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

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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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Drug Discovery Approaches to Target E3 Ligases

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Cyclic nucleotide phosphodiesterases as drug targets

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Disordered region of cereblon is required for efficient degradation by proteolysis-targeting chimera

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SP6616 as a Kv2.1 inhibitor efficiently ameliorates peripheral neuropathy in diabetic mice

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Selectively targeting individual bromodomain: Drug discovery and molecular mechanisms

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What influences the activity of Degrader−Antibody conjugates (DACs)

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Tubulin Resists Degradation by Cereblon-Recruiting PROTACs

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Identification and characterization of cancer vulnerabilities via targeted protein degradation

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Protein degraders - from thalidomide to new PROTACs

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An updated patent review of BRD4 degraders

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Targeting STAT3 with Proteolysis Targeting Chimeras and Next-Generation Antisense Oligonucleotides

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Small Molecule Modulators of RING-Type E3 Ligases: MDM and Cullin Families as Targets

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Promising new therapeutic targets for regulation of inflammation and immunity: RING-type E3 ubiquitin ligases

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Targeting epigenetic reader domains by chemical biology

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A covalent BTK ternary complex compatible with targeted protein degradation

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Targeted degradation of PCNA outperforms stoichiometric inhibition to result in programed cell death

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Expanding the ligand spaces for E3 ligases for the design of protein degraders

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Development of Chimeric Molecules That Degrade the Estrogen Receptor Using Decoy Oligonucleotide Ligands

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

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Ubiquitin E3 ligases assisted technologies in protein degradation: Sharing pathways in neurodegenerative disorders and cancer

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Development of a Small Hybrid Molecule That Mediates Degradation of His-Tag Fused Proteins

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The application of ubiquitin ligases in the PROTAC drug design

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PROTAC: Novel degradable approach for different targets to treat breast cancer

Wang, Z., Che, S., & Yu, Z. (2024) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2024.106793 · Cited by 25

Development of a peptide-based inducer of protein degradation targeting NOTCH1

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Probing ubiquitin and SUMO conjugation and deconjugation

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Targeted degradation of CD147 proteins in melanoma

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A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins

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Development of DNA Aptamer-Based PROTACs That Degrade the Estrogen Receptor

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Advances in designing ternary complexes: Integrating in-silico and biochemical methods for PROTAC optimisation in target protein degradation

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Development of Gilteritinib-Based Chimeric Small Molecules that Potently Induce Degradation of FLT3-ITD Protein

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Advancing Design Strategy of PROTACs for Cancer Therapy

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Pooled endogenous protein tagging and recruitment for systematic profiling of protein function

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Selective Degradation of Target Proteins by Chimeric Small-Molecular Drugs, PROTACs and SNIPERs

Ishikawa, M., Tomoshige, S., Demizu, Y., & Naito, M. (2020) · Pharmaceuticals · doi:10.3390/ph13040074 · Cited by 22

Targeted Protein Degradation: An Emerging Therapeutic Strategy in Cancer

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

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Development of a Potent Protein Degrader against Oncogenic BCR-ABL Protein

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Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs)

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Identification of PDE6D as a potential target of sorafenib via PROTAC technologyPreprint

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Proteolysis Targeting Chimeras (PROTACs) in Breast Cancer Therapy

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Primary Amine Tethered Small Molecules Promote the Degradation of X-Linked Inhibitor of Apoptosis Protein

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Proteolysis-targeting chimeras: A promising technique in cancer therapy for gaining insights into tumor development

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Targeted protein degraders of SARS-CoV-2 Mpro are more active than enzymatic inhibition alone with activity against nirmatrelvir resistant virus

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Estrogen Receptor-α Targeting: PROTACs, SNIPERs, Peptide-PROTACs, Antibody Conjugated PROTACs and SNIPERs

Negi, A., Kesari, K. K., & Voisin‐Chiret, A. S. (2022) · Pharmaceutics · doi:10.3390/pharmaceutics14112523 · Cited by 18

An “OFF–ON–OFF” fluorescence protein-labeling probe for real-time visualization of the degradation of short-lived proteins in cellular systems

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

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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

PROTAC-mediated conditional degradation of the WRN helicase as a potential strategy for selective killing of cancer cells with microsatellite instability

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Targeted protein degradation and drug discovery

Naito, M. (2022) · The Journal of Biochemistry · doi:10.1093/jb/mvac041 · Cited by 16

Current Status of Oligonucleotide-Based Protein Degraders

Shih, P., Naganuma, M., Demizu, Y., & Naito, M. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15030765 · Cited by 15

