Targeted protein degraders crowd into the clinic

Targeted protein modification as a paradigm shift in drug discovery

Amirian, R., Azadi Badrbani, M., Izadi, Z., Samadian, H., Bahrami, G., Sarvari, S., Abdolmaleki, S., Nabavi, S. M., Derakhshankhah, H., & Jaymand, M. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115765 · Cited by 18

A Perspective on Newly Emerging Proteolysis-Targeting Strategies in Antimicrobial Drug Discovery

Venkatesan, J., Murugan, D., & Rangasamy, L. (2022) · Antibiotics · doi:10.3390/antibiotics11121717 · Cited by 18

Targeted Degradation of Androgen Receptor by VNPP433-3β in Castration-Resistant Prostate Cancer Cells Implicates Interaction with E3 Ligase MDM2 Resulting in Ubiquitin-Proteasomal Degradation

Thomas, E. B., Thankan, R. S., Purushottamachar, P., Weber, D. J., & Njar, V. C. O. (2023) · Cancers · doi:10.3390/cancers15041198 · Cited by 20

Design and Evaluation of a Low Hydrogen Bond Donor Count Fragment Screening Set to Aid Hit Generation of PROTACs Intended for Oral Delivery

Whitehurst, B. C., Bauer, M. R., Edfeldt, F., Gunnarsson, A., Margreitter, C., Rawlins, P. B., & Storer, R. I. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00493 · Cited by 18

A Degron Blocking Strategy Towards Improved CRL4 CRBN Recruiting PROTAC Selectivity**

Bouguenina, H., Scarpino, A., O’Hanlon, J. A., Warne, J. M., Wang, H., Hak, L. C. W., Sadok, A., McAndrew, C., Stubbs, M., Pierrat, O. A., et al. (2023) · ChemBioChem · doi:10.1002/cbic.202300351 · Cited by 19

Coming of Age: Targeting Cyclin K in Cancers

Xiao, Y., & Dong, J. (2023) · Cells · doi:10.3390/cells12162044 · Cited by 19

Patent landscape of inhibitors and PROTACs of the anti-apoptotic BCL-2 family proteins

Pal, P., Zhang, P., Poddar, S. K., & Zheng, G. (2022) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2022.2116311 · Cited by 18

Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications

Li, Q., Zhou, L., Qin, S., Huang, Z., Li, B., Li, B., Yang, M., Nice, E. C., Zhu, H., & Huang, C. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115447 · Cited by 17

Recent advances of PROTACs technology in neurodegenerative diseases

Wang, C., Zhang, Y., Yang, S., & Xing, D. (2023) · Arabian Journal of Chemistry · doi:10.1016/j.arabjc.2023.105015 · Cited by 17

Recognition and reprogramming of E3 ubiquitin ligase surfaces by α-helical peptides

Tokareva, O. S., Li, K., Travaline, T. L., Thomson, T. M., Swiecicki, J., Moussa, M., Ramirez, J. D., Litchman, S., Verdine, G. L., & McGee, J. H. (2023) · Nature Communications · doi:10.1038/s41467-023-42395-z · Cited by 20

Design, synthesis, and biological evaluation of RSL3-based GPX4 degraders with hydrophobic tags

Ning, Y., Zhu, Z., Wang, Y., Fan, X., Wang, J., Qian, H., Qiu, X., & Wang, Y. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116719 · Cited by 17

Design and characterization of PROTAC degraders specific to protein N-terminal methyltransferase 1

Zhou, Q., Wu, W., Jia, K., Qi, G., Sun, X. S., & Li, P. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114830 · Cited by 18

Structural overview and perspectives of the nuclear receptors, a major family as the direct targets for<?A3B2 ACK?>small-molecule drugs

Li, F., Song, C. M., Zhang, Y., & Wu, D. (2021) · Acta Biochimica et Biophysica Sinica · doi:10.3724/abbs.2021001 · Cited by 16

Complexity‐to‐Diversity and Pseudo‐Natural Product Strategies as Powerful Platforms for Deciphering Next‐Generation Therapeutics

Alkubaisi, B. O., Shahin, A. I., Zenati, R. A., Ravi, A., Alchami, R., Alkalla, M., Khaled, R., El-Gamal, M. I., & Al‐Tel, T. H. (2023) · ChemMedChem · doi:10.1002/cmdc.202300117 · Cited by 17

