Light-Induced Protein Degradation with Photocaged PROTACs

Selective inhibition of BET bromodomains

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Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation

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Photoremovable Protecting Groups in Chemistry and Biology: Reaction Mechanisms and Efficacy

Petr Klán, A., Šolomek, T., Bochet, C. G., Blanc, A., Givens, R. S., Rubina, M. Y., Popik, V. V., Kostikov, A. P., & Wirz, J. (2012) · Chemical Reviews · doi:10.1021/cr300177k · Cited by 1,846 · see citing works

Phthalimide conjugation as a strategy for in vivo target protein degradation

Winter, G. E., Buckley, D. L., Paulk, J., Roberts, J. M., Souza, A., Dhe-Paganon, S., & Bradner, J. E. (2015) · Science · doi:10.1126/science.aab1433 · Cited by 1,760 · see citing works

Suppression of inflammation by a synthetic histone mimic

Nicodeme, E., Jeffrey, K. L., Schaefer, U., Beinke, S., Dewell, S., Chung, C.-W., Chandwani, R., Marazzi, I., Wilson, P., Coste, H., et al. (2010) · Nature · doi:10.1038/nature09589 · Cited by 1,563 · see citing works

Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

Fischer, E. S., Böhm, K., Lydeard, J. R., Yang, H., Stadler, M. B., Cavadini, S., Nagel, J., Serluca, F., Acker, V., Lingaraju, G. M., et al. (2014) · Nature · doi:10.1038/nature13527 · Cited by 1,141 · see citing works

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Lu, J., Qian, Y., Altieri, M., Dong, H., Wang, J., Raina, K., Hines, J., Winkler, J. D., Crew, A. P., Coleman, K., et al. (2015) · Chemistry & Biology · doi:10.1016/j.chembiol.2015.05.009 · Cited by 1,140 · see citing works

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

Zengerle, M., Chan, K.-H., & Ciulli, A. (2015) · ACS Chemical Biology · doi:10.1021/acschembio.5b00216 · Cited by 1,056 · see citing works

Headwaters of the zebrafish — emergence of a new model vertebrate

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A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

Matyskiela, M. E., Lu, G., Ito, T., Pagarigan, B., Lu, C.-C., Miller, K., Fang, W., Wang, N.-Y., Nguyen, D., Houston, J., et al. (2016) · Nature · doi:10.1038/nature18611 · Cited by 701 · see citing works

Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase

Pan, Z., Scheerens, H., Li, S., Schultz, B. E., Sprengeler, P. A., Burrill, L. C., Mendonca, R. V., Sweeney, M. D., Scott, K. C. K., Grothaus, P. G., et al. (2006) · ChemMedChem · doi:10.1002/cmdc.200600221 · Cited by 690 · see citing works

Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

Petzold, G., Fischer, E. S., & Thomä, N. H. (2016) · Nature · doi:10.1038/nature16979 · Cited by 620 · see citing works

Zebrafish: An Emerging Model System for Human Disease and Drug Discovery

Kari, G., Rodeck, U., & Dicker, A. P. (2007) · Clinical Pharmacology & Therapeutics · doi:10.1038/sj.clpt.6100223 · Cited by 467 · see citing works

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader

Huang, H.-T., Dobrovolsky, D., Paulk, J., Yang, G., Weisberg, E. L., Doctor, Z. M., Buckley, D. L., Cho, J.-H., Ko, E., Jang, J., et al. (2018) · Cell Chemical Biology · doi:10.1016/j.chembiol.2017.10.005 · Cited by 437 · see citing works

Drugging the undruggables: exploring the ubiquitin system for drug development

Huang, X., & Dixit, V. M. (2016) · Cell Research · doi:10.1038/cr.2016.31 · Cited by 427 · see citing works

Delineating the role of cooperativity in the design of potent PROTACs for BTK

Zorba, A., Nguyen, C., Xu, Y., Starr, J., Borzilleri, K., Smith, J., Zhu, H., Farley, K. A., Ding, W., Schiemer, J., et al. (2018) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1803662115 · Cited by 419 · see citing works

Targeting the C481S ibrutinib-resistance mutation in Bruton’s tyrosine kinase using PROTAC-mediated degradation