The emerging role of targeted protein degradation to treat and study cancer

Brodermann, M. H., Henderson, E. K., & Sellar, R. S. (2024) · The Journal of Pathology · doi:10.1002/path.6301 · Cited by 15

Targeted Protein Degradation by Chimeric Compounds using Hydrophobic E3 Ligands and Adamantane Moiety

Shoda, T., Ohoka, N., Tsuji, G., Fujisato, T., Inoue, H., Demizu, Y., Naito, M., & Kurihara, M. (2020) · Pharmaceuticals · doi:10.3390/ph13030034 · Cited by 15

Development of Versatile Solid-Phase Methods for Syntheses of PROTACs with Diverse E3 Ligands

Xu, H., Kurohara, T., Ohoka, N., Tsuji, G., Inoué, T., Naito, M., & Demizu, Y. (2023) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2023.117293 · Cited by 16

PROTACs: Promising Approaches for Epigenetic Strategies to Overcome Drug Resistance

Giardina, S. F., Valdambrini, E., Warren, J. D., & Barany, F. (2021) · Current Cancer Drug Targets · doi:10.2174/1568009621666210203110857 · Cited by 14

In vivo synthetic chemistry of proteolysis targeting chimeras (PROTACs)

Tomoshige, S., & Ishikawa, M. (2021) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2021.116221 · Cited by 17

Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines

Yan, Z., Lyu, X., Lin, D., Wu, G., Gong, Y., Ren, X., Xiao, J., Lou, J., Huang, H., Chen, Y., et al. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115381 · Cited by 14

Recent advancements in targeted protein knockdown technologies—emerging paradigms for targeted therapy

Joshi, M., Dey, P., & De, A. (2023) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2023.00194 · Cited by 15

UBE3A: The Role in Autism Spectrum Disorders (ASDs) and a Potential Candidate for Biomarker Studies and Designing Therapeutic Strategies

Roy, B., Amemasor, E., Hussain, S., & Castro, K. (2023) · Diseases · doi:10.3390/diseases12010007 · Cited by 15

Inducing the Degradation of Disease-Related Proteins Using Heterobifunctional Molecules

Delport, A., & Hewer, R. (2019) · Molecules · doi:10.3390/molecules24183272 · Cited by 14

Drug Discovery Researches on Modulators of Lysine-Modifying Enzymes Based on Strategic Chemistry Approaches

Itoh, Y. (2019) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.c19-00741 · Cited by 15

Chimera induced protein degradation: PROTACs and beyond

Yin, L., & Hu, Q. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112494 · Cited by 14

Development of a potent small‐molecule degrader against oncogenic BRAFV600E protein that evades paradoxical MAPK activation

Ohoka, N., Suzuki, M., Uchida, T., Tsukumo, Y., Yoshida, M., Inoué, T., Ohki, H., & Naito, M. (2022) · Cancer Science · doi:10.1111/cas.15401 · Cited by 13

Targeted protein degradation might present a novel therapeutic approach in the fight against African trypanosomiasis

Danazumi, A. U., Ishmam, I. T., Idris, S., Izert, M. A., Balogun, E. O., & Górna, M. W. (2023) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2023.106451 · Cited by 14

Recent Advances in the Design and Development of Anticancer Molecules based on PROTAC Technology

Mukhamejanova, Z., Tong, Y., Xiang, Q., Xu, F., & Pang, J. (2020) · Current Medicinal Chemistry · doi:10.2174/0929867327666200312112412 · Cited by 13

Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models

Sun, D., Nikonova, A. S., Zhang, P., Deneka, A. Y., Fitzgerald, M. E., Michael, R. E., Lee, L., Lilly, A. C., Fisher, S. L., Phillips, A. J., et al. (2021) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-20-0831 · Cited by 13

Recent Advances in PROTAC Technology Toward New Therapeutic Modalities

Yokoo, H., Naganuma, M., Oba, M., & Demizu, Y. (2022) · Chemistry & Biodiversity · doi:10.1002/cbdv.202200828 · Cited by 14

Targeting Oncoproteins for Degradation by Small Molecule-Based Proteolysis-Targeting Chimeras (PROTACs) in Sex Hormone-Dependent Cancers

Liu, L., Shi, L., Wang, Z., Zeng, J., Wang, Y., Xiao, H., & Zhu, Y. (2022) · Frontiers in Endocrinology · doi:10.3389/fendo.2022.839857 · Cited by 13