Turn On, Tune In, Turnover! Target Biology Impacts In Vivo Potency, Efficacy, and Clearance

Gabrielsson, J., & Hjorth, S. (2023) · Pharmacological Reviews · doi:10.1124/pharmrev.121.000524 · Cited by 15

Emerging trends in IRAK-4 kinase research

Yadav, H. K., & Shirumalla, R. K. (2023) · Molecular Biology Reports · doi:10.1007/s11033-023-08438-w · Cited by 15

Development of PROTACS degrading KRAS and SOS1

Hamilton, G., Eggerstorfer, M.-T., & Stickler, S. (2024) · Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics · doi:10.32604/or.2024.051653 · Cited by 16

Design, synthesis, anti-tumor activity and mechanism of novel PROTACs as degraders of PD-L1 and inhibitors of PD-1/PD-L1 interaction

Zhang, F., Yu, Q., Wu, C., Sun, S., Wang, Y., Wang, Y., Zejie, C., Zhang, H., Xiong, X., Awadasseid, A., et al. (2024) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2024.117867 · Cited by 16

Degraders: The Ultimate Weapon Against Amplified Driver Kinases in Cancer

Torres‐Ayuso, P., & Brognard, J. (2022) · Molecular Pharmacology · doi:10.1124/molpharm.121.000306 · Cited by 15

Feasible Column Chromatography-Free, Multi-Gram Scale Synthetic Process of VH032 Amine, Which Could Enable Rapid PROTAC Library Construction

Yan, W., Pan, B., Shao, J., Lin, H.-K., & Li, H. (2022) · ACS Omega · doi:10.1021/acsomega.2c00245 · Cited by 15

A Versatile Bioorthogonal Theranostic Platform Enables Relay Activation of Tumor Cell Imaging and Targeted Protein Degradation

Sun, F., Wang, T., Wang, P., Shi, J., Shen, Y., Wang, G., Yang, B., Li, H., Zhang, Q., Chen, Y., et al. (2025) · Journal of the American Chemical Society · doi:10.1021/jacs.5c11564 · Cited by 15

Advancing targeted protein degrader discovery by measuring cereblon engagement in cells

Zerfas, B. L., Huerta, F., Liu, H., Du, G., Gray, N. S., Jones, L. H., & Nowak, R. P. (2022) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/bs.mie.2022.08.013 · Cited by 14

Degradation of extracellular and membrane proteins in targeted therapy: Status quo and quo vadis

Li, Z., Ma, S., Zhang, S., Ma, Z., Du, L., & Li, M. (2023) · Drug Discovery Today · doi:10.1016/j.drudis.2023.103716 · Cited by 14

ASPSCR1-TFE3 reprograms transcription by organizing enhancer loops around hexameric VCP/p97

Pozner, A., Li, L., Verma, S. P., Wang, S., Barrott, J. J., Nelson, M. L., Yu, J. S. E., Negri, G. L., Colborne, S., Hughes, C. S., et al. (2024) · Nature Communications · doi:10.1038/s41467-024-45280-5 · Cited by 15

Discovery of Potent Dual PROTAC Degraders Targeting BET-Kinase To Overcome FLT3 Inhibitor Resistance

Xiang, Q., Sun, Y., Hua, H., Hu, M., Li, X., Guo, M., Niu, L., Zhang, Z., Cai, T., & Zhu, D. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00831 · Cited by 13

Synthesis of Lathyrol PROTACs and Evaluation of Their Anti-Inflammatory Activities

Wang, W., Liu, Y., Xiong, L., Sun, D., Wang, H., Song, Z., Li, Y., Li, H., & Chen, L. (2023) · Journal of Natural Products · doi:10.1021/acs.jnatprod.2c00912 · Cited by 13

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 · doi:10.1002/ange.202308049 · Cited by 14

Discovery of a Promising CBP/p300 Degrader XYD129 for the Treatment of Acute Myeloid Leukemia

Wu, T., Hu, J., Zhao, X., Zhang, C., Dong, R., Hu, Q., Xu, H., Shen, H., Zhang, X., Zhang, Y., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00335 · Cited by 14

Precise Modulation of Protein Degradation by Smart PROTACs

Cheng, J., Dong, G., Wang, W., & Sheng, C. (2024) · ChemBioChem · doi:10.1002/cbic.202400682 · Cited by 13

