Targeted protein degraders crowd into the clinic

Discovery of a potent and selective proteolysis targeting chimera (PROTAC) degrader of NSD3 histone methyltransferase

Sun, Y., Zhang, Y., Chen, X., Yu, A., Du, W., Huang, Y., Wu, F., Yu, L., Li, J., Wen, C., et al. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114528 · Cited by 49

Marine Arthropods as a Source of Antimicrobial Peptides

Saucedo-Vázquez, J. P., Gushque, F., Vispo, N. S., Rodríguez, J. A., Gomezjurado, M. E. G., Alberício, F., Tellkamp, M. P., & Alexis, F. (2022) · Marine Drugs · doi:10.3390/md20080501 · Cited by 48

A Cell-Permeant Nanobody-Based Degrader That Induces Fetal Hemoglobin

Shen, F., Zheng, G., Setegne, M. T., Tenglin, K., Izadi, M., Xie, H. T. H., Zhai, L., Orkin, S. H., & Dassama, L. M. K. (2022) · ACS Central Science · doi:10.1021/acscentsci.2c00998 · Cited by 49

Supramolecular artificial Nano-AUTACs enable tumor-specific metabolism protein degradation for synergistic immunotherapy

Wang, Y., Yang, L., Yan, C., Du, Y., Li, T., Yang, W., Lei, L., He, B., Gao, H., Peppas, N. A., et al. (2024) · Science Advances · doi:10.1126/sciadv.adn8079 · Cited by 48

Biophysical and Computational Approaches to Study Ternary Complexes: A ‘Cooperative Relationship’ to Rationalize Targeted Protein Degradation

Ward, J. A., Perez‐Lopez, C., & Mayor‐Ruiz, C. (2023) · ChemBioChem · doi:10.1002/cbic.202300163 · Cited by 48

The cyclimids: Degron-inspired cereblon binders for targeted protein degradation

Ichikawa, S., Payne, N. C., Xu, W., Chang, C., Vallavoju, N., Frome, S., Flaxman, H. A., Mazitschek, R., & Woo, C. M. (2024) · Cell chemical biology · doi:10.1016/j.chembiol.2024.01.003 · Cited by 49

Powering up targeted protein degradation through active and passive tumour-targeting strategies: Current and future scopes

Venkatesan, J., Murugan, D., Lakshminarayanan, K., Smith, A. R., Thirumalaiswamy, H. V., Kandhasamy, H., Zender, B., Zheng, G., & Rangasamy, L. (2024) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2024.108725 · Cited by 48

Selectivity through Targeted Protein Degradation (TPD)

Gopalsamy, A. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00397 · Cited by 45

VRK1 as a synthetic lethal target in VRK2 promoter-methylated cancers of the nervous system

So, J., Mabe, N. W., Englinger, B., Chow, K.-H., Moyer, S. M., Yerrum, S., Trissal, M. C., Marques, J. G., Kwon, J. J., Shim, B., et al. (2022) · JCI Insight · doi:10.1172/jci.insight.158755 · Cited by 45

Targeting key proteins involved in transcriptional regulation for cancer therapy: Current strategies and future prospective

Pei, H., Guo, W., Peng, Y., Xiong, H., & Chen, Y. (2022) · Medicinal Research Reviews · doi:10.1002/med.21886 · Cited by 45

Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation

Yan, J., Li, T., Miao, Z., Wang, P., Sheng, C., & Zhuang, C. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00728 · Cited by 46

PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models

Berlin, M. Y., Cantley, J. L., Bookbinder, M., Bortolon, E., Broccatelli, F., Cadelina, G., Chan, E. W., Chen, H., Chen, X., Cheng, Y., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01781 · Cited by 43

Development of miRNA-based PROTACs targeting Lin28 for breast cancer therapy

Xu, J., Zhao, X., Liang, X., Guo, D., Wang, J., Wang, Q., & Tang, X. (2024) · Science Advances · doi:10.1126/sciadv.adp0334 · Cited by 44

Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer

Sun, N., Kabir, M., Lee, Y., Xie, L., Hu, X., Velez, J., Chen, X., Kanıskan, H. Ü., & Jin, J. J. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01505 · Cited by 43

The application of PROTAC in HDAC

Chen, S., Zheng, Y., Liang, B., Yin, Y., Yao, J., Wang, Q., Liu, Y., & Neamati, N. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115746 · Cited by 45

