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Selective inhibition of BET bromodomains

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Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

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BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

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Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation

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Integration, scaling, space-group assignment and post-refinement

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Function and regulation of cullin–RING ubiquitin ligases

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Identification of a Primary Target of Thalidomide Teratogenicity

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Discovery of Small-Molecule Degraders for Alpha-Synuclein Aggregates

Tong, Y., Zhu, W., Chen, J., Wen, T., Xu, F., & Pang, J. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00274 · Cited by 39

Cooperatively designed aptamer-PROTACs for spatioselective degradation of nucleocytoplasmic shuttling protein for enhanced combinational therapy

Liu, R., Liu, Z., Chen, M., Xing, H., Zhang, P., & Zhang, J. (2023) · Chemical Science · doi:10.1039/d3sc04249a · Cited by 39

Selective Degradation of Polo‐like Kinase 1 by a Hydrophobically Tagged Inhibitor of the Polo‐Box Domain

Rubner, S., Scharow, A., Schubert, S., & Berg, T. (2018) · Angewandte Chemie International Edition · doi:10.1002/anie.201809640 · Cited by 38

Degrading proteins in animals: “PROTAC”tion goes in vivo

Guo, J., Liu, J., & Wei, W. (2019) · Cell Research · doi:10.1038/s41422-019-0144-9 · Cited by 38

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

The clinical advances of proteolysis targeting chimeras in oncology

Xie, H., Liu, J., Alem, D., & Fleming, J. B. (2021) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2021.00061 · 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

Synthesis of 7-benzylguanosine cap-analogue conjugates for eIF4E targeted degradation

Kaur, T., Menon, A., & Garner, A. L. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.01.080 · Cited by 38

Inducing Protein Degradation as a Therapeutic Strategy

Crews, C. M., Georg, G. I., & Wang, S. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00735 · Cited by 38

Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog–Thalidomide PROTACs

Kim, G. Y., Song, C. W., Yang, Y., Lee, N.-R., Yoo, H., Son, S. H., Lee, S., Park, J. S., Lee, J. K., Inn, K., et al. (2021) · Molecules · doi:10.3390/molecules26092525 · Cited by 37

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

Novel Design Strategies to Enhance the Efficiency of Proteolysis Targeting Chimeras

Zhao, C., & Dekker, F. J. (2022) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.2c00089 · Cited by 38

Oligo-PROTAC strategy for cell-selective and targeted degradation of activated STAT3

Hall, J., Zhang, Z., Bhattacharya, S., Wang, D., Alcantara, M. B., Liang, Y., Swiderski, P. M., Forman, S. J., Kwak, L. W., Vaidehi, N., et al. (2024) · Molecular Therapy — Nucleic Acids · doi:10.1016/j.omtn.2024.102137 · Cited by 39

Applications of protein ubiquitylation and deubiquitylation in drug discovery

Chen, Y., Xue, H., & Jin, J. (2024) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2024.107264 · Cited by 41

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

Targeting glucocorticoid receptor signaling pathway for treatment of stress-related brain disorders

Göver, T., & Ślęzak, M. (2024) · Pharmacological Reports · doi:10.1007/s43440-024-00654-w · Cited by 45

Sensitive and Accurate Quantitation of Phosphopeptides Using TMT Isobaric Labeling Technique

Jiang, X., Bomgarden, R. D., Brown, J., Drew, D. L., Robitaille, A. M., Viner, R., & Hühmer, A. F. R. (2017) · Journal of Proteome Research · doi:10.1021/acs.jproteome.7b00610 · Cited by 36

Human cytomegalovirus IE2 drives transcription initiation from a select subset of late infection viral promoters by host RNA polymerase II

Li, M., Ball, C. B., Collins, G., Hu, Q., Luse, D. S., Price, D. H., & Meier, J. L. (2020) · PLoS Pathogens · doi:10.1371/journal.ppat.1008402 · Cited by 37

A Buchwald–Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3‐Ligase PROTACs**

Hayhow, T. G., Borrows, R. E. A., Diène, C. R., Fairley, G., Fallan, C., Fillery, S. M., Scott, J. S., & Watson, D. W. (2020) · Chemistry - A European Journal · doi:10.1002/chem.202003137 · Cited by 36

A kinetic proofreading model for bispecific protein degraders

Bartlett, D. W., & Gilbert, A. M. (2020) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1007/s10928-020-09722-z · Cited by 38

Targeting the Ubiquitin System in Glioblastoma

Scholz, N., Kurian, K. M., Siebzehnrübl, F. A., & Licchesi, J. D. F. (2020) · Frontiers in Oncology · doi:10.3389/fonc.2020.574011 · Cited by 37