Small-Molecule Degraders of Cyclin-Dependent Kinase Protein: A Review

Yu, B., Du, Z., Zhang, Y., Li, Z., & Bian, J. (2021) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0154 · Cited by 14

Targeted Protein Degradation: An Important Tool for Drug Discovery for “Undruggable” Tumor Transcription Factors

Dai, M., Sridhar, R., Li, R., Tan, R., Yan, K., Fan, G., & Liu, M. (2022) · Technology in Cancer Research & Treatment · doi:10.1177/15330338221095950 · Cited by 14

Applications and Limitations of Oxime‐Linked “Split PROTACs”

Gui, W., & Kodadek, T. J. (2022) · ChemBioChem · doi:10.1002/cbic.202200275 · Cited by 14

A novel inhibitor of ARfl and ARv7 induces protein degradation to overcome enzalutamide resistance in advanced prostate cancer

Li, Y., Chu, Y., Shi, G., Wang, X., Ye, W., Shan, C., Wang, D., Zhang, D., He, W., Jiang, J., et al. (2022) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2022.05.003 · Cited by 12

Discovery of a Chemical Probe to Study Implications of BPTF Bromodomain Inhibition in Cellular and in vivo Experiments

Martinelli, P., Schaaf, O., Mantoulidis, A., Martin, L. J., Fuchs, J. E., Bader, G., Gollner, A., Wolkerstorfer, B., Rogers, C. M., Balıkçı, E., et al. (2023) · ChemMedChem · doi:10.1002/cmdc.202200686 · Cited by 12

Degradation of MK2 with natural compound andrographolide: A new modality for anti-inflammatory therapy

Tran, Q. T. N., Gan, P. X. L., Liao, W., Mok, Y., Chai, C. L. L., & Wong, W. S. F. (2023) · Pharmacological Research · doi:10.1016/j.phrs.2023.106861 · Cited by 12

Review of the impact of fragment-based drug design on PROTAC degrader discovery

Chen, P., Li, Q., & Lei, X. (2024) · TrAC Trends in Analytical Chemistry · doi:10.1016/j.trac.2024.117539 · Cited by 13

MEGA PROTAC, MEGA DOCK-based PROTAC mediated ternary complex formation pipeline with sequential filtering and rank aggregation

Ugurlu, S. Y., McDonald, D., Enisoglu, R., Zhu, Z., & He, S. (2025) · Scientific Reports · doi:10.1038/s41598-024-83558-2 · Cited by 12

Engineered PROTAC-CID Systems for Mammalian Inducible Gene Regulation

Ma, D., Yuan, Q., Peng, F., Paredes, V., Zeng, H., Osikpa, E. C., Yang, Q., Peddi, A., Patel, A., Liu, M. S., et al. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c09129 · Cited by 14

The human E3 ligase RNF185 is a regulator of the SARS-CoV-2 envelope protein

Zou, C., Yoon, H., Park, P. M. C., Patten, J. J., Pellman, J., Carreiro, J., Tsai, J. M., Li, Y.-D., Burman, S. S. R., Donovan, K. A., et al. (2023) · iScience · doi:10.1016/j.isci.2023.106601 · Cited by 12

Native Mass Spectrometry: Insights and Opportunities for Targeted Protein Degradation

Sternicki, L. M., & Poulsen, S. (2023) · Analytical Chemistry · doi:10.1021/acs.analchem.3c03853 · Cited by 12

A one-pot photocatalytic triazole-based linkerology for PROTACs

Liu, J., Deng, Y., Yin, J., Ji, J., Guan, C., Chen, X., Wu, X., Zhu, T., & Liu, S. (2024) · Cell Reports Physical Science · doi:10.1016/j.xcrp.2024.102139 · Cited by 11

Modulation of OGG1 enzymatic activities by small molecules, promising tools and current challenges

Renaudin, X., & Campalans, A. (2025) · DNA repair · doi:10.1016/j.dnarep.2025.103827 · Cited by 13

Research Progress in Targeting GSPT1: Molecular Glues, Bifunctional Degraders, and Antibody-Enabled Molecular Glues for Cancer Therapy

Cheng, B., Wang, Y., Hong, Y., Zhou, Y., Chen, J., & Zeng, C. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00783 · Cited by 11

Crystallizing the Uncrystallizable: Insights from Extensive Screening of PROTACs

Screen, M. A., McCabe, J. F., Askin, S., Guest, J. L., Hodgkinson, P., Cabeza, A. J. C., Blundell, T. J., Rainer, D. N., Coles, S. J., Longcake, A., et al. (2025) · Journal of the American Chemical Society · doi:10.1021/jacs.5c07977 · Cited by 11