PAC1 receptor–mediated clearance of tau in postsynaptic compartments attenuates tau pathology in mouse brain

Schaler, A. W., Runyan, A. M., Clelland, C. L. T., Sydney, E. J., Fowler, S. L., Figueroa, H. Y., Shioda, S., Santa‐María, I., Duff, K., & Myeku, N. (2021) · Science Translational Medicine · doi:10.1126/scitranslmed.aba7394 · Cited by 41

Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity

Desantis, J., Bazzacco, A., Eleuteri, M., Tuci, S., Bianconi, E., Macchiarulo, A., Mercorelli, B., Loregian, A., & Goracci, L. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116202 · Cited by 41

Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs

Ermondi, G., Jiménez, D. G., Sebastiano, M. R., & Caron, G. (2021) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.1c00298 · Cited by 40

Options to Improve the Action of PROTACs in Cancer: Development of Controlled Delivery Nanoparticles

Juan, A., Noblejas‐López, M. D. M., Arenas-Moreira, M., Alonso‐Moreno, C., & Ocaña, A. (2022) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.805336 · Cited by 39

Targeted Protein Degradation Technology and Nanomedicine: Powerful Allies against Cancer

Lin, J., Liu, H., Wu, Y., Jin, J., Zhou, Y., Zhang, H., Nagle, D. G., Chen, H., Zhang, W., & Luan, X. (2023) · Small · doi:10.1002/smll.202207778 · Cited by 38

BRD9 Degradation Disrupts Ribosome Biogenesis in Multiple Myeloma

Kurata, K., Samur, M., Liow, P., Wen, K., Yamamoto, L., Liu, J., Morelli, E., Gullà, A., Tai, Y., Qi, J., et al. (2023) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-22-3668 · Cited by 40

Substrate and Functional Diversity of Protein Lysine Post-translational Modifications

Hao, B., Chen, K., Zhai, L., Liu, M., Liu, B., & Tan, M. (2024) · Genomics Proteomics & Bioinformatics · doi:10.1093/gpbjnl/qzae019 · Cited by 41

DiffPROTACs is a deep learning-based generator for proteolysis targeting chimeras

Li, F., Hu, Q., Zhou, Y., Yang, H., & Bai, F. (2024) · Briefings in Bioinformatics · doi:10.1093/bib/bbae358 · Cited by 42

Light-Controllable PROTACs for Temporospatial Control of Protein Degradation

Liu, J., Peng, Y., & Wei, W. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.678077 · Cited by 38

Designing HDAC-PROTACs: Lessons Learned So Far

Fischer, F., Avelar, L. A. A., Murray, L., & Kurz, T. (2021) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0206 · Cited by 38

Addressing the Enzyme-independent tumor-promoting function of NAMPT via PROTAC-mediated degradation

Zhu, X., Liu, H., Chen, L., Wu, C., Liu, X., Cang, Y., Jiang, B., Yang, X., & Fan, G. (2022) · Cell chemical biology · doi:10.1016/j.chembiol.2022.10.007 · Cited by 38

Targeted protein degradation at the host–pathogen interface

Grohmann, C., Marapana, D. S., & Ebert, G. (2021) · Molecular Microbiology · doi:10.1111/mmi.14849 · Cited by 38

Discovery of Highly Potent Nicotinamide Phosphoribosyltransferase Degraders for Efficient Treatment of Ovarian Cancer

Bi, K., Cheng, J., He, S., Fang, Y., Huang, M., Sheng, C., & Dong, G. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01990 · Cited by 38

Targeted Protein Degradation (TPD) for Immunotherapy: Understanding Proteolysis Targeting Chimera-Driven Ubiquitin-Proteasome Interactions

Kamaraj, R., Ghosh, S., Das, S., Sen, S., Kumar, P. R., Majumdar, M., Dasgupta, R., Mukherjee, S., Das, S., Ghose, I., et al. (2024) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.4c00253 · Cited by 37

Targeted protein degradation: current molecular targets, localization, and strategies

Pliatsika, D., Blatter, C., & Riedl, R. (2024) · Drug Discovery Today · doi:10.1016/j.drudis.2024.104178 · Cited by 40

PROTAC Degrader of Estrogen Receptor α Targeting DNA-Binding Domain in Breast Cancer

