Targeted protein degraders crowd into the clinic

PROTAC targeted protein degraders: the past is prologue

Békés, M., Langley, D. R., & Crews, C. M. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00371-6 · Cited by 3,395 · see citing works

Targeted protein degradation: mechanisms, strategies and application

Zhao, L., Zhao, J., Zhong, K., Tong, A., & Jia, D. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00966-4 · Cited by 986 · 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

Antibody–drug conjugates come of age in oncology

Dumontet, C., Reichert, J. M., Senter, P. D., Lambert, J. M., & Beck, A. (2023) · Nature Reviews Drug Discovery · doi:10.1038/s41573-023-00709-2 · Cited by 858 · see citing works

Targeted protein degradation: from mechanisms to clinic

Tsai, J. M., Nowak, R. P., Ebert, B. L., & Fischer, E. S. (2024) · Nature Reviews Molecular Cell Biology · doi:10.1038/s41580-024-00729-9 · Cited by 438 · see citing works

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

Xie, X., Yu, T., Li, X., Zhang, N., Foster, L. J., Peng, C., Huang, W., & He, G. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01589-z · Cited by 396 · 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

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

The PROTACtable genome

Schneider, M., Radoux, C. J., Hercules, A., Ochoa, D., Dunham, I., Zalmas, L.-P., Hessler, G., Ruf, S., Shanmugasundaram, V., Hann, M. M., et al. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00245-x · Cited by 273 · see citing works

Molecular Glues: The Adhesive Connecting Targeted Protein Degradation to the Clinic

Sasso, J. M., Tenchov, R., Wang, D.-S., Johnson, L. S., Wang, X., & Zhou, Q. A. (2022) · Biochemistry · doi:10.1021/acs.biochem.2c00245 · Cited by 259 · see citing works

Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras

Bemis, T. A., Clair, J. J. L., & Burkart, M. D. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00482 · Cited by 244 · see citing works

A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo

Kofink, C. C., Trainor, N. B., Mair, B., Wöhrle, S., Wurm, M., Mischerikow, N., Roy, M. J., Bader, G., Greb, P., Garavel, G., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-33430-6 · Cited by 239 · see citing works

Chasing molecular glue degraders: screening approaches

Domostegui, A., Nieto-Barrado, L., Perez-Lopez, C., & Mayor-Ruiz, C. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00197g · Cited by 200 · see citing works

Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood–Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2

Liu, X., Kalogeropulou, A. F., Domingos, S., Makukhin, N., Nirujogi, R. S., Singh, F., Shpiro, N., Saalfrank, A., Sammler, E. M., Ganley, I. G., et al. (2022) · Journal of the American Chemical Society · doi:10.1021/jacs.2c05499 · Cited by 198 · see citing works

Elucidating the cellular determinants of targeted membrane protein degradation by lysosome-targeting chimeras

Ahn, G., Riley, N. M., Kamber, R. A., Wisnovsky, S., von Hase, S. M., Bassik, M. C., Banik, S. M., & Bertozzi, C. R. (2023) · Science · doi:10.1126/science.adf6249 · Cited by 197 · 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

ALK-positive lung cancer: a moving target

Schneider, J. L., Lin, J. J., & Shaw, A. T. (2023) · Nature Cancer · doi:10.1038/s43018-023-00515-0 · Cited by 190 · see citing works

Clinical application of advanced multi-omics tumor profiling: Shaping precision oncology of the future

Akhoundova, D., & Rubin, M. A. (2022) · Cancer Cell · doi:10.1016/j.ccell.2022.08.011 · Cited by 188 · 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

Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation

Hendrick, C. E., Jorgensen, J. R., Chaudhry, C., Strambeanu, I. I., Brazeau, J.-F., Schiffer, J. M., Shi, Z., Venable, J. D., & Wolkenberg, S. E. (2022) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.2c00124 · Cited by 170 · see citing works

Expanding the arsenal of E3 ubiquitin ligases for proximity-induced protein degradation

