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Global PROTAC Toolbox for Degrading BCR–ABL Overcomes Drug-Resistant Mutants and Adverse Effects

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Development of selective small molecule MDM2 degraders based on nutlin

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FAK-targeting PROTAC as a chemical tool for the investigation of non-enzymatic FAK function in mice

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BRD4 degrader ARV-825 produces long-lasting loss of BRD4 protein and exhibits potent efficacy against cholangiocarcinoma cells.

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Strategies for designing proteolysis targeting chimaeras (PROTACs)

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A PROTAC‐Based Cuproptosis Sensitizer in Lung Cancer Therapy

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Nucleic-Acid-Based Targeted Degradation in Drug Discovery

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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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MDM2-Based Proteolysis-Targeting Chimeras (PROTACs): An Innovative Drug Strategy for Cancer Treatment

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Folate‐PEG‐PROTAC Micelles for Enhancing Tumor‐Specific Targeting Proteolysis In Vivo

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Proteolysis‐Targeting Chimera (PROTAC): Current Applications and Future Directions

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

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PROTAC: targeted drug strategy. Principles and limitations

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Targeted Protein Degradation: Clinical Advances in the Field of Oncology

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An overview of PROTACs targeting MDM2 as a novel approach for cancer therapy

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Progress of proteolysis-targeting chimeras (PROTACs) delivery system in tumor treatment

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More than Toxins—Current Prospects in Designing the Next Generation of Antibody Drug Conjugates

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Function, mechanism and drug discovery of ubiquitin and ubiquitin-like modification with multiomics profiling for cancer therapy

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Ternary Complex‐Templated Dynamic Combinatorial Chemistry for the Selection and Identification of Homo‐PROTACs

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Targeted protein modification as a paradigm shift in drug discovery

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Discovery of Novel p53-MDM2 Inhibitor (RG7388)-Conjugated PlatinumIV Complexes as Potent Antitumor Agents

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An update patent review of MDM2–p53 interaction inhibitors (2019–2023)

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Small-Molecule Approaches to Target Transcription Factors

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Self-Assembled Peptide PROTAC Prodrugs Targeting FOXM1 for Cancer Therapy

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MDM2-BCL-XL PROTACs enable degradation of BCL-XL and stabilization of p53

Chang, M., Gao, F., Chen, J., Gnawali, G. R., & Wang, W. (2022) · Acta Materia Medica · doi:10.15212/amm-2022-0022 · Cited by 14 · see citing works

Discovery of a potent and selective JAK1-targeting PROTAC degrader with anti-tumor activities

Zhang, X., Wang, W., Dong, G., Song, Y., Zhai, X., & Sheng, C. (2024) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2024.129838 · Cited by 13 · see citing works

Development of FBXO22 Degraders and the Recruitment Ligand 2-Pyridinecarboxyaldehyde (2-PCA)

Qiu, T., Zhuang, Z., Byun, W. S., Kozicka, Z., Baek, K., Zhong, J., Thornhill, A. M., Ryan, J. K., Donovan, K. A., Fischer, E. S., et al. (2025) · Journal of the American Chemical Society · doi:10.1021/jacs.5c14141 · Cited by 11 · see citing works

Exploring the potential mechanism of ginsenoside Rg1 to regulate ferroptosis in Alzheimer's disease based on network pharmacology

Deng, X., Qiu, Z., Chen, X., Liu, J., Wang, X., Li, J., Zhang, J., Cui, X., Fu, Y., & Jiang, M. (2024) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2024.176859 · Cited by 11 · see citing works

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 11 · see citing works

Bifunctional robots inducing targeted protein degradation

Sobhia, M. E., Kumar, H., & Kumari, S. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115384 · Cited by 11 · see citing works

Targeted therapy based on ubiquitin-specific proteases, signalling pathways and E3 ligases in non-small-cell lung cancer

Yang, Y., Zhao, C.-J., Jin, Z.-F., Zheng, J., & Ma, L. (2023) · Frontiers in Oncology · doi:10.3389/fonc.2023.1120828 · Cited by 11 · see citing works

Targeting reversible post-translational modifications with PROTACs: a focus on enzymes modifying protein lysine and arginine residues

Pichlak, M., Sobierajski, T., Błażewska, K. M., & Gendaszewska‐Darmach, E. (2023) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2023.2254012 · Cited by 10 · see citing works

Design of Murine Double Minute 2 Proteolysis Targeting Chimera Degraders with a Built-In Tumor-Targeting Ability