Zhang, X., Zhang, Z., Xue, X., Fan, T., Tan, C., Liu, F., Tan, Y. C., & Jiang, Y. (2022) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.2c00109 · Cited by 38

PROTAC: targeted drug strategy. Principles and limitations

Koroleva, O. A., Dutikova, Y. V., Trubnikov, A. V., Zenov, F. A., Manasova, E. V., Shtil, A. A., & Kurkin, A. V. (2022) · Russian Chemical Bulletin · doi:10.1007/s11172-022-3659-z · Cited by 38

Small-molecule PIK-93 modulates the tumor microenvironment to improve immune checkpoint blockade response

Lin, C., Huang, K., Kao, S.-H., Lin, M.-S., Lin, C.-C., Yang, S., Chung, W.-C., Chang, Y.-H., Chein, R., & Yang, P. (2023) · Science Advances · doi:10.1126/sciadv.ade9944 · Cited by 37

RAS degraders: The new frontier for RAS-driven cancers

Escher, T. E., & Satchell, K. J. F. (2023) · Molecular Therapy · doi:10.1016/j.ymthe.2023.03.017 · Cited by 36

Lowering low-density lipoprotein cholesterol: from mechanisms to therapies

Luo, J., Wang, J.-K., & Song, B. (2022) · Life Metabolism · doi:10.1093/lifemeta/loac004 · Cited by 37

NRX-0492 degrades wild-type and C481 mutant BTK and demonstrates in vivo activity in CLL patient-derived xenografts

Zhang, D., Harris, H. M., Chen, J., Judy, J., James, G., Kelly, A., McIntosh, J., Tenn-McClellan, A., Ambing, E., Tan, Y. S., et al. (2023) · Blood · doi:10.1182/blood.2022016934 · Cited by 35

Discovery of Novel PDEδ Autophagic Degraders: A Case Study of Autophagy-Tethering Compound (ATTEC)

Bao, J., Chen, Z., Li, Y., Chen, L., Wang, W., Sheng, C., & Dong, G. (2023) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.3c00161 · Cited by 36

Gene regulation technologies for gene and cell therapy

Butterfield, G. L., Reisman, S. J., Iglesias, N., & Gersbach, C. A. (2025) · Molecular Therapy · doi:10.1016/j.ymthe.2025.04.004 · Cited by 43

Discovery and characterization of novel potent BCR-ABL degraders by conjugating allosteric inhibitor

Liu, H., Mi, Q., Ding, X., Lin, C., Liu, L., Ren, C., Shen, S., Shao, Y., Chen, J., Zhou, Y., et al. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114810 · Cited by 36

Key Considerations in Targeted Protein Degradation Drug Discovery and Development

Qin, L., Dai, H., & Wang, J. (2022) · Frontiers in Chemistry · doi:10.3389/fchem.2022.934337 · Cited by 35

Aptamers: Promising Reagents in Biomedicine Application

Zhou, H., Li, Y., & Wu, W. (2024) · Advanced Biology · doi:10.1002/adbi.202300584 · Cited by 37

The interplay between non-coding RNAs and alternative splicing: from regulatory mechanism to therapeutic implications in cancer

Liu, M., Zhang, S., Zhou, H., Hu, X., Li, J., Fu, B., Wei, M., Huang, H., & Wu, H. (2023) · Theranostics · doi:10.7150/thno.83920 · Cited by 36

Regulated Induced Proximity Targeting Chimeras (RIPTACs): a Novel Heterobifunctional Small Molecule Therapeutic Strategy for Killing Cancer Cells SelectivelyPreprint

Raina, K., Forbes, C. D., Stronk, R., Rappi, J. P., Eastman, K. J., Gerritz, S. W., Yu, X., Li, H., Bhardwaj, A., Forgione, M., et al. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.01.01.522436 · Cited by 34

Development of a GC-376 Based Peptidomimetic PROTAC as a Degrader of 3-Chymotrypsin-like Protease of SARS-CoV-2

Grifagni, D., Lenci, E., Santis, A. D., Orsetti, A., Barracchia, C. G., Tedesco, F., Puglielli, R. B., Lucarelli, F., Lauriola, A., Assfalg, M., et al. (2024) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.3c00498 · Cited by 33