Kannt, A., & Đikić, I. (2021) · Cell chemical biology · doi:10.1016/j.chembiol.2021.04.007 · Cited by 148 · see citing works

Proteolysis-targeting chimeras with reduced off-targets

Nguyen, T. M., Sreekanth, V., Deb, A., Kokkonda, P., Tiwari, P. K., Donovan, K. A., Shoba, V. M., Chaudhary, S. K., Mercer, J. A. M., Lai, S., et al. (2023) · Nature Chemistry · doi:10.1038/s41557-023-01379-8 · Cited by 145 · see citing works

MDM2 Inhibitors for Cancer Therapy: The Past, Present, and Future

Wang, W., Albadari, N. G., Du, Y., Fowler, J. F., Sang, H. T., Xian, W., McKeon, F., Li, W., Zhou, J., & Zhang, R. (2024) · Pharmacological Reviews · doi:10.1124/pharmrev.123.001026 · Cited by 147 · see citing works

The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells

Kurimchak, A. M., Herrera-Montávez, C., Montserrat-Sangrà, S., Araiza-Olivera, D., Hu, J., Neumann-Domer, R., Kuruvilla, M., Bellacosa, A., Testa, J. R., Jin, J., et al. (2022) · Science Signaling · doi:10.1126/scisignal.abn2707 · Cited by 136 · see citing works

Driving E3 Ligase Substrate Specificity for Targeted Protein Degradation: Lessons from Nature and the Laboratory

Cowan, A. D., & Ciulli, A. (2022) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-032620-104421 · Cited by 129 · see citing works

Integrative Modeling of PROTAC-Mediated Ternary Complexes

Weng, G., Li, D., Kang, Y., & Hou, T. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01576 · Cited by 130 · 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

Overcoming Cancer Drug Resistance Utilizing PROTAC Technology

Burke, M. R., Smith, A. R., & Zheng, G. (2022) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2022.872729 · Cited by 126 · see citing works

Folate-Guided Protein Degradation by Immunomodulatory Imide Drug-Based Molecular Glues and Proteolysis Targeting Chimeras

Chen, H., Liu, J., Kanıskan, H. Ü., Wei, W., & Jin, J. J. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00901 · Cited by 125 · see citing works

Development of a novel PROTAC using the nucleic acid aptamer as a targeting ligand for tumor selective degradation of nucleolin

Zhang, L., Li, L., Wang, X., Liu, H., Zhang, Y., Xie, T., Zhang, H., Li, X., Peng, T., Sun, X. H., et al. (2022) · Molecular Therapy — Nucleic Acids · doi:10.1016/j.omtn.2022.09.008 · Cited by 122 · see citing works

Protein kinases: drug targets for immunological disorders

Castelo‐Soccio, L. A., Kim, H., Gadina, M., Schwartzberg, P. L., Laurence, A. D. J., & O’Shea, J. J. (2023) · Nature reviews. Immunology · doi:10.1038/s41577-023-00877-7 · Cited by 125 · see citing works

Destruction of DNA‐Binding Proteins by Programmable Oligonucleotide PROTAC (O'PROTAC): Effective Targeting of LEF1 and ERG

Shao, J., Yan, Y., Ding, D., Wang, D., He, Y., Pan, Y., Yan, W., Kharbanda, A., Li, H., & Huang, H. (2021) · Advanced Science · doi:10.1002/advs.202102555 · Cited by 120 · 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

Targeted degradation via direct 26S proteasome recruitment

Bashore, C., Prakash, S., Johnson, M. C., Conrad, R. J., Kekessie, I. A., Scales, S. J., Ishisoko, N., Kleinheinz, T., Liu, P. S., Popovych, N., et al. (2022) · Nature Chemical Biology · doi:10.1038/s41589-022-01218-w · Cited by 118 · see citing works

PROTAC’ing oncoproteins: targeted protein degradation for cancer therapy

Kelm, J. M., Pandey, D. S., Malin, E., Kansou, H. W., Arora, S., Kumar, R., & Gavande, N. S. (2023) · Molecular Cancer · doi:10.1186/s12943-022-01707-5 · Cited by 115 · see citing works