Buhimschi, A. D., Armstrong, H. A., Toure, M., Jaime-Figueroa, S., Chen, T. L., Lehman, A. M., Woyach, J. A., Johnson, A. J., Byrd, J. C., & Crews, C. M. (2018) · Biochemistry · doi:10.1021/acs.biochem.8b00391 · Cited by 394 · see citing works

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Zhou, B. N., Hu, J., Xu, F., Chen, Z., Bai, L., Fernández‐Salas, E., Lin, M., Liu, L., Yang, C., Zhao, Y., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01816 · Cited by 373 · see citing works

PHOTACs enable optical control of protein degradation

Reynders, M., Matsuura, B. S., Bérouti, M., Simoneschi, D., Marzio, A., Pagano, M., & Trauner, D. H. (2020) · Science Advances · doi:10.1126/sciadv.aay5064 · Cited by 333 · see citing works

Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs

Pfaff, P., Samarasinghe, K. T. G., Crews, C. M., & Carreira, E. M. (2019) · ACS Central Science · doi:10.1021/acscentsci.9b00713 · Cited by 314 · see citing works

PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

Sun, Y., Zhao, X., Ding, N., Gao, H., Wu, Y., Yang, Y., Zhao, M., Hwang, J., Song, Y., Liu, W., et al. (2018) · Cell Research · doi:10.1038/s41422-018-0055-1 · Cited by 295 · see citing works

Zebrafish: an emerging technology for in vivo pharmacological assessment to identify potential safety liabilities in early drug discovery

de Barros, T. P., ALDERTON, W. K., Reynolds, H. M., Roach, A. G., & Berghmans, S. (2008) · British Journal of Pharmacology · doi:10.1038/bjp.2008.249 · Cited by 276 · see citing works

Optical Control of Small Molecule-Induced Protein Degradation

Naro, Y., Darrah, K. E., & Deiters, A. (2020) · Journal of the American Chemical Society · doi:10.1021/jacs.9b12718 · Cited by 226 · see citing works

Photodynamic therapy and pain: A systematic review

Ang, J. M., Riaz, I. B., Kamal, M. U., Paragh, G., & Zeitouni, N. C. (2017) · Photodiagnosis and Photodynamic Therapy · doi:10.1016/j.pdpdt.2017.07.002 · Cited by 150 · see citing works

Suppression of BRD4 inhibits human hepatocellular carcinoma by repressing MYC and enhancing BIM expression

Li, G.-Q., Guo, W.-Z., Zhang, Y., Seng, J.-J., Zhang, H., Ma, X.-X., Zhang, G., Li, J., Yan, B., Tang, H., et al. (2015) · Oncotarget · doi:10.18632/oncotarget.6275 · Cited by 122 · see citing works

A chemical approach for global protein knockdown from mice to non-human primates

Sun, X., Wang, J., Yao, X., Zheng, W., Mao, Y., Lan, T., Wang, L., Sun, Y., Zhang, X., Zhao, Q., et al. (2019) · Cell Discovery · doi:10.1038/s41421-018-0079-1 · Cited by 118 · see citing works

Neuroprotective effects of targeting BET proteins for degradation with dBET1 in aged mice subjected to ischemic stroke

DeMars, K. M., Yang, C., & Candelario‐Jalil, E. (2019) · Neurochemistry International · doi:10.1016/j.neuint.2019.03.004 · Cited by 63 · see citing works

Brd4 associates with mitotic chromosomes throughout early zebrafish embryogenesis

Toyama, R., Rebbert, M. L., Dey, A., Ozato, K., & Dawid, I. B. (2008) · Developmental Dynamics · doi:10.1002/dvdy.21576 · Cited by 31 · see citing works

PROTACs: past, present and future

Li, K., & Crews, C. M. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00193d · Cited by 869 · see citing works

Advancing targeted protein degradation for cancer therapy

Dale, B., Cheng, M., Park, K., Kanıskan, H. Ü., Xiong, Y., & Jin, J. J. (2021) · Nature reviews. Cancer · doi:10.1038/s41568-021-00365-x · Cited by 671 · see citing works

PROTACs: great opportunities for academia and industry

Sun, X., Gao, H., Yang, Y., He, M., Wu, Y., Song, Y.-G., Tong, Y., & Rao, Y. (2019) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-019-0101-6 · Cited by 651 · see citing works

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy

Li, X., & Song, Y. (2020) · Journal of Hematology & Oncology · doi:10.1186/s13045-020-00885-3 · Cited by 550 · see citing works