Wang, Z., Yue, S., Chen, X., Li, J., Zhu, P., Chen, H., Qiu, F., Xie, D., Liang, Y., Li, D., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01228 · Cited by 11 · see citing works

Next‐Generation Proteolysis‐Targeting Chimeras in Precision Oncology: Multifunctional Designs, Emerging Modalities, and Translational Prospects in Targeted Protein Degradation

Nafie, M. S., Diab, M. K., Yassen, A. S. A., Elshamy, A. M., Tohamy, M. R. E., Tawfik, H. O., & Fahmy, S. A. (2025) · Drug Development Research · doi:10.1002/ddr.70192 · Cited by 9 · see citing works

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 9 · see citing works

Discovery of Drugs Targeting Mutant p53 and Progress in Nano-Enabled Therapeutic Strategy for p53-Mutated Cancers

Zhang, N., Jing, Z., Song, J., Liang, Q., Xu, Y., Xu, Z., Wen, L., & Wei, P. (2025) · Biomolecules · doi:10.3390/biom15060763 · Cited by 11 · see citing works

PROTAC Degraders

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

Chemical knockdown of Keap1 and homoPROTAC-ing allergic rhinitis

Yan, J., Wang, T., Yu, R., Xu, L., Shao, H., Li, T., Wang, Z., Cha, X., Miao, Z., Xing, C., et al. (2025) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2025.05.025 · Cited by 7 · see citing works

Mdm2 targeting via PROteolysis TArgeting Chimeras (PROTAC) is efficient in p53 wildtype, p53-mutated, and abemaciclib-resistant estrogen receptor-positive cell lines and superior to mdm2 inhibition

Goerg, A., Piendl, G., Albert, V., Ortmann, O., Wege, A. K., & Brockhoff, G. (2025) · BMC Cancer · doi:10.1186/s12885-025-14361-z · Cited by 7 · see citing works

Dual functionality of MDM2 in PROTACs expands the horizons of targeted protein degradation

Zhao, J., Chen, H., & Liang, C. (2025) · Biomarker Research · doi:10.1186/s40364-025-00826-7 · Cited by 7 · see citing works

Synthesis and Antineoplastic Activity of a Dimer, Spiroindolinone Pyrrolidinecarboxamide

Cui, J., Wang, Y., Li, X., Xiao, F., Ren, H., & Wu, M. Y. (2023) · Molecules · doi:10.3390/molecules28093912 · Cited by 7 · see citing works

N-Heterocycle based Degraders (PROTACs) Manifesting Anticancer Efficacy: Recent Advances

Banerjee, S., Sharma, S., Thakur, A., Sachdeva, R., Sharma, R., Nepali, K., & Liou, J. (2023) · Current Drug Targets · doi:10.2174/0113894501273969231102095615 · Cited by 7 · see citing works

The Expanding E3 Ligase-Ligand Landscape for PROTAC Technology

Li, Z., Huang, X., Zhao, X., Zhang, Y., & Li, P. (2025) · Targets · doi:10.3390/targets3040030 · Cited by 8 · see citing works

Linkerology in PROTACs: learnings for proximity-inducing therapeutics

Prieto‐Díaz, R., Urbina, A., Rodriguez-Rios, M., & Ciulli, A. (2026) · Trends in Biochemical Sciences · doi:10.1016/j.tibs.2026.07.004 · Cited by 6 · see citing works

A pharmacological modality to sequester homomeric proteins

Livnah, E., Suss, O., Rogel, A., Gilat, A., Abdan, Y., Villegas, J. A., Gabizon, R., Nadir, A., Shamir, Y., Steinman, N. Y., et al. (2026) · Nature Chemical Biology · doi:10.1038/s41589-026-02141-0 · Cited by 4 · see citing works

Upregulation of p53 through induction of MDM2 degradation: improved potency through the introduction of an alkylketone sidechain on the anthraquinone core

Tripathi, R. S., Anifowose, A., Lu, W., Yang, X., & Wang, B. (2022) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2022.2116699 · Cited by 4 · see citing works

Revolutionizing lung cancer treatment: Introducing PROTAC therapy as a novel paradigm in targeted therapeutics

Mahajan, A. A., Panzade, G., Bhuniya, T., Das, P., Bhattacharjee, B., Das, S., Chowdhury, A., Chakraborty, K., Guha, S., Samant, A., et al. (2024) · Current Problems in Cancer · doi:10.1016/j.currproblcancer.2024.101172 · Cited by 4 · see citing works

