Sun X, Gao H, Yang Y, He M, Wu Y, Song Y, et al. PROTACs: great opportunities for academia and industry. Signal Transduct Target Ther. 2019;4:64.

Article  PubMed  PubMed Central  Google Scholar 

Toure M, Crews CM. Small-molecule PROTACS: new approaches to protein degradation. Angew Chem Int Ed Engl. 2016;55:1966–73.

Article  CAS  PubMed  Google Scholar 

Liu J, Ma J, Liu Y, Xia J, Li Y, Wang ZP, et al. PROTACs: a novel strategy for cancer therapy. Semin Cancer Biol. 2020;67:171–9.

Article  CAS  PubMed  Google Scholar 

Lai AC, Crews CM. Induced protein degradation: an emerging drug discovery paradigm. Nat Rev Drug Discov. 2017;16:101–14.

Article  CAS  PubMed  Google Scholar 

Li X, Song Y. Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy. J Hematol Oncol. 2020;13:50.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Burslem GM, Crews CM. Proteolysis-targeting chimeras as therapeutics and tools for biological discovery. Cell. 2020;181:102–14.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Luh LM, Scheib U, Juenemann K, Wortmann L, Brands M, Cromm PM. Prey for the proteasome: targeted protein degradation-a medicinal chemist’s perspective. Angew Chem Int Ed Engl. 2020;59:15448–66.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Popovic D, Vucic D, Dikic I. Ubiquitination in disease pathogenesis and treatment. Nat Med. 2014;20:1242–53.

Article  CAS  PubMed  Google Scholar 

Chamberlain PP, Hamann LG. Development of targeted protein degradation therapeutics. Nat Chem Biol. 2019;15:937–44.

Article  CAS  PubMed  Google Scholar 

Dale B, Cheng M, Park KS, Kaniskan HU, Xiong Y, Jin J. Advancing targeted protein degradation for cancer therapy. Nat Rev Cancer. 2021;21:638–54.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Noblejas-Lopez MDM, Nieto-Jimenez C, Burgos M, Gomez-Juarez M, Montero JC, Esparis-Ogando A, et al. Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer. J Exp Clin Cancer Res. 2019;38:383.

Article  PubMed  PubMed Central  Google Scholar 

Lu J, Qian Y, Altieri M, Dong H, Wang J, Raina K, et al. Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4. Chem Biol. 2015;22:755–63.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Minko T. Nanoformulation of BRD4-degrading PROTAC: improving druggability to target the ‘Undruggable’ MYC in pancreatic cancer. Trends Pharmacol Sci. 2020;41:684–6.

Article  CAS  PubMed  Google Scholar 

Schapira M, Calabrese MF, Bullock AN, Crews CM. Targeted protein degradation: expanding the toolbox. Nat Rev Drug Discov. 2019;18:949–63.

Article  CAS  PubMed  Google Scholar 

Ocana A, Pandiella A. Proteolysis targeting chimeras (PROTACs) in cancer therapy. J Exp Clin Cancer Res. 2020;39:189.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Moreau K, Coen M, Zhang AX, Pachl F, Castaldi MP, Dahl G, et al. Proteolysis-targeting chimeras in drug development: a safety perspective. Br J Pharmacol. 2020;177:1709–18.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Chen Y, Tandon I, Heelan W, Wang Y, Tang W, Hu Q. Proteolysis-targeting chimera (PROTAC) delivery system: advancing protein degraders towards clinical translation. Chem Soc Rev. 2022;51:5330–50.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Yokoo H, Naito M, Demizu Y. Investigating the cell permeability of proteolysis-targeting chimeras (PROTACs). Expert Opin Drug Discov. 2023;18:357–61.

Article  PubMed  Google Scholar 

Li J, Chen X, Lu A, Liang C. Targeted protein degradation in cancers: orthodox PROTACs and beyond. Innovation. 2023;4:100413.

