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

Table 3.

The structures of PROTAC molecules targeting apoptosis or angiogenesis in cancers. (red: POI ligand; yellow: E3 ligand)

Target PROTAC PROTAC structure Cancer Ref Target PROTAC PROTAC structure Cancer Ref
Bcl-xL DT2216 graphic file with name 12943_2021_1434_Figca_HTML.gif T-ALL [167] BCR-ABL DAS-6-2-2-6-CRBN graphic file with name 12943_2021_1434_Figcb_HTML.gif CML [171]
Bcl-xL XZ739 graphic file with name 12943_2021_1434_Figcc_HTML.gif T-ALL [184] BCR-ABL Azo-PROTAC-4C graphic file with name 12943_2021_1434_Figcd_HTML.gif CML [19]
Bcl-xL compound 8a graphic file with name 12943_2021_1434_Figce_HTML.gif TL [185] BCR-ABL SNIPER(ABL)-38 graphic file with name 12943_2021_1434_Figcf_HTML.gif CML [89]
Bcl-xL XZ424 graphic file with name 12943_2021_1434_Figcg_HTML.gif T-ALL [168] BCR-ABL compound 19 graphic file with name 12943_2021_1434_Figch_HTML.gif CML [186]
Bcl-xL PROTAC 6 graphic file with name 12943_2021_1434_Figci_HTML.gif AML [187] BCR-ABL GMB-475 graphic file with name 12943_2021_1434_Figcj_HTML.gif CML [172]
PARP1 compound 2 graphic file with name 12943_2021_1434_Figck_HTML.gif CRC [188] BCR-ABL GMB-805 graphic file with name 12943_2021_1434_Figcl_HTML.gif CML [189]
PARP1 iRucaparib-AP5 graphic file with name 12943_2021_1434_Figcm_HTML.gif CC, RCC, BC, PC [170] BCR-ABL SIAIS178 graphic file with name 12943_2021_1434_Figcn_HTML.gif CML [190]
PARP1 compound 3 graphic file with name 12943_2021_1434_Figco_HTML.gif TNBC [191] BCR-ABL BT1 graphic file with name 12943_2021_1434_Figcp_HTML.gif CML [192]
PARP1 SK-575 graphic file with name 12943_2021_1434_Figcq_HTML.gif BC, CRC, PC, PaC [169] AKT INY-03-041 graphic file with name 12943_2021_1434_Figcr_HTML.gif BC [173]
Bcl-2 C5 graphic file with name 12943_2021_1434_Figcs_HTML.gif CC, CML, NSCLC [174] eIF4E PROTAC 23a graphic file with name 12943_2021_1434_Figct_HTML.gif TNBC, CML [176]
Bcl-6 PROTAC 15 graphic file with name 12943_2021_1434_Figcu_HTML.gif DLBCL [193] HDAC1/2/3 PROTAC 4 graphic file with name 12943_2021_1434_Figcv_HTML.gif CRC [194]
c-IAP compound 6 graphic file with name 12943_2021_1434_Figcw_HTML.gif FS [175] HDAC1/2/3 XZ9002 graphic file with name 12943_2021_1434_Figcx_HTML.gif TNBC [195]
CK2 PROTAC 2 graphic file with name 12943_2021_1434_Figcy_HTML.gif TNBC, NSCLC [196] HDAC6 PROTAC 4 graphic file with name 12943_2021_1434_Figcz_HTML.gif OSCC, GB [197]
CRABP I/II compound 4b graphic file with name 12943_2021_1434_Figda_HTML.gif NB [8] HDAC6 degrader 12d graphic file with name 12943_2021_1434_Figdb_HTML.gif MM [198]
CRABP I/II compound 6 graphic file with name 12943_2021_1434_Figdc_HTML.gif FS [175] HDAC6 NP8 graphic file with name 12943_2021_1434_Figdd_HTML.gif MM, CC [199]
CRABP I/II β-NF-ATRA graphic file with name 12943_2021_1434_Figde_HTML.gif BC, NB [140] HDAC6 NH2 graphic file with name 12943_2021_1434_Figdf_HTML.gif MM, CC [200]
eEF2K compound 11l graphic file with name 12943_2021_1434_Figdg_HTML.gif BC [201] HDAC6 P1 graphic file with name 12943_2021_1434_Figdh_HTML.gif MM [202]
HDAC6 compound 3j graphic file with name 12943_2021_1434_Figdi_HTML.gif MM [203]

CBP/

p300

dCBP-1 graphic file with name 12943_2021_1434_Figdj_HTML.gif MM [181]
Mcl-1 dMCL1-2 graphic file with name 12943_2021_1434_Figdk_HTML.gif MM [177] RIPK2 PROTAC_RIPK2 graphic file with name 12943_2021_1434_Figdl_HTML.gif BC, AML [17]
Mcl-1 C3 graphic file with name 12943_2021_1434_Figdm_HTML.gif CC, CML, NSCLC [174] SGK3 SGK3-PROTAC1 graphic file with name 12943_2021_1434_Figdn_HTML.gif BC [204]
MDM2 MD-224 graphic file with name 12943_2021_1434_Figdo_HTML.gif ALL, AML [179] SirT2 PROTAC 12 graphic file with name 12943_2021_1434_Figdp_HTML.gif CC [182]
MDM2 degrader 32 graphic file with name 12943_2021_1434_Figdq_HTML.gif ALL [178] VEGFR2 PROTAC-5 graphic file with name 12943_2021_1434_Figdr_HTML.gif / [183]
PI3K compound D graphic file with name 12943_2021_1434_Figds_HTML.gif HCC [180]