An updated patent review of BRD4 degraders

Ma, Z., Zhang, C., Bolinger, A. A., & Zhou, J. (2024) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2024.2400166 · Cited by 35

Mathematical Model for Covalent Proteolysis Targeting Chimeras: Thermodynamics and Kinetics Underlying Catalytic Efficiency

Chaudhry, C. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c02076 · Cited by 35

Epidermal growth factor receptor PROTACs as an effective strategy for cancer therapy: A review

Wang, C., Zhang, Y., Chen, W., Wang, Y., & Xing, D. (2023) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2023.188927 · Cited by 34

Chemical Probes for Understudied Kinases: Challenges and Opportunities

Serafim, R. A. M., Elkins, J. M., Zuercher, W. J., Laufer, S., & Gehringer, M. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00980 · Cited by 32

Progress of small molecules for targeted protein degradation: PROTACs and other technologies

Zhao, H., Xin, M., & Zhang, S. (2023) · Drug Development Research · doi:10.1002/ddr.22026 · Cited by 31

Unifying Catalysis Framework to Dissect Proteasomal Degradation Paradigms

Rodriguez-Rivera, F. P., & Levi, S. M. (2021) · ACS Central Science · doi:10.1021/acscentsci.1c00389 · Cited by 30

The BAF chromatin remodeling complexes: structure, function, and synthetic lethalities

Varga, J., Kube, M., Luck, K., & Schick, S. (2021) · Biochemical Society Transactions · doi:10.1042/bst20190960 · Cited by 31

Novel therapeutic approaches to target neurodegeneration

de la Fuente, A. G., Pelucchi, S., Mertens, J., Luca, M. D., Mauceri, D., & Marcello, E. E. (2023) · British Journal of Pharmacology · doi:10.1111/bph.16078 · Cited by 32

PROTACs in the Management of Prostate Cancer

Poornachandra, Y., Babalghith, A. O., Andra, V. V., & Syed, R. (2023) · Molecules · doi:10.3390/molecules28093698 · Cited by 31

Current strategies for improving limitations of proteolysis targeting chimeras

Pu, C., Wang, S., Liu, L., Feng, Z., Zhang, H., Gong, Q., Sun, Y., Guo, Y., & Li, R. (2022) · Chinese Chemical Letters · doi:10.1016/j.cclet.2022.107927 · Cited by 32

Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders

Lu, J., Huang, Y.-J., Huang, J., He, R. R., Huang, M., Lu, X., Xu, Y., Zhou, F., Zhang, Z., & Ding, K. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01768 · Cited by 29

Small-Molecule PROTACs for Cancer Immunotherapy

Liu, Z., Zhang, Y., Xiang, Y., & Kang, X. (2022) · Molecules · doi:10.3390/molecules27175439 · Cited by 30

Discovery of NAFLD-Improving Agents by Promoting the Degradation of Keap1

Mingming, Q., Zhong, H., Cheng, Z., Chen, S., Han, X., Shang, J., Chen, L., & Sun, J. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00822 · Cited by 29

The new direction of drug development: Degradation of undruggable targets through targeting chimera technology

Liang, X., Ren, H., Han, F., Liang, R., Zhao, J., & Liu, H. (2023) · Medicinal Research Reviews · doi:10.1002/med.21992 · Cited by 31

Protacs in cancer therapy: mechanisms, design, clinical trials, and future directions

Vikal, A., Maurya, R., Patel, B. B., Sharma, R. K., Patel, P., Patil, U. K., & Kurmi, B. D. (2024) · Drug Delivery and Translational Research · doi:10.1007/s13346-024-01754-z · Cited by 29

Targeted Protein Degradation: The New Frontier of Antimicrobial Discovery?