PROTACs: An Emerging Therapeutic Modality in Precision Medicine

Nalawansha, D. A., & Crews, C. M. (2020) · Cell chemical biology · doi:10.1016/j.chembiol.2020.07.020 · Cited by 514 · see citing works

Current strategies for the design of PROTAC linkers: a critical review

Troup, R. I., Fallan, C., & Baud, M. G. J. (2020) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2020.00018 · Cited by 424 · see citing works

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Li, X., Pu, W., Zheng, Q., Ai, M., Chen, S., & Peng, Y. (2022) · Molecular Cancer · doi:10.1186/s12943-021-01434-3 · Cited by 374 · see citing works

An overview of PROTACs: a promising drug discovery paradigm

Zi, L., Hu, M., Yu, Y., Du, C., Zhou, H., Liu, C., Chen, Y., Fan, L., Ma, H., Gong, Y., et al. (2022) · Molecular Biomedicine · doi:10.1186/s43556-022-00112-0 · Cited by 366 · see citing works

Epigenetics-targeted drugs: current paradigms and future challenges

Dai, W., Qiao, X., Fang, Y., Guo, R., Bai, P., Liu, S., Li, T., Jiang, Y., Wei, S., Na, Z., et al. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-02039-0 · Cited by 378 · see citing works

Proteolysis-targeting chimera (PROTAC) delivery system: advancing protein degraders towards clinical translation

Chen, Y., Tandon, I., Heelan, W. J., Wang, Y., Tang, W., & Hu, Q. (2022) · Chemical Society Reviews · doi:10.1039/d1cs00762a · Cited by 327 · see citing works

Targeted protein degradation: advances in drug discovery and clinical practice

Zhong, G., Chang, X., Xie, W., & Zhou, X. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-02004-x · Cited by 326 · see citing works

Target and tissue selectivity of PROTAC degraders

Guenette, R. G., Yang, S. W., Min, J., Pei, B., & Potts, P. R. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00200k · Cited by 324 · see citing works

Chemistries of bifunctional PROTAC degraders

Cao, C., He, M., Wang, L., He, Y., & Rao, Y. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00220e · Cited by 313 · see citing works

Cancer Selective Target Degradation by Folate-Caged PROTACs

Liu, J., Chen, H., Liu, Y., Shen, Y., Meng, F., Kanıskan, H. Ü., Jin, J. J., & Wei, W. (2021) · Journal of the American Chemical Society · doi:10.1021/jacs.1c00451 · Cited by 310 · see citing works

Light-induced control of protein destruction by opto-PROTAC

Liu, J., Chen, H., Ma, L., He, Z., Wang, D., Liu, Y., Lin, Q., Zhang, T., Gray, N. S., Kanıskan, H. Ü., et al. (2020) · Science Advances · doi:10.1126/sciadv.aay5154 · Cited by 305 · see citing works

Targeted protein degradation: A promise for undruggable proteins

Samarasinghe, K. T. G., & Crews, C. M. (2021) · Cell chemical biology · doi:10.1016/j.chembiol.2021.04.011 · Cited by 291 · see citing works

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

He, M., Cao, C., Ni, Z., Liu, Y., Song, P., Hao, S., He, Y., Sun, X., & Rao, Y. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00999-9 · Cited by 283 · see citing works

Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs

Alabi, S. B., & Crews, C. M. (2021) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2021.100647 · Cited by 271 · see citing works

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

Zeng, S., Huang, W., Zheng, X., Cheng, L., Zhang, Z., Wang, J., & Shen, Z. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112981 · Cited by 262 · see citing works

Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

Diehl, C. J., & Ciulli, A. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00387b · Cited by 257 · see citing works

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

Khan, S., He, Y., Zhang, X., Yuan, Y., Pu, S., Kong, Q., Zheng, G., & Zhou, D. (2020) · Oncogene · doi:10.1038/s41388-020-1336-y · Cited by 252 · see citing works

Recent Developments in PROTAC‐Mediated Protein Degradation: From Bench to Clinic

Hu, Z., & Crews, C. M. (2022) · ChemBioChem · doi:10.1002/cbic.202100270 · Cited by 231 · see citing works