Nano Proteolysis Targeting Chimeras (PROTACs) with Anti‐Hook Effect for Tumor Therapy

Zhang, N., Hou, D., Hu, X., Liang, J., Wang, M., Song, Z., Li, Y., Wang, Z., An, H., Xu, W., et al. (2023) · Angewandte Chemie International Edition · doi:10.1002/anie.202308049 · Cited by 113 · see citing works

Design principles for cyclin K molecular glue degraders

Kozicka, Z., Suchyta, D. J., Focht, V., Kempf, G., Petzold, G., Jentzsch, M., Zou, C., Di Genua, C., Donovan, K. A., Coomar, S., et al. (2024) · Nature Chemical Biology · doi:10.1038/s41589-023-01409-z · Cited by 113 · see citing works

Targeted protein degrader development for cancer: advances, challenges, and opportunities

Fang, Y., Wang, S., Han, S., Zhao, Y., Yu, C., Liu, H., & Li, N. (2023) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2023.03.003 · Cited by 110 · see citing works

Aptamer-Based Targeted Protein Degradation

Liu, Y., Qian, X., Ran, C., Li, L., Fu, T., Su, D., Xie, S., & Tan, W. (2023) · ACS Nano · doi:10.1021/acsnano.2c10379 · Cited by 106 · see citing works

The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation

Riching, K. M., Caine, E. A., Urh, M., & Daniels, D. L. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00339b · Cited by 105 · see citing works

Involvement of the pro-oncogenic enzyme fatty acid synthase in the hallmarks of cancer: a promising target in anti-cancer therapies

Vanauberg, D., Schulz, C., & Lefebvre, T. (2023) · Oncogenesis · doi:10.1038/s41389-023-00460-8 · Cited by 104 · see citing works

Discovery of a Highly Potent and Selective Dual PROTAC Degrader of CDK12 and CDK13

Yang, J., Chang, Y., Tien, J. C.-Y., Wang, Z., Zhou, Y., Zhang, P., Huang, W., Vo, J. N., Apel, I. J., Wang, C., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00384 · Cited by 96 · see citing works

Ispinesib as an Effective Warhead for the Design of Autophagosome-Tethering Chimeras: Discovery of Potent Degraders of Nicotinamide Phosphoribosyltransferase (NAMPT)

Dong, G., Wu, Y., Cheng, J., Chen, L., Liu, R., Ding, Y., Wu, S., Ma, J., & Sheng, C. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c02001 · Cited by 95 · see citing works

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands

Zhao, H., Wang, H., Mao, Y.-Z., Zhang, H., Xin, M., Xi, X.-X., Lei, H., Mao, S., Li, D., & Zhang, S. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01827 · Cited by 94 · see citing works

Degrader–Antibody Conjugates: Emerging New Modality

Hong, K. B., & An, H. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01791 · Cited by 90 · see citing works

Regulated induced proximity targeting chimeras—RIPTACs—A heterobifunctional small molecule strategy for cancer selective therapies

Raina, K., Forbes, C. D., Stronk, R., Rappi, J. P., Eastman, K. J., Zaware, N., Yu, X., Li, H., Bhardwaj, A., Gerritz, S. W., et al. (2024) · Cell chemical biology · doi:10.1016/j.chembiol.2024.07.005 · Cited by 90 · see citing works

PROTAC therapy as a new targeted therapy for lung cancer

Li, J. W., Zheng, G., Kaye, F. J., & Wu, L. (2023) · Molecular Therapy · doi:10.1016/j.ymthe.2022.11.011 · Cited by 87 · 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

Target 2035 – update on the quest for a probe for every protein

Müller, S., Ackloo, S. Z., Chawaf, A. A., Al‐Lazikani, B., Antolín, A. A., Baell, J. B., Beck, H., Beedie, S., Betz, U. A. K., Bezerra, G. A., et al. (2021) · RSC Medicinal Chemistry · doi:10.1039/d1md00228g · Cited by 85 · see citing works