Powell, M., Blaskovich, M. A. T., & Hansford, K. A. (2021) · ACS Infectious Diseases · doi:10.1021/acsinfecdis.1c00203 · Cited by 29

Recent advances in induced proximity modalities

Ng, C. S. C., & Banik, S. M. (2022) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2021.102107 · Cited by 27

Discovery of an Exceptionally Orally Bioavailable and Potent HPK1 PROTAC with Enhancement of Antitumor Efficacy of Anti-PD-L1 Therapy

Wu, M., Wu, Y., Jin, Y., Mao, X., Zeng, S., Yu, H., Zhang, J., Jin, Y., Wu, Y., Xu, T., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00644 · Cited by 27

PROTAC unleashed: Unveiling the synthetic approaches and potential therapeutic applications

Pravin, N., & Jóźwiak, K. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116837 · Cited by 29

Strategy and Design of In Situ Activated Protein Hydrolysis Targeted Chimeras

Lv, M.-Y., Hou, D., Liu, S., Cheng, D., & Wang, H. (2024) · ACS Nano · doi:10.1021/acsnano.4c11903 · Cited by 30

Diverse drug delivery systems for the enhancement of cancer immunotherapy: an overview

Liu, X., Cheng, Y., Mu, Y., Zhang, Z., Tian, D., Liu, Y., Hu, X., & Wen, T. (2024) · Frontiers in Immunology · doi:10.3389/fimmu.2024.1328145 · Cited by 29

Proteolysis Targeting Chimeras in Antiviral Research

Desantis, J., & Goracci, L. (2022) · Future Medicinal Chemistry · doi:10.4155/fmc-2022-0005 · Cited by 27

Structural Basis of Conformational Dynamics in the PROTAC‐Induced Protein Degradation

Zhao, H. (2024) · ChemMedChem · doi:10.1002/cmdc.202400171 · Cited by 25

Conditional PROTAC: Recent Strategies for Modulating Targeted Protein Degradation

Yim, J., Park, J., Kim, G., Lee, H. H., Chung, J. S., Jo, A., Koh, M., & Park, J. (2024) · ChemMedChem · doi:10.1002/cmdc.202400326 · Cited by 28

Degradome analysis to identify direct protein substrates of small-molecule degraders

Jochem, M., Schrempf, A., Wagner, L.-M., Segal, D., Cisneros, J., Ng, A., Winter, G. E., & Krijgsveld, J. (2025) · Cell Chemical Biology · doi:10.1016/j.chembiol.2024.10.007 · Cited by 25

Redefining the Scope of Targeted Protein Degradation: Translational Opportunities in Hijacking the Autophagy–Lysosome Pathway

Cassidy, K. B., & Zhao, H. (2021) · Biochemistry · doi:10.1021/acs.biochem.1c00330 · Cited by 25

Translating PROTAC chemical series optimization into functional outcomes underlying BRD7 and BRD9 protein degradation

Riching, K. M., Vasta, J. D., Hughes, S. J., Zoppi, V., Maniaci, C., Testa, A., Urh, M., Ciulli, A., & Daniels, D. L. (2021) · Current Research in Chemical Biology · doi:10.1016/j.crchbi.2021.100009 · Cited by 26

Advances in the Design and Development of PROTAC-mediated HDAC Degradation

Rodrigues, D. A., Roe, A. J., Griffith, D. M., & Chonghaile, T. N. (2021) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026621666211015092047 · Cited by 27

Estimating the cooperativity of PROTAC-induced ternary complexes using 19 F NMR displacement assay

Castro, G. V., & Ciulli, A. (2021) · RSC Medicinal Chemistry · doi:10.1039/d1md00215e · Cited by 25

Are we ready to design oral PROTACs®?

Jiménez, D. G., Sebastiano, M. R., Caron, G., & Ermondi, G. (2021) · ADMET & DMPK · doi:10.5599/admet.1037 · Cited by 24

Design, synthesis, and characterization of PROTACs targeting the androgen receptor in prostate and lung cancer models

Gockel, L. M., Pfeifer, V., Baltes, F., Bachmaier, R. D., Wagner, K. G., Bendas, G., Gütschow, M., Sosič, I., & Steinebach, C. (2022) · Archiv der Pharmazie · doi:10.1002/ardp.202100467 · Cited by 24

Development of selective FGFR1 degraders using a Rapid synthesis of proteolysis targeting Chimera (Rapid-TAC) platform

Guo, L., Liu, J., Nie, X., Wang, T., Ma, Z., Yin, D., & Tang, W. (2022) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2022.128982 · Cited by 24

Development of an orally bioavailable CDK12/13 degrader and induction of synthetic lethality with AKT pathway inhibition

Chang, Y., Wang, X., Yang, J., Tien, J. C.-Y., Mannan, R., Cruz, G., Zhang, Y., Vo, J. N., Magnuson, B., Mahapatra, S., et al. (2024) · Cell Reports Medicine · doi:10.1016/j.xcrm.2024.101752 · Cited by 24