E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points

Bricelj, A., Steinebach, C., Kuchta, R. D., Gütschow, M., & Sosič, I. (2021) · Frontiers in Chemistry · doi:10.3389/fchem.2021.707317 · Cited by 226 · see citing works

Optical Control of Small Molecule-Induced Protein Degradation

Naro, Y., Darrah, K. E., & Deiters, A. (2020) · Journal of the American Chemical Society · doi:10.1021/jacs.9b12718 · Cited by 226 · see citing works

Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy

Gao, J., Hou, B., Zhu, Q., Yang, L., Jiang, X., Zou, Z., Li, X., Xu, T., Zheng, M., Chen, Y., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-32050-4 · Cited by 226 · see citing works

Functional characterization of SOX2 as an anticancer target

Zhang, S., Xiong, X., & Sun, Y. (2020) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-020-00242-3 · Cited by 208 · see citing works

Emerging New Concepts of Degrader Technologies

Ding, Y., Fei, Y., & Lu, B. (2020) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2020.04.005 · Cited by 204 · see citing works

Prey for the Proteasome: Targeted Protein Degradation—A Medicinal Chemist's Perspective

Luh, L. M., Scheib, U., Juenemann, K., Wortmann, L., Brands, M., & Cromm, P. M. (2020) · Angewandte Chemie International Edition · doi:10.1002/anie.202004310 · Cited by 200 · see citing works

From Conception to Development: Investigating PROTACs Features for Improved Cell Permeability and Successful Protein Degradation

Cecchini, C., Pannilunghi, S., Tardy, S., & Scapozza, L. (2021) · Frontiers in Chemistry · doi:10.3389/fchem.2021.672267 · Cited by 198 · see citing works

Radiotherapy-Triggered Proteolysis Targeting Chimera Prodrug Activation in Tumors

Yang, C., Yang, Y., Li, Y., Ni, Q., & Li, J. (2022) · Journal of the American Chemical Society · doi:10.1021/jacs.2c10177 · Cited by 194 · see citing works

New-generation advanced PROTACs as potential therapeutic agents in cancer therapy

Wang, C., Zhang, Y., Chen, W., Wu, Y., & Xing, D. (2024) · Molecular Cancer · doi:10.1186/s12943-024-02024-9 · Cited by 192 · see citing works

Targeted protein degradation as a powerful research tool in basic biology and drug target discovery

Wu, T., Yoon, H., Xiong, Y., Dixon-Clarke, S. E., Nowak, R. P., & Fischer, E. S. (2020) · Nature Structural & Molecular Biology · doi:10.1038/s41594-020-0438-0 · Cited by 188 · see citing works

PROTACs: A novel strategy for cancer therapy

Liu, J., Ma, J., Liu, Y., Xia, J., Li, Y., Wang, Z. P., & Wei, W. (2020) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2020.02.006 · Cited by 186 · see citing works

E3 ligase ligand chemistries: from building blocks to protein degraders

Sosič, I., Bricelj, A., & Steinebach, C. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00148a · Cited by 173 · see citing works

Improved Accuracy for Modeling PROTAC-Mediated Ternary Complex Formation and Targeted Protein Degradation <i>via</i> New <i>In Silico</i> Methodologies

Drummond, M. L., Henry, A., Li, H., & Williams, C. I. (2020) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.0c00897 · Cited by 166 · see citing works

Bioorthogonal PROTAC Prodrugs Enabled by On-Target Activation

Chang, M., Gao, F., Pontigon, D., Gnawali, G. R., Xu, H., & Wang, W. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.3c05159 · Cited by 148 · see citing works

Self-Assembled Nano-PROTAC Enables Near-Infrared Photodynamic Proteolysis for Cancer Therapy

Wang, W., Zhu, C., Zhang, B., Feng, Y., Zhang, Y., & Li, J. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.3c04109 · Cited by 147 · see citing works

Characteristic roadmap of linker governs the rational design of PROTACs

Dong, Y., Ma, T., Xu, T., Feng, Z., Li, Y., Song, L., Yao, X., Ashby, C. R., & Hao, G.-F. (2024) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2024.04.007 · Cited by 146 · see citing works

Rational Design for Nitroreductase (NTR)-Responsive Proteolysis Targeting Chimeras (PROTACs) Selectively Targeting Tumor Tissues

Shi, S., Du, Y., Zou, Y., Niu, J., Cai, Z., Wang, X., Qiu, F., Ding, Y., Yang, G., Wu, Y., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c02221 · Cited by 137 · see citing works

