-1 graphic file with name 12943_2021_1434_Figbr_HTML.gif FS, OS, CRC [130]
ERK1/2 ERK-CLIPTAC graphic file with name 12943_2021_1434_Figbs_HTML.gif CC, M, CRC [26] TRIM 24 dTRIM24 graphic file with name 12943_2021_1434_Figbt_HTML.gif AML [131]
FLT-3 FLT-3 PROTAC graphic file with name 12943_2021_1434_Figbu_HTML.gif AML [132] TRKA/C CG416 graphic file with name 12943_2021_1434_Figbv_HTML.gif CRC, AML [133]
HER2 PROTAC 1 graphic file with name 12943_2021_1434_Figbw_HTML.gif OC, BC [79] Wee1 ZNL-02-096 graphic file with name 12943_2021_1434_Figbx_HTML.gif OC, T-ALL [88]
MEK1/2 compound 3 graphic file with name 12943_2021_1434_Figby_HTML.gif M [85] α1A-AR α1A-AR graphic file with name 12943_2021_1434_Figbz_HTML.gif PC [134]