Proteome-Wide Discovery of Degradable Proteins Using Bifunctional Molecules

Forrest, I., Conway, L. P., Gathmann, C., Jadhav, A. M., Chiu, T.-Y., Chaheine, C. M., Estrada, M. A., Shrestha, A., Sarris, K., Reitsma, J. M., et al. (2025) · ACS Central Science · doi:10.1021/acscentsci.5c01594 · Cited by 12

Heterobifunctional Ligase Recruiters Enable pan-Degradation of Inhibitor of Apoptosis Proteins

Ng, Y. L. D., Bricelj, A., Jansen, J. A., Murgai, A., Peter, K., Donovan, K. A., Gütschow, M., Krönke, J., Steinebach, C., & Sosič, I. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01817 · Cited by 10

Perspectives on the Development of First-in-Class Protein Degraders

Rambacher, K. M., Calabrese, M. F., & Yamaguchi, M. (2021) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0033 · Cited by 11

New therapeutic modalities in drug discovery and development: Insights & opportunities

Kansy, M., & Caron, G. (2021) · ADMET & DMPK · doi:10.5599/admet.1209 · Cited by 11

Constitutive protein degradation induces acute cell death via proteolysis productsPreprint

Chen, S., Prakash, S., Helgason, E., Gilchrist, C. L., Kenner, L. R., Srinivasan, R., Sterne‐Weiler, T., Hafner, M. A., Piskol, R., Dueber, E. C., et al. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.02.06.527237 · Cited by 11

Discovery and Characterization of PROTACs Targeting Tissue Transglutaminase (TG2)

Valdivia, A., Vagadia, P. P., Guo, G., O’Brien, E., Matei, D. E., & Schiltz, G. E. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01859 · Cited by 10

Redirecting the specificity of tripartite motif containing-21 scaffolds using a novel discovery and design approach

VanDyke, D., Xu, L., Sargunas, P. R., Gilbreth, R. N., Baca, M., Gao, C., Hunt, J., & Spangler, J. B. (2023) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2023.105381 · Cited by 10

Degrading mutant IDH1 employing a PROTAC-based approach impairs STAT3 activation

Dutta, H., & Jain, N. (2025) · Archives of Biochemistry and Biophysics · doi:10.1016/j.abb.2024.110281 · Cited by 10

Exploitation of Proximity-Mediated Effects in Drug Discovery: An Update of Recent Research Highlights in Perturbing Pathogenic Proteins and Correlated Issues

Zhao, C., Wang, H., Zhan, W., Lv, X., & Ma, X. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00079 · Cited by 9

Next-generation strategies to improve safety and efficacy of adeno-associated virus-based gene therapy for hemophilia: lessons from clinical trials in other gene therapies

Minno, G. D., Miesbach, W., Castaman, G., & Peyvandi, F. (2024) · Haematologica · doi:10.3324/haematol.2023.284622 · Cited by 13

Harnessing the Power of Natural Products for Targeted Protein Degradation

Zhu, B., Wu, Z., Shou, Y., Zhao, K., Lu, Q., Qin, J., & Guo, H. (2025) · Medicinal Research Reviews · doi:10.1002/med.22113 · Cited by 12

The Impact of Continuous Flow Technology and Collaboration between Academia and Industry

Jamieson, P., Bannon, R., Cronly, D., Smyth, M., Wharry, S., Moody, T. S., Lennon, G., & Baumann, M. (2026) · JACS Au · doi:10.1021/jacsau.5c01617 · Cited by 10

Dégradation induite des protéines par des molécules PROTAC et stratégies apparentées : développements à visée thérapeutique

Reboud‐Ravaux, M. (2021) · Biologie Aujourd hui · doi:10.1051/jbio/2021007 · Cited by 10

From DNA Copy Number Gains and Tumor Dependencies to Novel Therapeutic Targets for High-Risk Neuroblastoma

Decaesteker, B., Durinck, K., Roy, N. V., Wilde, B. D., Neste, C. V., Haver, S. V., Roberts, S. S., Preter, K. D., Vermeirssen, V., & Speleman, F. (2021) · Journal of Personalized Medicine · doi:10.3390/jpm11121286 · Cited by 9