Targeted Protein Degradation

Mainolfi, N., & Rasmusson, T. (2017) · Annual reports in medicinal chemistry · doi:10.1016/bs.armc.2017.08.005 · Cited by 11

Hydrophobic CPP/HDO conjugates: a new frontier in oligonucleotide-warheaded PROTAC delivery

Naganuma, M., Ohoka, N., Hirano, M., Watanabe, D., Tsuji, G., Inoué, T., & Demizu, Y. (2024) · RSC Medicinal Chemistry · doi:10.1039/d4md00546e · Cited by 12

Potential application of proteolysis targeting chimera (PROTAC) modification technology in natural products for their targeted protein degradation

Gu-liang, Y., Zhong, H., Xia, X., Qi, Z., Wang, C., & Li, S. (2021) · Food Science and Human Wellness · doi:10.1016/j.fshw.2021.11.001 · Cited by 10

The role of E3 ubiquitin ligase in multiple myeloma: potential for cereblon E3 ligase modulators in the treatment of relapsed/refractory disease

Richardson, P. G. G., Mateos, M., Vangsted, A. J., Ramasamy, K., Abildgaard, N., Ho, P. J., Quach, H., & Bahlis, N. J. (2022) · Expert Review of Proteomics · doi:10.1080/14789450.2022.2142564 · Cited by 11

Simple and efficient knockdown of His-tagged proteins by ternary molecules consisting of a His-tag ligand, a ubiquitin ligase ligand, and a cell-penetrating peptide

Hattori, T., Okitsu, K., Yamazaki, N., Ohoka, N., Shibata, N., Misawa, T., Kurihara, M., Demizu, Y., & Naito, M. (2017) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2017.08.001 · Cited by 9

Development of PROTACs targeting estrogen receptor: an emerging technique for combating endocrine resistance

Peng, R., Liu, X., Chen, C., Guo, R., & Min, J. (2024) · RSC Medicinal Chemistry · doi:10.1039/d4md00961d · Cited by 8

Lead discovery and chemical biology approaches targeting the ubiquitin proteasome system

Akinjiyan, F. A., Carbonneau, S., & Ross, N. T. (2017) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2017.08.058 · Cited by 8

PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

Tomoshige, S., & Ishikawa, M. (2020) · Angewandte Chemie · doi:10.1002/ange.202004746 · Cited by 8

Discovery of Small Molecules that Induce the Degradation of Huntingtin

Tomoshige, S., Nomura, S., Ohgane, K., Hashimoto, Y., & Ishikawa, M. (2017) · Angewandte Chemie · doi:10.1002/ange.201706529 · Cited by 8

Development of Protein Knockdown Technology as Emerging Drug Discovery Strategy

Ohoka, N. (2018) · YAKUGAKU ZASSHI · doi:10.1248/yakushi.18-00113 · Cited by 8

Selective degradation of the estrogen receptor in the treatment of cancers

Wang, Z., Ma, Z., & Shen, Z. (2021) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2021.105848 · Cited by 7

Expansion of targeted degradation by Gilteritinib-Warheaded PROTACs to ALK fusion proteins

Yokoo, H., Tsuji, G., Inoué, T., Naito, M., Demizu, Y., & Ohoka, N. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2024.107204 · Cited by 7

Targeted protein degradation of PDE4 shortforms by a novel proteolysis targeting chimera

Sin, Y. Y., Giblin, A., Judina, A., Rujirachaivej, P., Corral, L. G., Glennon, E., Tai, Z. X., Tian, F., Torres, E., Zorn, A., et al. (2024) · FEBS Journal · doi:10.1111/febs.17359 · Cited by 9

Biomaterial-based drug delivery systems used to improve chemotherapeutic activity of pharmaceuticals and to target inhibitors of apoptosis proteins

Kuo, Y., & Rajesh, R. (2020) · Journal of the Taiwan Institute of Chemical Engineers · doi:10.1016/j.jtice.2020.05.011 · Cited by 7

Development of a degrader against oncogenic fusion protein FGFR3-TACC3

Shibata, N., Cho, N., Koyama, H., & Naito, M. (2022) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2022.128584 · Cited by 9

Hybrid molecule between platanic acid and LCL-161 as a yes-associated protein degrader

Nakano, N., Fukuda, K., Tashiro, E., Ishikawa, H., Nagano, W., Kawamoto, R., Mori, A., Watanabe, M., Yamasaki, R., Nakane, T., et al. (2022) · The Journal of Biochemistry · doi:10.1093/jb/mvac021 · Cited by 7