Hijacking the MDM2 E3 Ligase with Novel BRD4‐Targeting Proteolysis‐Targeting Chimeras in Pancreatic Cancer Cells

Ficu, M. P., Niculescu‐Duvaz, D., Aljarah, M., Kershaw, C. S., & Springer, C. J. (2025) · ChemBioChem · doi:10.1002/cbic.202500133 · Cited by 4 · see citing works

Design and synthesis of novel HDAC6 inhibitor dimer as HDAC6 degrader for cancer treatment by palladium catalysed dimerisation

Lin, C., Hsu, J., Hsu, Y., Fan, K.-C., Wu, S., Lin, M., Guh, J., & Yu, C. (2025) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2025.2468355 · Cited by 3 · see citing works

Proteolysis-Targeting Chimeras: A Kaleidoscope of Targeted Protein Degradation

Mou, Y., Wen, S., Gao, X., & Jiang, Z. (2021) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0199 · Cited by 3 · see citing works

Discovery of a First‐in‐Class Murine Double Minute 2‐Recruiting Positive Transcription Elongation Factor B PROTAC Degrader With Selective Antitumor Activity

Guan, X., Xie, L., Guo, H., Ma, L., Zhou, J., Luo, L., Yang, H., Wu, Y., Liu, J., Wang, Y., et al. (2026) · MedComm · doi:10.1002/mco2.70723 · Cited by 2 · see citing works

Isolation and characterization of β-transducin repeat-containing protein ligands screened using a high-throughput screening system

LIU, X., Sanada, E., Li, J., Li, X., Osada, H., & Watanabe, N. (2023) · Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics · doi:10.32604/or.2023.030240 · Cited by 2 · see citing works

Ternary Complex‐Templated Dynamic Combinatorial Chemistry for the Selection and Identification of Homo‐PROTACs

Diehl, C. J., Salerno, A., & Ciulli, A. (2024) · Angewandte Chemie · doi:10.1002/ange.202319456 · Cited by 1 · see citing works

Bis-dispiro-indolinone-pyrrolidine-imidazolones with polymethylene linkers between imidazolone fragments

Polyakov, V. S., Pervakova, E. V., Grishin, Y. K., & Beloglazkina, E. K. (2025) · Tetrahedron Letters · doi:10.1016/j.tetlet.2025.155589 · Cited by 1 · see citing works

Synthesis of bis(dispiro[indolinone-pyrrolidine-imidazolones])

Polyakov, V. S., Pervakova, E. V., Zyk, N. V., & Beloglazkina, E. K. (2025) · Russian Chemical Bulletin · doi:10.1007/s11172-025-4693-4 · Cited by 1 · see citing works

Multi-Step Synthesis of Chimeric Nutlin–DCA Compounds Targeting Dual Pathways for Treatment of Cancer

Illuminati, D., Foschi, R., Marchetti, P., Zanirato, V., Fantinati, A., Trapella, C., Voltan, R., & Cristofori, V. (2025) · Molecules · doi:10.3390/molecules30193908 · Cited by 1 · see citing works

Dispiroindolinone–Glutarimide Conjugates: Synthesis and Evaluation as Potential Hetero-PROTACs for p53 Reactivation

Polyakov, V. S., Grishin, Y. K., Tafeenko, V. A., Ivanova, E. S., Pogodaeva, S. S., Moldavskii, D. V., Shtil, A. A., & Beloglazkina, E. K. (2026) · Molecules · doi:10.3390/molecules31101602 · Cited by 1 · see citing works

Self-Assembling Amphiphilic PROTACs: A Chemical Strategy for Improved EGFR-Targeted Protein Degradation

Ma, J., Fang, L., Wu, Y. H., Jiao, H., Xiang, G., & Ma, X. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c00971 · Cited by 1 · see citing works

Design of Mdm2 Protac Degraders with a Built-In Tumor-Targeting AbilityPreprint

Wang, Z., Yue, S., Chen, X., Li, J., Zhu, P., Chen, H., Qiu, F., Xie, D., Liang, Y., Li, D., et al. (2024) · SSRN Electronic Journal · doi:10.2139/ssrn.4845142

A novel antitumor therapy: degradation of c-SRC by PROTAC

Xing, Y. A. N. G., Ji, Y., Li, W., JingChao, Y. A. N. G., Li, N., Tian, S., Li, J., HaiTao, C. H. E. N., FengTang, Y. A. N. G., Cui, Y., et al. (2025) · Scientia Sinica Vitae · doi:10.1360/ssv-2025-0055