Repurposing Immunomodulatory Imide Drugs (IMiDs) in Neuropsychiatric and Neurodegenerative Disorders

Jung, Y. J., Tweedie, D., Scerba, M. T., Kim, D. S., Palmas, M. F., Pisanu, A., Carta, A. R., & Greig, N. H. (2021) · Frontiers in Neuroscience · doi:10.3389/fnins.2021.656921 · Cited by 37

A novel Cereblon E3 ligase modulator with antitumor activity in gastrointestinal cancer

Lier, S., Sellmer, A., Orben, F., Heinzlmeir, S., Krauß, L., Schneeweis, C., Hassan, Z., Schneider, C., Patricia Gloria Schäfer, A., Pongratz, H., et al. (2022) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.105505 · Cited by 37

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

Development of Oligomeric Mannose-6-phosphonate Conjugates for Targeted Protein Degradation

Stevens, C. M., Zhou, Y., Teng, P., Rault, L. N., Liao, Y., & Tang, W. (2023) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.2c00479 · Cited by 40

Exploiting the Cullin E3 Ligase Adaptor Protein SKP1 for Targeted Protein Degradation

Hong, S. H., Divakaran, A., Osa, A., Huang, O. W., Wertz, I. E., & Nomura, D. K. (2024) · ACS Chemical Biology · doi:10.1021/acschembio.3c00642 · Cited by 38

Targeting a lineage-specific PI3Kɣ–Akt signaling module in acute myeloid leukemia using a heterobifunctional degrader molecule

Kelly, L. M., Rutter, J. C., Lin, K., Ling, F., Duchmann, M., Latour, E., Arang, N., Pasquer, H., Ho‐Nhat, D., Charles, J., et al. (2024) · Nature Cancer · doi:10.1038/s43018-024-00782-5 · Cited by 41

Drug Discovery Approaches to Target E3 Ligases

Rodríguez-Gimeno, A., & Galdeano, C. (2024) · ChemBioChem · doi:10.1002/cbic.202400656 · Cited by 39

Targeted Protein Degradation through Cytosolic Delivery of Monobody Binders Using Bacterial Toxins

Schmit, N. E., Neopane, K., & Hantschel, O. D. (2019) · ACS Chemical Biology · doi:10.1021/acschembio.9b00113 · Cited by 36

C–N Coupling of Azoles or Imides with Carbocations Generated by Electrochemical Oxidation

Shao, X., Tian, L., & Wang, Y. (2019) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201900714 · Cited by 37

Proteolytic Targeting Chimeras with Specificity for Plasma Membrane and Intracellular Estrogen Receptors

Lu, A. S., Rouhimoghadam, M., Arnatt, C. K., Filardo, E. J., & Salem, A. K. (2021) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.1c00018 · Cited by 40

A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders

Fischer, P. D., Papadopoulos, E., Dempersmier, J. M., Wang, Z., Nowak, R. P., Donovan, K. A., Kalabathula, J., Gorgulla, C., Junghanns, P., Kabha, E., et al. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113435 · Cited by 37

Ubiquitin-dependent regulation of transcription in development and disease

Mark, K. G., & Rapé, M. (2021) · EMBO Reports · doi:10.15252/embr.202051078 · Cited by 39

A PROTAC targets splicing factor 3B1

Gama-Brambila, R. A., Chen, J., Zhou, J., Tascher, G., Münch, C., & Cheng, X. (2021) · Cell chemical biology · doi:10.1016/j.chembiol.2021.04.018 · Cited by 37

PROTACs for BRDs proteins in cancer therapy: a review

Wang, C., Zhang, Y., Yang, S., Chen, W., & Xing, D. (2022) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2022.2081164 · Cited by 37

Cell-Permeable PROTAC Degraders against KEAP1 Efficiently Suppress Hepatic Stellate Cell Activation through the Antioxidant and Anti-Inflammatory Pathway

Wang, F., Zhan, Y., Li, M., Wang, L., Zheng, A., Liu, C.-B., Wang, H., & Wang, T. (2022) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.2c00165 · Cited by 36

Luteolin binds Src, promotes STAT3 protein ubiquitination and exerts anti-melanoma effects in cell and mouse models

Li, T., Fu, X., Liu, B., Wang, X., Li, J., Zhu, P., Niu, X., Bai, J., Liu, Y., Lu, X., et al. (2022) · Biochemical Pharmacology · doi:10.1016/j.bcp.2022.115044 · Cited by 38

Precise Conformational Control Yielding Highly Potent and Exceptionally Selective BRD4 Degraders with Strong Antitumor Activity

Hu, J., Hu, B., Xu, F., Wang, M., Qin, C., McEachern, D., Stuckey, J. A., & Wang, S. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00520 · Cited by 36