Major Advances in Emerging Degrader Technologies

Luo, H., Wu, L., He, Y., Qin, C., & Tang, X. (2022) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2022.921958 · Cited by 7

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

Atomic-Resolution Prediction of Degrader-mediated Ternary Complex Structures by Combining Molecular Simulations with Hydrogen Deuterium Exchange

Dixon, T., MacPherson, D., Mostofian, B., Dauzhenka, T., Lotz, S., McGee, D., Shechter, S., Shrestha, U. R., Wiewiora, R., McDargh, Z. A., et al. (2021) · doi:10.1101/2021.09.26.461830 · Cited by 7

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 9

Chemical immunology: Recent advances in tool development and applications

Shi, Y., Bashian, E. E., Hou, Y., & Wu, P. (2024) · Cell chemical biology · doi:10.1016/j.chembiol.2024.02.006 · Cited by 6

PROTAC-mediated Target Degradation: A Paradigm Changer in Drug Discovery?

Cromm, P. M., Crews, C. M., & Weinmann, H. (2020) · Royal Society of Chemistry eBooks · doi:10.1039/9781839160691-00001 · Cited by 6

PROTACs: A Hope for Breast Cancer Patients?

Kaur, R., Chaudhary, G., Kaur, A., Singh, P., Longowal, G. D., Sapkale, G. P., & Arora, S. (2021) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/1871520621666210308100327 · Cited by 6

Phosphorothioate-Modified DNA Aptamer-Based PROTACs for Targeted Degradation of Estrogen Receptor α

Watanabe, D., Terauchi, H., Osawa, H., Naganuma, M., Tsuji, G., & Demizu, Y. (2025) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.5c00242 · Cited by 5

Clozapine as an E3 Ligand for PROTAC Technology

Takano, R., Ohoka, N., Kurohara, T., Arakawa, N., Ohgane, K., Inoué, T., Yokoo, H., & Demizu, Y. (2025) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.4c00500 · Cited by 6

Design of bifunctional molecules to accelerate post-translational modifications: achievements and challenges

Wang, Y., He, Y., You, Q., & Wang, L. (2024) · Drug Discovery Today · doi:10.1016/j.drudis.2024.104194 · Cited by 5

Breaking the Fourth Wall: Modulating Quaternary Associations for Protein Regulation and Drug Discovery

Long, M. J. C., Hnedzko, D., Kim, B. K., & Aye, Y. (2018) · ChemBioChem · doi:10.1002/cbic.201800716 · Cited by 5

PROTACs in targeted protein degradation: Advances in development and AI-enhanced drug discovery

Du, M., Liu, T., Wang, W., Fan, S., Tian, M., Du, Q., Wang, Z., Li, X., Liu, X., Xia, Q., et al. (2026) · European Journal of Medicinal Chemistry Reports · doi:10.1016/j.ejmcr.2026.100332 · Cited by 4

Mechanisms and Design Principles of Proteolysis-Targeting Chimeras and Their Emerging Applications

Knoll, N., Neamati, N., & Üren, A. (2026) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.5c00730 · 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

Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation

Ohoka, N., Morita, Y., Nagai, K., Shimokawa, K., Ujikawa, O., Fujimori, I., Ito, M., Hayase, Y., Okuhira, K., Shibata, N., et al. (2018) · Journal of Biological Chemistry · doi:10.1074/jbc.ra117.001091 · Cited by 105

Development of Protein Knockdown Technology as Emerging Drug Discovery Strategy

Ohoka, N. (2018) · YAKUGAKU ZASSHI · doi:10.1248/yakushi.18-00113 · Cited by 8

SNIPERs—Hijacking IAP activity to induce protein degradation

Naito, M., Ohoka, N., & Shibata, N. (2019) · Drug Discovery Today Technologies · doi:10.1016/j.ddtec.2018.12.002 · Cited by 171

Protein Knockdown Technology: Application of Ubiquitin Ligase to Cancer Therapy

Ohoka, N., Shibata, N., Hattori, T., & Naito, M. (2016) · Current Cancer Drug Targets · doi:10.2174/1568009616666151112122502 · Cited by 55

Different Degradation Mechanisms of Inhibitor of Apoptosis Proteins (IAPs) by the Specific and Nongenetic IAP-Dependent Protein Eraser (SNIPER)

Ohoka, N., Ujikawa, O., Shimokawa, K., Sameshima, T., Shibata, N., Hattori, T., Nara, H., Cho, N., & Naito, M. (2018) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.c18-00567 · Cited by 56