Single-Molecule-Based, Label-Free Monitoring of Molecular Glue Efficacies for Promoting Protein–Protein Interactions Using YaxAB Nanopores

Ryu, M., Oh, S., Jeong, K., Hwang, S., Kim, J., Chung, M., & Chi, S. (2024) · ACS Nano · doi:10.1021/acsnano.4c11436 · Cited by 23

Enzyme-Activated Sugar-Coated Bifunctional Degraders

Zhu, Q., Fischer, G., Cheng, S. V., Payne, N. C., Peter, D., Mody, A. C., Arce-Solano, S., Shen, D., Lin, Z., Mazitschek, R., et al. (2025) · Journal of the American Chemical Society · doi:10.1021/jacs.5c09843 · Cited by 22

Targeting Triple-Negative Breast Cancer by the Phytopolyphenol Carnosol: ROS-Dependent Mechanisms

Alsamri, H., Dhaheri, Y. A., & Iratni, R. (2023) · Antioxidants · doi:10.3390/antiox12071349 · Cited by 23

Commentary: PROTACs make undruggable targets druggable: Challenge and opportunity

Lü, B., & Ye, J. (2021) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2021.07.017 · Cited by 23

M1/M2 macrophage-targeted nanotechnology and PROTAC for the treatment of atherosclerosis

Ma, Y., Yang, X., Ning, K., & Guo, H. (2024) · Life Sciences · doi:10.1016/j.lfs.2024.122811 · Cited by 23

Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs

Vicente, A. T. S., Moura, S. P. S. P., & Salvador, J. A. R. (2025) · Communications Chemistry · doi:10.1038/s42004-025-01598-9 · Cited by 23

Photoredox Csp3−Csp2 Reductive Cross‐Couplings of Cereblon Ligands for PROTAC Linker Exploration in Batch and Flow

Steiner, A., Krieger, J., Jones, R. C., Böse, D., Wang, Y., Eggenweiler, H., Williams, J. D., & Kappe, C. O. (2022) · ChemCatChem · doi:10.1002/cctc.202201184 · Cited by 22

Receptor-interacting protein kinase 1 (RIPK1) inhibitor: a review of the patent literature (2018-present)

Xu, L., Zhang, W., & Zhuang, C. (2023) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2023.2195548 · Cited by 22

Industry perspective on the nonclinical safety assessment of heterobifunctional degraders

Hemkens, M. D., Stamp, K., Loberg, L. I., Moreau, K., & Hart, T. K. (2023) · Drug Discovery Today · doi:10.1016/j.drudis.2023.103643 · Cited by 22

Alkenyl oxindole is a novel PROTAC moiety that recruits the CRL4DCAF11 E3 ubiquitin ligase complex for targeted protein degradation

Wang, Y., Wei, T., Zhao, M., Huang, A., Sun, F., Chen, L., Lin, R., Xie, Y., Zhang, M., Xu, S., et al. (2024) · PLoS Biology · doi:10.1371/journal.pbio.3002550 · Cited by 24

Lysineless HiBiT and NanoLuc Tagging Systems as Alternative Tools for Monitoring Targeted Protein Degradation

Lin, H., Riching, K. M., Lai, M. P., Lu, D., Cheng, R., Qi, X., & Wang, J. (2024) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.4c00271 · Cited by 24

Induced proximity at the cell surface

Till, N. A., Ramanathan, M., & Bertozzi, C. R. (2025) · Nature Biotechnology · doi:10.1038/s41587-025-02592-1 · Cited by 21

Exploiting E3 ligases for lung cancer therapy: The promise of DCAF-PROTACs

Hussain, M. S., Eltaib, L., Rana, A. J., Maqbool, M., Ashique, S., Alanazi, M. N., Khan, Y., & Agrawal, M. (2025) · Pathology - Research and Practice · doi:10.1016/j.prp.2025.156001 · Cited by 24

3-Aminophthalic acid, a new cereblon ligand for targeted protein degradation by O’PROTAC

Yan, Y., Shao, J., Ding, D., Pan, Y., Tran, P., Yan, W., Wang, Z., Li, H., & Huang, H. (2022) · Chemical Communications · doi:10.1039/d1cc06525d · Cited by 22

Proteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges

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