Piperlongumine conjugates induce targeted protein degradation

Pei, J., Xiao, Y., Liu, X., Hu, W., Sobh, A., Yuan, Y., Zhou, S., Hua, N., Mackintosh, S. G., Zhang, X., et al. (2023) · Cell chemical biology · doi:10.1016/j.chembiol.2023.01.004 · Cited by 84 · see citing works

The rise and rise of protein degradation: Opportunities and challenges ahead

Hughes, S. J., Testa, A., Thompson, N., & Churcher, I. (2021) · Drug Discovery Today · doi:10.1016/j.drudis.2021.08.006 · Cited by 83 · see citing works

Development of folate receptor targeting chimeras for cancer selective degradation of extracellular proteins

Zhou, Y., Li, C., Chen, X., Zhao, Y., Liao, Y., Huang, P., Wu, W., Nieto, N. S., Li, L., & Tang, W. (2024) · Nature Communications · doi:10.1038/s41467-024-52685-9 · Cited by 80 · see citing works

Drug delivery challenges and formulation aspects of proteolysis targeting chimera (PROTACs)

Saraswat, A. L., Vartak, R., Hegazy, R. R., Patel, A., & Patel, K. R. (2022) · Drug Discovery Today · doi:10.1016/j.drudis.2022.103387 · Cited by 81 · see citing works

PROTAC Delivery Strategies for Overcoming Physicochemical Properties and Physiological Barriers in Targeted Protein Degradation

Syahputra, E. W., Lee, H., Cho, H. J., Park, H. J., Park, K., & Hwang, D. (2025) · Pharmaceutics · doi:10.3390/pharmaceutics17040501 · Cited by 82 · see citing works

Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity

Sinatra, L., Yang, J. C., Schliehe‐Diecks, J., Dienstbier, N., Vogt, M., Gebing, P., Bachmann, L. M., Sönnichsen, M., Lenz, T., Stühler, K., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01659 · Cited by 74 · see citing works

Integrated Direct-to-Biology Platform for the Nanoscale Synthesis and Biological Evaluation of PROTACs

Stevens, R., Bendito-Moll, E., Battersby, D. J., Miah, A. H., Wellaway, N., Law, R. P., Stacey, P., Klimaszewska, D., Macina, J. M., Burley, G. A., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01604 · Cited by 74 · see citing works

Gαs–Protein Kinase A (PKA) Pathway Signalopathies: The Emerging Genetic Landscape and Therapeutic Potential of Human Diseases Driven by Aberrant Gαs-PKA Signaling

Ramms, D. J., Raimondi, F., Arang, N., Herberg, F. W., Taylor, S. S., & Gutkind, J. S. (2021) · Pharmacological Reviews · doi:10.1124/pharmrev.120.000269 · Cited by 73 · see citing works

Amorphous solid dispersions: Utilization and challenges in preclinical drug development within AstraZeneca

Anane‐Adjei, A. B., Jacobs, E., Nash, S. C., Askin, S., Soundararajan, R., Kyobula, M., Booth, J., & Campbell, A. D. (2021) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2021.121387 · Cited by 73 · see citing works

Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands

Bricelj, A., Ng, Y. L. D., Ferber, D., Kuchta, R. D., Müller, S., Monschke, M., Wagner, K. G., Krönke, J., Sosič, I., Gütschow, M., et al. (2021) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.1c00368 · Cited by 71 · see citing works

Discovery of KRAS(G12D) selective degrader ASP3082

Yoshinari, T., Nagashima, T., Ishioka, H., Inamura, K., Nishizono, Y., Tasaki, M., Iguchi, K., Suzuki, A., Sato, C., Nakayama, A., et al. (2025) · Communications Chemistry · doi:10.1038/s42004-025-01662-4 · Cited by 71 · see citing works