Intracellular Degradation of SARS-CoV-2 N-Protein Caused by Modular Nanotransporters Containing Anti-N-Protein Monobody and a Sequence That Recruits the Keap1 E3 Ligase

Khramtsov, Y. V., Ulasov, A. V., Lupanova, T. N., Slastnikova, T. A., Rosenkranz, A. A., Bunin, E. S., Georgiev, G. P., & Sobolev, A. S. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics16010004 · Cited by 8

Discovery of novel penetrating peptides able to target human leukemia and lymphoma for enhanced PROTAC delivery

Zhang, Q., Liu, Y., Zhang, J., Li, Y., Wang, J., Li, Y., Wang, J., & Pan, X. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116734 · Cited by 10

Lysosome-Targeting Chimeras: Design, Mechanisms, and Degradation of “Rogue” Proteins

Rehman, M. U., Wu, X., Chen, Q., Liu, Z., & Long, S. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.109249 · Cited by 8

Discovery of a Series of Orally Bioavailable Androgen Receptor Degraders for the Treatment of Prostate Cancer

Bagal, S. K., Astles, P. C., Diène, C. R., Argyrou, A., Crafter, C., Cassar, D. J., Fallan, C., Hock, A., Jones, T., Moreau, K., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00269 · Cited by 8

Discovery of a New and Selective HPK1 PROTAC for Enhancing Tumor Immunotherapy through Eliminating GLK Degradation

Wu, M., Mao, X., Wu, Y., Wang, W.-T., Jin, Y., Yu, H., Hu, L., Shen, Z., Shen, L., Zeng, S., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c02972 · Cited by 9

New Frontiers in the Discovery and Development of PROTACs

Barghout, S. H. (2022) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/1871520622666220412132759 · Cited by 8

PROTAC Degraders

Ciulli, A., & Hsia, O. (2022) · Wiley eBooks · doi:10.1002/9781119774198.ch9 · Cited by 8

Applications of contemporary tools to measure plasma protein binding of targeted protein degraders

Niosi, M., Zhang, S., Burchett, W., Heck, C. J. S., Goetz, G. H., Federico, J. J., Gernhardt, S., Jordan, S., Gilbert, A. M., Calabrese, M. F., et al. (2025) · Drug Metabolism and Disposition · doi:10.1016/j.dmd.2025.100066 · Cited by 7

Targeted protein degradation with small molecules for cancer immunotherapy

Yang, Z., Xu, J., Yang, X., & Chen, J. (2025) · Asian Journal of Pharmaceutical Sciences · doi:10.1016/j.ajps.2025.101058 · Cited by 7

PROTACs in Antivirals: Current Advancements and Future Perspectives

Jin, J., Quan, M., Cao, X., Zhang, Y., Xu, X., & Wang, Z. (2025) · Molecules · doi:10.3390/molecules30163402 · Cited by 8

Developing Multi-Component Solid Formulation Strategies for PROTAC Dissolution Enhancement

Screen, M. A., Askin, S., McCabe, J. F., Jacobs, E., Anane‐Adjei, A. B., Mahon, C. S., Wilson, M. R., & Steed, J. W. (2025) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.5c01107 · Cited by 7

A Phenotypic Approach for the Identification of New Molecules for Targeted Protein Degradation Applications

Stacey, P., Lithgow, H., Lewell, X. Q., Konopacka, A., Besley, S., Green, G., Whatling, R., Law, R. P., Röth, S., Sapkota, G. P., et al. (2021) · SLAS DISCOVERY · doi:10.1177/24725552211017517 · Cited by 7

Recent breakthroughs in innovative elements, multidimensional enhancements, derived technologies, and novel applications of PROTACs

Zhang, S.-H., Zeng, N., Xu, J., Liu, C., Xu, M., Sun, J., An, Y., Zhong, X., Miao, L.-T., Wang, S., et al. (2024) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2024.117584 · Cited by 9

DUB be good to me

Liu, X., & Ciulli, A. (2022) · Nature Chemical Biology · doi:10.1038/s41589-022-00978-9 · Cited by 7

Developing PROteolysis TArgeting Chimeras (PROTACs) for hematologic malignancies

Wu, Y., Zhang, J., Zhu, X., & Zhang, Y. (2022) · Cancer Letters · doi:10.1016/j.canlet.2022.215808 · Cited by 8

Capsule-based automated synthesis for the efficient assembly of PROTAC like molecules