A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

Kounde, C. S., Shchepinova, M. M., Saunders, C. N., Muelbaier, M., Rackham, M. D., Harling, J. D., & Tate, E. W. (2020) · Chemical Communications · doi:10.1039/d0cc00523a · Cited by 136 · see citing works

Development of hypoxia-activated PROTAC exerting a more potent effect in tumor hypoxia than in normoxia

Cheng, W., Li, S., Wen, X., Han, S., Wang, S., Han, W., Song, Z., Wang, Y., Tian, X., & Zhang, X. (2021) · Chemical Communications · doi:10.1039/d1cc05715d · Cited by 129 · see citing works

The state of the art of PROTAC technologies for drug discovery

Wang, C., Zheng, C., Wang, H., Zhang, L., Liu, Z., & Xu, P. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114290 · Cited by 129 · see citing works

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies

He, Y., Khan, S., Huo, Z., Lv, D., Zhang, X., Liu, X., Yuan, Y., Hromas, R., Xu, M., Zheng, G., et al. (2020) · Journal of Hematology &amp; Oncology · doi:10.1186/s13045-020-00924-z · Cited by 126 · see citing works

Clip Chemistry: Diverse (Bio)(macro)molecular and Material Function through Breaking Covalent Bonds

Shieh, P., Hill, M. R., Zhang, W., Kristufek, S. L., & Johnson, J. A. (2021) · Chemical Reviews · doi:10.1021/acs.chemrev.0c01282 · Cited by 119 · see citing works

Strategies for designing proteolysis targeting chimaeras (PROTACs)

He, S., Dong, G., Cheng, J., Wu, Y., & Sheng, C. (2022) · Medicinal Research Reviews · doi:10.1002/med.21877 · Cited by 118 · see citing works

Microneedle Patch Delivery of PROTACs for Anti-Cancer Therapy

Cheng, X., Hu, S., & Cheng, K. (2023) · ACS Nano · doi:10.1021/acsnano.3c03166 · Cited by 119 · see citing works

Recent Advances in Pro-PROTAC Development to Address On-Target Off-Tumor Toxicity

Chen, C., Yang, Y., Wang, Z., Li, H., Dong, C., & Zhang, X. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00302 · Cited by 117 · see citing works

Annual review of PROTAC degraders as anticancer agents in 2022

Wang, X., Qin, Z.-L., Li, N., Jia, M.-Q., Liu, Q.-G., Bai, Y., Song, J., Yuan, S., & Zhang, S. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116166 · Cited by 107 · see citing works

PROTACs: Emerging Targeted Protein Degradation Approaches for Advanced Druggable Strategies

Sincere, N. I., Anand, K., Ashique, S., Yang, J., & You, C. (2023) · Molecules · doi:10.3390/molecules28104014 · Cited by 109 · see citing works

Photo-controllable biochemistry: Exploiting the photocages in phototherapeutic window

Xiong, H., Xu, Y., Kim, B., Rha, H., Zhang, B., Li, M., Yang, G., & Kim, J. S. (2022) · Chem · doi:10.1016/j.chempr.2022.11.007 · Cited by 106 · see citing works

A region-confined PROTAC nanoplatform for spatiotemporally tunable protein degradation and enhanced cancer therapy

Gao, J., Jiang, X., Lei, S., Cheng, W., Lai, Y., Li, M., Yang, L., Liu, P., Chen, X., Huang, M., et al. (2024) · Nature Communications · doi:10.1038/s41467-024-50735-w · Cited by 102 · see citing works

Progress and Challenges in Targeted Protein Degradation for Neurodegenerative Disease Therapy

Fang, Y., Wang, J., Zhao, M., Zheng, Q., Ren, C., Wang, Y., & Zhang, J. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00844 · Cited by 100 · see citing works

BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications

To, K. K. W., Xing, E., Larue, R. C., & Li, P. (2023) · Molecules · doi:10.3390/molecules28073043 · Cited by 95 · see citing works

Exploring the target scope of KEAP1 E3 ligase-based PROTACs

Du, G., Jiang, J., Henning, N. J., Safaee, N., Koide, E., Nowak, R. P., Donovan, K. A., Yoon, H., You, I., Yue, H., et al. (2022) · Cell chemical biology · doi:10.1016/j.chembiol.2022.08.003 · Cited by 94 · see citing works