Development of Potent and Selective Coactivator-Associated Arginine Methyltransferase 1 (CARM1) Degraders

Xie, H., Bacabac, M. S., Ma, M., Kim, E., Wang, Y., Wu, W., Li, L., Xu, W., & Tang, W. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00982 · Cited by 35

Acute Pharmacologic Degradation of a Stable Antigen Enhances Its Direct Presentation on MHC Class I Molecules

Moser, S. C., Voerman, J. S. A., Buckley, D. L., Winter, G. E., & Schliehe, C. (2018) · Frontiers in Immunology · doi:10.3389/fimmu.2017.01920 · Cited by 35

Ligand-induced genetic degradation as a tool for target validation

Yesbolatova, A., Tominari, Y., & Kanemaki, M. T. (2018) · Drug Discovery Today Technologies · doi:10.1016/j.ddtec.2018.11.001 · Cited by 35

Highly Parallel Quantification and Compartment Localization of Transcription Factors and Nuclear Proteins

Alexander Joel Federation, Nandakumar, V., Searle, B. C., Stergachis, A. B., Wang, H., Pino, L. K., Merrihew, G. E., Ting, Y. S., Howard, N., Kutyavin, T. V., et al. (2020) · Cell Reports · doi:10.1016/j.celrep.2020.01.096 · Cited by 36

Scaffold hopping enables direct access to more potent PROTACs with in vivo activity

Burslem, G. M., Bondeson, D. P., & Crews, C. M. (2020) · Chemical Communications · doi:10.1039/d0cc02201b · Cited by 35

Histone H3K4 Methyltransferases as Targets for Drug-Resistant Cancers

Liu, Y., Jin, M., & Jeong, K. W. (2021) · Biology · doi:10.3390/biology10070581 · Cited by 36

Selectively targeting individual bromodomain: Drug discovery and molecular mechanisms

Wang, Q., Shao, X., Leung, E. L., Chen, Y., & Yao, X. (2021) · Pharmacological Research · doi:10.1016/j.phrs.2021.105804 · Cited by 34

SJPYT-195: A Designed Nuclear Receptor Degrader That Functions as a Molecular Glue Degrader of GSPT1

Huber, A. D., Li, Y., Lin, W., Galbraith, A. N., Mishra, A., Porter, S. N., Wu, J., Gee, R. R. F., Zhuang, W., Pruett‐Miller, S. M., et al. (2022) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.2c00223 · Cited by 34

Preclinical evaluation of proteolytic targeting of LCK as a therapeutic approach in T cell acute lymphoblastic leukemia

Hu, J., Jarusiewicz, J., Du, G., Nishiguchi, G., Yoshimura, S., Panetta, J. C., Li, Z., Min, J., Yang, L., Chepyala, D., et al. (2022) · Science Translational Medicine · doi:10.1126/scitranslmed.abo5228 · Cited by 35

CRL4CRBN E3 Ligase Complex as a Therapeutic Target in Multiple Myeloma

Barankiewicz, J., Salomon‐Perzyński, A., Misiewicz-Krzemińska, I., & Lech‐Marańda, E. (2022) · Cancers · doi:10.3390/cancers14184492 · Cited by 38

A comprehensive review of BET-targeting PROTACs for cancer therapy

Zhou, X., Zhao, F., Xu, Y.-T., Guan, Y., Yu, T., Zhang, Y., Duan, Y., & Zhao, Y. (2022) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2022.117033 · Cited by 36

Chemically induced degradation of epigenetic targets

Kabir, M., Yu, X., Kanıskan, H. Ü., & Jin, J. J. (2023) · Chemical Society Reviews · doi:10.1039/d3cs00100h · Cited by 36

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

Guo, Y., Li, X., Xie, Y., & Wang, D. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116216 · Cited by 38

IMHB-Mediated Chameleonicity in Drug Design: A Focus on Structurally Related PROTACs

Jiménez, D. G., Sebastiano, M. R., Vallaro, M., Ermondi, G., & Caron, G. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01200 · Cited by 34

Chemical Epigenetics: The Impact of Chemical and Chemical Biology Techniques on Bromodomain Target Validation

Schiedel, M., Moroglu, M., Ascough, D. M. H., Chamberlain, A. E. R., Kamps, J. J. A. G., Sekirnik, A. R., & Conway, S. J. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201812164 · Cited by 34

Tubulin Resists Degradation by Cereblon-Recruiting PROTACs

Gasic, I., Groendyke, B. J., Nowak, R. P., Yuan, J., Kalabathula, J., Fischer, E. S., Gray, N. S., & Mitchison, T. J. (2020) · Cells · doi:10.3390/cells9051083 · Cited by 36