High-power screening (HPS) empowered by DNA-encoded libraries

Sunkari, Y. K., Siripuram, V. K., Nguyen, T.-L., & Flajolet, M. (2021) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2021.10.008 · Cited by 69 · see citing works

Expanding the landscape of E3 ligases for targeted protein degradation

Kramer, L. T. S., & Zhang, X. (2022) · Current Research in Chemical Biology · doi:10.1016/j.crchbi.2022.100020 · Cited by 69 · see citing works

Opportunities and challenges of protein-based targeted protein degradation

Shen, F., & Dassama, L. M. K. (2023) · Chemical Science · doi:10.1039/d3sc02361c · Cited by 69 · see citing works

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

Teng, X., Zhao, X., Dai, Y., Zhang, X., Zhang, Q., Wu, Y., Hu, D., & Li, J. (2024) · Journal of the American Chemical Society · doi:10.1021/jacs.4c06402 · Cited by 69 · see citing works

Discovery of Novel PROTAC SIRT6 Degraders with Potent Efficacy against Hepatocellular Carcinoma

Huang, J., Su, J., Wang, H., Chen, J., Tian, Y., Zhang, J., Feng, T., Di, L., Lu, X., Sheng, H., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01223 · Cited by 70 · see citing works

Allostery: Allosteric Cancer Drivers and Innovative Allosteric Drugs

Nussinov, R., Zhang, M., Maloney, R., Liu, Y., Tsai, C.-J., & Jang, H. (2022) · Journal of Molecular Biology · doi:10.1016/j.jmb.2022.167569 · Cited by 66 · see citing works

A Versatile and Sustainable Multicomponent Platform for the Synthesis of Protein Degraders: Proof-of-Concept Application to BRD4-Degrading PROTACs

Bhela, I. P., Ranza, A., Balestrero, F. C., Serafini, M. T., Aprile, S., Martino, R. M. C. D., Condorelli, F., & Pirali, T. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01218 · Cited by 67 · see citing works

Development of Substituted Phenyl Dihydrouracil as the Novel Achiral Cereblon Ligands for Targeted Protein Degradation

Xie, H., Li, C., Tang, H., Tandon, I., Liao, J., Roberts, B. L., Zhao, Y. Q., & Tang, W. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01941 · Cited by 67 · see citing works

The rise of degrader drugs

Teng, M., & Gray, N. S. (2023) · Cell chemical biology · doi:10.1016/j.chembiol.2023.06.020 · Cited by 67 · see citing works

Antiviral strategies against influenza virus: an update on approved and innovative therapeutic approaches

Bonomini, A., Mercorelli, B., & Loregian, A. (2025) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-025-05611-1 · Cited by 67 · see citing works

FOXA1: A Pioneer of Nuclear Receptor Action in Breast Cancer

Seachrist, D. D., Anstine, L. J., & Keri, R. A. (2021) · Cancers · doi:10.3390/cancers13205205 · Cited by 66 · see citing works

Recent advances in the development of EGFR degraders: PROTACs and LYTACs

Hong, D., Zhou, B., Zhang, B., Ren, H., Zhu, L., Zheng, G., Ge, M., & Ge, J. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114533 · Cited by 66 · see citing works

Beyond Proteolysis-Targeting Chimeric Molecules: Designing Heterobifunctional Molecules Based on Functional Effectors

Hua, L., Zhang, Q., Zhu, X., Wang, R., You, Q., & Wang, L. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00316 · Cited by 66 · see citing works

The era of high-quality chemical probes

Licciardello, M. P., & Workman, P. (2022) · RSC Medicinal Chemistry · doi:10.1039/d2md00291d · Cited by 60 · see citing works

A beginner’s guide to current synthetic linker strategies towards VHL-recruiting PROTACs

Zografou-Barredo, N. A., Hallatt, A. J., Goujon-Ricci, J., & Cano, C. (2023) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2023.117334 · Cited by 64 · see citing works

Importance of Three-Body Problems and Protein–Protein Interactions in Proteolysis-Targeting Chimera Modeling: Insights from Molecular Dynamics Simulations