PROTACS- targeted protein degradation as a path to precision cancer therapeutics

Gatley, H. R., Fisher, P. B., & Das, S. K. (2025) · Advances in cancer research · doi:10.1016/bs.acr.2025.08.001

The Functions and Regulatory Chemicals of Human Leucine Zipper Transcription Factors (LZ TFs)

Yang, H., Bi, S., Yu, B., Fang, P., & Wang, J. (2025) · 化学学报 · doi:10.6023/a25020042

Dual Target E3 Ligase Ligands: A New Way to Overcome Drug Resistance

潘, 相. (2026) · Hans Journal of Medicinal Chemistry · doi:10.12677/hjmce.2026.141006

PROTAC-mediated regulation of programmed cell death: From molecular mechanisms to therapeutic breakthroughs

Huang, H., Deng, A., Pan, F., Lu, Y., Chen, L., Cao, J., Tang, Q., Liu, Y., Wu, Y., Du, J., et al. (2026) · The Innovation · doi:10.1016/j.xinn.2026.101359

Comprendre et cibler la molécule intracellulaire "CISH" dans les cellules Natural Killer : une stratégie pour optimiser les traitements en immunothérapies

Bernard, P.-L. (2023) · theses.fr (ABES) · doi:10.70675/b8c6e6e6z06f4z4377z80e6z1bce4ed7771a

Navigating the p53‐MDM2 Landscape: Molecular Insights and Therapeutic Strategies

Mansour, M. A., Hassan, G. S., & Abouzid, K. A. M. (2026) · Archiv der Pharmazie · doi:10.1002/ardp.70264

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

Regulatory mechanisms of E3 ubiquitin ligases in cholesterol homeostasis

Deng, Q., Hu, Y., Liao, D., & Zhang, C. (2026) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2026.154691

Overview of screening assays used to evaluate PROTACs for cancer treatment

Obidat, R., Reyes-Martinez, J., AlRawashdeh, S., Loredo-Calderón, E. L., & Velázquez‐Martínez, C. A. (2026) · Drug Discovery Today · doi:10.1016/j.drudis.2026.104822

BindingDB Entry 50018545: Blocking Non-enzymatic Functions by PROTAC-Mediated Targeted Protein Degradation.

BindingDB (2024) · UC San Diego · doi:10.7270/q26t0rwh

BindingDB Entry 50021863: Discovery of a potent and selective JAK1-targeting PROTAC degrader with anti-tumor activities.

BindingDB (2025) · UC San Diego · doi:10.7270/q2dr3148

BindingDB Entry 50016515: Nucleic-Acid-Based Targeted Degradation in Drug Discovery.

BindingDB (2023) · UC San Diego · doi:10.7270/q2k35zpc

BindingDB Entry 50016429: Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond.

BindingDB (2023) · UC San Diego · doi:10.7270/q2jd51ts

BindingDB Entry 50018114: Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation.

BindingDB (2024) · UC San Diego · doi:10.7270/q2833x64

BindingDB Entry 50022109: An overview of PROTACs targeting MDM2 as a novel approach for cancer therapy.

BindingDB (2025) · UC San Diego · doi:10.7270/q2wq08f2

Design of Mdm2 Protac Degraders with a Built-In Tumor-Targeting AbilityPreprint

Wang, Z., Yue, S., Chen, X., Li, J., Zhu, P., Chen, H., Qiu, F., Xie, D., Liang, Y., Li, D., et al. (2024) · SSRN Electronic Journal · doi:10.2139/ssrn.4845142

PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective

Han, X., Wei, W., & Sun, Y. (2022) · Acta Materia Medica · doi:10.15212/amm-2022-0010 · Cited by 67 · see citing works

MDM2-Based Proteolysis-Targeting Chimeras (PROTACs): An Innovative Drug Strategy for Cancer Treatment

Vicente, A. T. S., & Salvador, J. A. R. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms231911068 · Cited by 53 · see citing works

Mdm2 targeting via PROteolysis TArgeting Chimeras (PROTAC) is efficient in p53 wildtype, p53-mutated, and abemaciclib-resistant estrogen receptor-positive cell lines and superior to mdm2 inhibition

Goerg, A., Piendl, G., Albert, V., Ortmann, O., Wege, A., & Brockhoff, G. (2025) · Senologie - Zeitschrift für Mammadiagnostik und -therapie · doi:10.1055/s-0045-1807642

An overview of PROTACs targeting MDM2 as a novel approach for cancer therapy

Li, H., Cai, X., Yang, X., & Zhang, X. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116506 · Cited by 29 · see citing works