Stimuli‐Responsive PROTACs for Controlled Protein Degradation

An, K., Deng, X., Chi, H., Zhang, Y., Li, Y., Cheng, M., Ni, Z., Yang, Z., Wang, C., Chen, J., et al. (2023) · Angewandte Chemie International Edition · doi:10.1002/anie.202306824 · Cited by 94 · see citing works

Photopharmacology and photoresponsive drug delivery

Liu, Y., Wang, T., & Wang, W. (2025) · Chemical Society Reviews · doi:10.1039/d5cs00125k · Cited by 97 · see citing works

PROTAC technology: From drug development to probe technology for target deconvolution

Yan, S., Zhang, G., Luo, W., Xu, M., Peng, R., Du, Z., Liu, Y., Bai, Z., Xiao, X., & Qin, S. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116725 · Cited by 92 · see citing works

Ultrasound-Activated PROTAC Prodrugs Overcome Immunosuppression to Actuate Efficient Deep-Tissue Sono-Immunotherapy in Orthotopic Pancreatic Tumor Mouse Models

Liu, Y., Wang, H., Ding, M., Wang, Y., Wang, K., Ullah, I., Bulatov, E., & Yuan, Y. (2024) · Nano Letters · doi:10.1021/acs.nanolett.4c02287 · Cited by 90 · see citing works

Targeted Biomolecule Regulation Platform: A Split-and-Mix PROTAC Approach

Yang, F., Luo, Q., Wang, Y., Liang, H., Wang, Y., Hou, Z., Wan, C., Wang, Y., Liu, Z., Ye, Y., et al. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c12824 · Cited by 88 · see citing works

Stimuli-activatable PROTACs for precise protein degradation and cancer therapy

Gao, J., Yang, L., Lei, S., Zhou, F., Nie, H., Peng, B., Xu, T., Chen, X., Yang, X., Sheng, C., et al. (2023) · 中国科学通报：英文版 · doi:10.1016/j.scib.2023.04.028 · Cited by 87 · see citing works

Reactive oxygen species-responsive Pre-PROTAC for tumor-specific protein degradation

Liu, H., Ren, C., Sun, R., Wang, H. H., Zhan, Y., Yang, X., Jiang, B., & Chen, H. (2022) · Chemical Communications · doi:10.1039/d2cc03367d · Cited by 86 · see citing works

Near-Infrared-Activatable PROTAC Nanocages for Controllable Target Protein Degradation and On-Demand Antitumor Therapy

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Overview of epigenetic degraders based on PROTAC, molecular glue, and hydrophobic tagging technologies

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Targeting the Ubiquitin-Proteasome System for Cancer Therapeutics by Small-Molecule Inhibitors

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Hypoxia deactivates epigenetic feedbacks via enzyme-derived clicking proteolysis-targeting chimeras

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Nano-PROTACs: state of the art and perspectives

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Advancing targeted protein degradation for metabolic diseases therapy

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Photo-controllable bioorthogonal chemistry for spatiotemporal control of bio-targets in living systems

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Optical control of targeted protein degradation

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Inducible Degradation of Oncogenic Nucleolin Using an Aptamer-Based PROTAC

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Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine

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Recent progress in degradation of membrane proteins by PROTACs and alternative targeted protein degradation techniques

Chen, S., Cui, J., Chen, H., Yu, B., & Long, S. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115911 · Cited by 70 · see citing works

ClickRNA-PROTAC for Tumor-Selective Protein Degradation and Targeted Cancer Therapy

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PROTAC 2.0: Expanding the frontiers of targeted protein degradation

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Recent Advances of Degradation Technologies Based on PROTAC Mechanism

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Targeted protein degradation in cancers: Orthodox PROTACs and beyond

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Molecular glue-mediated targeted protein degradation: A novel strategy in small-molecule drug development

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Targeted Cancer Therapy Using Compounds Activated by Light

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Proteolysis-Targeting Chimeras (PROTACs) in Cancer Therapy: Present and Future

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Targeted delivery of PROTAC-based prodrug activated by bond-cleavage bioorthogonal chemistry for microneedle-assisted cancer therapy

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Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation

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Journey of PROTAC: From Bench to Clinical Trial and Beyond