Li, W., Zhang, J., Guo, L., & Wang, Q. (2022) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.1c01150 · Cited by 63 · see citing works

A Complex Metabolic Network Confers Immunosuppressive Functions to Myeloid-Derived Suppressor Cells (MDSCs) within the Tumour Microenvironment

Hofer, F., Sario, G. D., Musiu, C., Sartoris, S., Sanctis, F. D., & Ugel, S. (2021) · Cells · doi:10.3390/cells10102700 · Cited by 59 · see citing works

A platform for the rapid synthesis of proteolysis targeting chimeras (Rapid-TAC) under miniaturized conditions

Guo, L., Zhou, Y., Nie, X., Zhang, Z., Zhang, Z., Li, C., Wang, T., & Tang, W. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114317 · Cited by 61 · see citing works

Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins

Thomas, J. E., Wang, M., Jiang, W., Wang, M., Wang, L., Wen, B., Sun, D., & Wang, S. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00492 · Cited by 61 · see citing works

Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation

Norris, S. H., Ba, X., Rhodes, J., Huang, D., Khambatta, G., Buenviaje, J., Nayak, S. K., Meiring, J., Reiss, S. M., Xu, S., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01848 · Cited by 61 · see citing works

Direct-to-biology, automated, nano-scale synthesis, and phenotypic screening-enabled E3 ligase modulator discovery

Wang, Z., Shaabani, S., Gao, X., Ng, Y. L. D., Sapozhnikova, V., Mertins, P., Krönke, J., & Dömling, A. S. S. (2023) · Nature Communications · doi:10.1038/s41467-023-43614-3 · Cited by 61 · see citing works

Overcoming Cancer Resistance: Strategies and Modalities for Effective Treatment

Koirala, M., & DiPaola, M. (2024) · Biomedicines · doi:10.3390/biomedicines12081801 · Cited by 67 · see citing works

Amelioration of hepatic steatosis by dietary essential amino acid-induced ubiquitination

Zhang, Y., Lin, S., Peng, J., Liang, X., Yang, Q., Bai, X., Li, Y., Li, J., Dong, W., Wang, Y., et al. (2022) · Molecular Cell · doi:10.1016/j.molcel.2022.01.021 · Cited by 58 · see citing works

Systematic Potency and Property Assessment of VHL Ligands and Implications on PROTAC Design

Krieger, J., Sorrell, F. J., Wegener, A. A., Leuthner, B., Machrouhi, F., Hecht, M., Leibrock, E.-M., Müller, J. E., Eisert, J., Hartung, I. V., et al. (2023) · ChemMedChem · doi:10.1002/cmdc.202200615 · Cited by 59 · see citing works

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

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Dual IKZF2 and CK1α degrader targets acute myeloid leukemia cells

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Clues to molecular glues

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A TRIM21-based bioPROTAC highlights the therapeutic benefit of HuR degradation

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

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Ubiquitination in T-Cell Activation and Checkpoint Inhibition: New Avenues for Targeted Cancer Immunotherapy

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

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Structure-based assessment and druggability classification of protein–protein interaction sites

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Making Protein Degradation Visible: Discovery of Theranostic PROTACs for Detecting and Degrading NAMPT

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Machine Learning Modeling of Protein-Intrinsic Features Predicts Tractability of Targeted Protein Degradation

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Rapid PROTAC Discovery Platform: Nanomole-Scale Array Synthesis and Direct Screening of Reaction Mixtures

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

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Proteomic characterization of post-translational modifications in drug discovery

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Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4

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Regulation of Mitogen-Activated Protein Kinase Signaling Pathways by the Ubiquitin-Proteasome System and Its Pharmacological Potential

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Protein degraders push into novel target space

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Targeted protein degradation: from mechanisms to clinic

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Targeted protein degraders - new modalities for drug discovery

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Targeted protein degradation: mechanistic diversity, therapeutic expansion, and clinical translation

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Targeted protein degradation comes of age

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