Bordi, S., Jiang, T., Konopka, A., Coin, G., Nichols, P. L., & Wanner, B. M. (2023) · Digital Discovery · doi:10.1039/d3dd00027c · Cited by 8

Circular RNAs With Efficacy in PreclinicalIn VitroandIn VivoModels of Esophageal Squamous Cell Carcinoma

Weidle, U. H., Sela, T., Brinkmann, U., & Niewoehner, J. (2022) · Cancer Genomics & Proteomics · doi:10.21873/cgp.20320 · Cited by 7

Harnessing targeted protein degradation to potentiate cancer immunotherapy: from molecular mechanisms to delivery strategies

Liu, Y., Ullah, I., Yuan, Y., & Wang, J. (2026) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2026.115776 · Cited by 6

Methods to Study the Molecular Mechanism and Drive the Design of Protein Degraders

Crowe, C., & Ciulli, A. (2026) · Chemical Reviews · doi:10.1021/acs.chemrev.5c00800 · Cited by 6

Identification of non-conventional small molecule degraders and stabilizers of squalene synthase

Hoock, J., Rossetti, C., Bilgin, M., Depta, L., Enemark‐Rasmussen, K., Christianson, J. C., & Laraia, L. (2023) · Chemical Science · doi:10.1039/d3sc04064j · Cited by 6

Discovery of an activatable near-infrared fluorescent and theranostic PROTAC for tumor-targeted detecting and degrading of BRD4

Li, K., Dong, G., Wu, S., & Sheng, C. (2024) · Chinese Chemical Letters · doi:10.1016/j.cclet.2024.110280 · Cited by 6

Endosome-microautophagy targeting chimera (eMIATAC) for targeted proteins degradation and enhance CAR-T cell anti-tumor therapy

Lei, K., Li, J., Tu, Z., Gong, C., Liu, J., Luo, M. H., Ai, W., Wu, L., Li, Y., Zhou, Z., et al. (2024) · Theranostics · doi:10.7150/thno.98574 · Cited by 6

Targeted protein degradation in autoimmune diseases: from mechanisms to therapeutic breakthroughs

Song, Y., Zhou, B., Long, J., & Peng, Y. (2025) · Journal of Autoimmunity · doi:10.1016/j.jaut.2025.103475 · Cited by 7

Ion channel inhibition by targeted recruitment of NEDD4-2 with divalent nanobodies

Darko-Boateng, A., Afriyie, E., Morgenstern, T. J., Shanmugam, S. K., Zou, X., Laloudakis, Y. D., Choudhury, P., Desai, M., Kass, R. S., Vallese, F., et al. (2025) · Nature Communications · doi:10.1038/s41467-025-67068-x · Cited by 8

Leveraging high-throughput proteomics and AI-based protein folding to accelerate VAV1 molecular glue discovery

Lin, H., Yu, X., Haiyang, Cheng, R., Zhang, M., Qi, X., Yang, Y., Zhou, S., Qi, R., Le, L., et al. (2026) · Nature Communications · doi:10.1038/s41467-026-77657-z · Cited by 8

Probing the CRL4DCAF12 interactions with MAGEA3 and CCT5 di-Glu C-terminal degrons

Righetto, G. L., Yin, Y., Duda, D. M., Vu, V., Szewczyk, M. M., Zeng, H., Li, Y., Loppnau, P., Mei, T., Li, Y.-Y., et al. (2024) · PNAS Nexus · doi:10.1093/pnasnexus/pgae153 · Cited by 5

E3Docker: a docking server for potential E3 binder discovery

Yan, K., He, W., Pang, M., Lu, X., Chen, Z., Piao, L., Zhang, H., Wang, Y., Chang, S., & Kong, R. (2025) · Nucleic Acids Research · doi:10.1093/nar/gkaf391 · Cited by 5

Drug Hunting at the Nexus of Medicinal Chemistry and Chemical Biology and the Discovery of Novel Therapeutic Modalities

Palacios, D. S. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01491 · Cited by 5

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

Zhang, L., Li, L., Wang, X., Liu, H., Zhang, Y., Xie, T., Zhang, H., Li, X., Peng, T., Sun, X., et al. (2021) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2021.08.05.455211 · Cited by 5

PROTAC-powered synergistic tumor therapy

Wang, X., Zou, J., Tao, Y., Zhou, Z., Bian, C., Mao, Z., & Liu, Z. (2026) · TrAC Trends in Analytical Chemistry · doi:10.1016/j.trac.2026.118678 · Cited by 4