CAS  PubMed  PubMed Central  Google Scholar 

Gao J, Yang L, Lei S, Zhou F, Nie H, Peng B, et al. Stimuli-activatable PROTACs for precise protein degradation and cancer therapy. Sci Bull. 2023;68:1069–85.

Article  CAS  Google Scholar 

Liu J, Chen H, Ma L, He Z, Wang D, Liu Y, et al. Light-induced control of protein destruction by opto-PROTAC. Sci Adv. 2020;6:eaay5154.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Reynders M, Matsuura BS, Berouti M, Simoneschi D, Marzio A, Pagano M, et al. PHOTACs enable optical control of protein degradation. Sci Adv. 2020;6:eaay5064.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Liu J, Chen H, Liu Y, Shen Y, Meng F, Kaniskan HU, et al. Cancer selective target degradation by folate-caged PROTACs. J Am Chem Soc. 2021;143:7380–7.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Dragovich PS, Pillow TH, Blake RA, Sadowsky JD, Adaligil E, Adhikari P, et al. Antibody-mediated delivery of chimeric BRD4 degraders. part 1: exploration of antibody linker, payload loading, and payload molecular properties. J Med Chem. 2021;64:2534–75.

Article  CAS  PubMed  Google Scholar 

Maneiro MA, Forte N, Shchepinova MM, Kounde CS, Chudasama V, Baker JR, et al. Antibody-PROTAC conjugates enable HER2-dependent targeted protein degradation of BRD4. ACS Chem Biol. 2020;15:1306–12.

Article  CAS  PubMed  PubMed Central  Google Scholar 

He S, Gao F, Ma J, Ma H, Dong G, Sheng C. Aptamer-PROTAC conjugates (APCs) for tumor-specific targeting in breast cancer. Angew Chem Int Ed Engl. 2021;60:23299–305.

Article  CAS  PubMed  Google Scholar 

Zhang C, Zeng Z, Cui D, He S, Jiang Y, Li J, et al. Semiconducting polymer nano-PROTACs for activatable photo-immunometabolic cancer therapy. Nat Commun. 2021;12:2934.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Zhang C, He S, Zeng Z, Cheng P, Pu K. Smart nano-PROTACs reprogram tumor microenvironment for activatable photo-metabolic cancer immunotherapy. Angew Chem Int Ed Engl. 2022;61:e202114957.

Article  CAS  PubMed  Google Scholar 

Gao J, Hou B, Zhu Q, Yang L, Jiang X, Zou Z, et al. Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy. Nat Commun. 2022;13:4318.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Yang C, Yang Y, Li Y, Ni Q, Li J. Radiotherapy-triggered proteolysis targeting chimera prodrug activation in tumors. J Am Chem Soc. 2023;145:385–91.

Article  CAS  PubMed  Google Scholar 

Hanahan D. Hallmarks of cancer: new dimensions. Cancer Discov. 2022;12:31–46.

Article  CAS  PubMed  Google Scholar 

Narayan RS, Molenaar P, Teng J, Cornelissen FMG, Roelofs I, Menezes R, et al. A cancer drug atlas enables synergistic targeting of independent drug vulnerabilities. Nat Commun. 2020;11:2935.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Jin H, Wang L, Bernards R. Rational combinations of targeted cancer therapies: background, advances and challenges. Nat Rev Drug Discov. 2023;22:213–34.

Article  CAS  PubMed  Google Scholar 

Vasan N, Baselga J, Hyman DM. A view on drug resistance in cancer. Nature. 2019;575:299–309.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Khan S, Zhang X, Lv D, Zhang Q, He Y, Zhang P, et al. A selective BCL-X(L) PROTAC degrader achieves safe and potent antitumor activity. Nat Med. 2019;25:1938–47.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Flanagan JJ, Qian Y, Gough SM, Andreoli M, Bookbinder M, Cadelina G, et al. Abstract P5-04-18: ARV-471, an oral estrogen receptor PROTAC degrader for breast cancer. Cancer Res. 2021;81:44.