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Biomarker-activated multifunctional lysosome-targeting chimeras mediated selective degradation of extracellular amyloid fibrils

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Novel approaches to targeted protein degradation technologies in drug discovery

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Current advances of small molecule E3 ligands for proteolysis-targeting chimeras design

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Enriching Proteolysis Targeting Chimeras with a Second Modality: When Two Are Better Than One

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Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

Zhong, Y., Chi, F., Wu, H., Liu, Y., Xie, Z., Huang, W., Shi, W., & Qian, H. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114142 · Cited by 51 · see citing works

Degraders upgraded: the rise of PROTACs in hematological malignancies

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In Vivo Self‐Assembly of PROTACs by Bioorthogonal Chemistry for Precision Cancer Therapy

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Applications of Bacterial Degrons and Degraders — Toward Targeted Protein Degradation in Bacteria

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Rational Design of Bioorthogonally Activatable PROTAC for Tumor-Targeted Protein Degradation

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Self‐Oxygenating PROTAC Microneedle for Spatiotemporally‐Confined Protein Degradation and Enhanced Glioblastoma Therapy

Jiang, X., Lai, Y., Xia, W., Yang, W., Wang, J., Pan, J., Zhao, Q., Zhou, X., Li, S., Zhang, S., et al. (2025) · Advanced Materials · doi:10.1002/adma.202411869 · Cited by 49 · see citing works

Research progress of MEK1/2 inhibitors and degraders in the treatment of cancer

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Proteases and Their Modulators in Cancer Therapy: Challenges and Opportunities

Song, R., Qiao, W., He, J., Huang, J., Luo, Y., & Yang, T. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01640 · Cited by 45 · see citing works

Development of photocontrolled BRD4 PROTACs for tongue squamous cell carcinoma (TSCC)

Li, Z., Ma, S., Yang, X., Zhang, L., Dong, L., Dong, G., Du, L., Lv, Z., & Li, M. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113608 · Cited by 45 · see citing works

Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer

Liu, Q., Tu, G., Hu, Y., Jiang, Q., Liu, J., Lin, S., Yu, Z., Li, G., Wu, X., Tang, Y., et al. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.114013 · Cited by 43 · see citing works

Ligation to Scavenging Strategy Enables On-Demand Termination of Targeted Protein Degradation

Jin, Y., Fan, J., Wang, R., Wang, X., Li, N., You, Q., & Jiang, Z. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c12809 · Cited by 43 · see citing works

Progress in the controllability technology of PROTAC

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Degraders in epigenetic therapy: PROTACs and beyond

Dai, X., Ji, S., Fu, M., Liu, G.-Z., Liu, H., Wang, S., Shen, L., Wang, N., Herdewijn, P. A., Zheng, Y., et al. (2024) · Theranostics · doi:10.7150/thno.92526 · Cited by 44 · see citing works

Radiation responsive PROTAC nanoparticles for tumor-specific proteolysis enhanced radiotherapy

Xu, M., Yun, Y., Li, C., Ruan, Y., Muraoka, O., Xie, W., & Sun, X. (2024) · Journal of Materials Chemistry B · doi:10.1039/d3tb03046f · Cited by 41 · see citing works

Inducing protein degradation using light

Singh, A. (2019) · Nature Methods · doi:10.1038/s41592-019-0685-3 · Cited by 1 · see citing works

A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

Kounde, C. S., Shchepinova, M. M., Saunders, C. N., Muelbaier, M., Rackham, M. D., Harling, J. D., & Tate, E. W. (2020) · Chemical Communications · doi:10.1039/d0cc00523a · Cited by 136 · see citing works

Development of visible-light-activatable photocaged PROTACs

Weng, W., Xue, G., & Pan, Z. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.116062 · Cited by 20 · see citing works

PHOTACs Enable Optical Control of Protein Degradation

Reynders, M., & Trauner, D. H. (2021) · Methods in molecular biology · doi:10.1007/978-1-0716-1665-9_17 · Cited by 17 · see citing works

Light-induced control of protein destruction by opto-PROTAC

Liu, J., Chen, H., Ma, L., He, Z., Wang, D., Liu, Y., Lin, Q., Zhang, T., Gray, N. S., Kanıskan, H. Ü., et al. (2020) · Science Advances · doi:10.1126/sciadv.aay5154 · Cited by 305 · see citing works