P4ward: An Automated Modeling Platform for Protac Ternary Complexes

Jofily, P., & Kalyaanamoorthy, S. (2025) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.5c00614 · Cited by 7

Targeted protein degradation in pancreatic cancer: advances and challenges of PROTAC-based therapeutics

Huang, M., Wei, F., Cao, J., & Jiang, H. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.108985 · Cited by 4

Proteostasis of immune checkpoint receptors

Tey, P. Y., Urbé, S., & Clague, M. J. (2025) · Biochemical Journal · doi:10.1042/bcj20253299 · Cited by 4

Potent and Selective IGF‐IIR‐Recruiting Bifunctional Molecules for Targeted Lysosomal Degradation of Extracellular and Membrane Proteins

Zhao, Y., Liao, Y., Li, P., de Gonzalez, R. S., Chen, X., Nieto, N. S., Brunel, F. M., Cox, N., Stock, J. R., McHenry, M., et al. (2026) · Advanced Science · doi:10.1002/advs.202518793 · Cited by 4

An ultrasound-activated PROTAC prodrug with self-reporting fluorescence for targeted protein degradation

Li, T., Tu, Y., Dong, H., Xie, W., Pan, X., & Yuan, Y. (2026) · Biomaterials · doi:10.1016/j.biomaterials.2026.124045 · Cited by 5

Targeted degradation of BRD4 by PROTACs: advances in cancer therapy

Hong, Y., Liu, X., Li, Y., Yu, M., Wang, C., Nie, C., & Xu, S. (2026) · Chemical Communications · doi:10.1039/d5cc05563f · Cited by 5

From undruggable to degradable: Strategic expansion of targeted protein degradation in cancer therapy

Sung, J., Seo, Y., & Lee, J.-Y. (2026) · Molecular Therapy · doi:10.1016/j.ymthe.2026.05.031 · Cited by 4

Drugit: crowd-sourcing molecular design of non-peptidic VHL binders

Scott, T., Smethurst, C. A., Westermaier, Y., Mayer, M., Greb, P., Kousek, R., Biberger, T., Bader, G., Jandová, Z., Schmalhorst, P. S., et al. (2025) · Nature Communications · doi:10.1038/s41467-025-58406-0 · Cited by 4

VRK1 is required in VRK2-methylated cancers of the nervous systemPreprint

So, J., Mabe, N. W., Englinger, B., Moyer, S. M., Trissal, M. C., Marques, J. G., Kwon, J. J., Shim, B. H., Panditharatna, E., Jeong, D., et al. (2021) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2021.12.28.474386 · Cited by 4

Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activityPreprint

Sinatra, L., Yang, J., Schliehe‐Diecks, J., Dienstbier, N., Vogt, M., Gebing, P., Bachmann, L. M., Sönnichsen, M., Lenz, T., Stühler, K., et al. (2022) · ChemRxiv · doi:10.26434/chemrxiv-2022-dntx4-v2 · Cited by 5

A triple-action PROTAC for wild-type p53 cancer therapy

Bird, G. H., Adhikary, U., Schmidt, M. J., Godes, M., Tesar, B. M., Camara, C. M., Paulo, J. A., Vidlak, J. F., DeAngelo, T. M., Marquez, M., et al. (2025) · Cell Reports Medicine · doi:10.1016/j.xcrm.2025.102467 · Cited by 4

E3 ubiquitin ligases: structural diversity, dysregulation in disease, and their emerging role in targeted therapeutic strategies

Sriram, S., Krishnakumar, P., & Sudandiradoss, C. (2026) · Frontiers in Molecular Biosciences · doi:10.3389/fmolb.2026.1745654 · Cited by 3

Protein degraders push into novel target space

Mullard, A. (2024) · Nature Reviews Drug Discovery · doi:10.1038/d41573-024-00170-9 · Cited by 18

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

Targeted protein degraders - new modalities for drug discovery

Hatakeyama, H. (2026) · Drug Delivery System · doi:10.2745/dds.41.93

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

Wang, C., Guo, Z., Liu, Y., Gao, Q., Wang, Q., Liu, Y., & Liu, Y. (2026) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2026.127323

Targeted protein degradation comes of age

Matyskiela, M. E. (2024) · Nature Chemical Biology · doi:10.1038/s41589-024-01789-w · Cited by 3