CDK9 activity is critical for maintaining MDM4 overexpression in tumor cells

Štětková, M., Growková, K., Fojtík, P., Valčíková, B., Palušová, V., Verlande, A., Jorda, R., Kryštof, V., Hejret, V., Alexiou, P., et al. (2020) · Cell Death and Disease · doi:10.1038/s41419-020-02971-3 · Cited by 34

Ubiquitination and Ubiquitin-Like Modifications in Multiple Myeloma: Biology and Therapy

Wirth, M., Schick, M., Keller, U. B., & Krönke, J. (2020) · Cancers · doi:10.3390/cancers12123764 · Cited by 35

High-Throughput Quantitative Assay Technologies for Accelerating the Discovery and Optimization of Targeted Protein Degradation Therapeutics

Simard, J. R., Lee, L., Vieux, E. F., Improgo, R., Tieu, T. N., Phillips, A. J., Fisher, S. L., Pollock, R. M., & Park, E. Y. (2021) · SLAS DISCOVERY · doi:10.1177/2472555220985049 · Cited by 33

Hydrophobic Tagging-Mediated Degradation of Transcription Coactivator SRC-1

Choi, S.-R., Wang, H. M., Shin, M. H., & Lim, H. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22126407 · Cited by 34

Identification and characterization of cancer vulnerabilities via targeted protein degradation

Mayor-Ruiz, C., & Winter, G. E. (2019) · Drug Discovery Today: Technologies · doi:10.1016/j.ddtec.2018.12.003 · Cited by 33

A Novel BRD Family PROTAC Inhibitor dBET1 Exerts Great Anti-Cancer Effects by Targeting c-MYC in Acute Myeloid Leukemia Cells

Zhang, K., Gao, L., Wang, J., Chu, X., Zhang, Z., Zhang, Y., Fang, F., Tao, Y., Li, X., Tian, Y., et al. (2022) · Pathology & Oncology Research · doi:10.3389/pore.2022.1610447 · Cited by 35

Protein degraders - from thalidomide to new PROTACs

Ito, T. (2023) · The Journal of Biochemistry · doi:10.1093/jb/mvad113 · Cited by 33

The Advent of Molecular Targeted Therapies Against Cancer. Toward Multi‐Targeting Drugs Through Materials Engineering: A Possible Future Scenario

Puzzo, M., Santo, M. D., Morelli, C., Leggio, A., & Pasqua, L. (2024) · Small Science · doi:10.1002/smsc.202400113 · Cited by 37

E3 ubiquitin ligases and deubiquitinases in colorectal cancer: Emerging molecular insights and therapeutic opportunities

Kumar, S., Basu, M., & Ghosh, M. K. (2024) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/j.bbamcr.2024.119827 · Cited by 35

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

When Kinases Meet PROTACs

Tan, L., & Gray, N. S. (2018) · Chinese Journal of Chemistry · doi:10.1002/cjoc.201800293 · Cited by 34

Structural basis for small molecule targeting of Doublecortin Like Kinase 1 with DCLK1-IN-1

Patel, O., Roy, M. J., Kropp, A., Hardy, J. M., Dai, W., & Lucet, I. S. (2021) · Communications Biology · doi:10.1038/s42003-021-02631-y · Cited by 28

From PROTAC to TPD: Advances and Opportunities in Targeted Protein Degradation

Wang, S., He, F., Tian, C., & Sun, A. (2024) · Pharmaceuticals · doi:10.3390/ph17010100 · Cited by 34

Methods to accelerate PROTAC drug discovery

Osman, J., Thompson, P. E., Jörg, M., & Scanlon, M. J. (2025) · Biochemical Journal · doi:10.1042/bcj20243018 · Cited by 34

Small molecule-mediated protein knockdown as a new approach to drug discovery

Tinworth, C. P., Lithgow, H., & Churcher, I. (2016) · MedChemComm · doi:10.1039/c6md00347h · Cited by 32

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

Shiah, J. V., Grandis, J. R., & Johnson, D. E. (2020) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-20-0599 · Cited by 32

Coupling an EML4-ALK–centric interactome with RNA interference identifies sensitizers to ALK inhibitors

Zhang, G., Scarborough, H. A., Kim, J., Rozhok, A. I., Chen, Y. A., Zhang, X., Song, L., Bai, Y., Fang, B., Liu, R. Z., et al. (2016) · Science Signaling · doi:10.1126/scisignal.aaf5011 · Cited by 30

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

Bulatov, E., Zagidullin, A. A., Valiullina, A., Sayarova, R., & Rizvanov, A. A. (2018) · Frontiers in Pharmacology · doi:10.3389/fphar.2018.00450 · Cited by 34

Applying the auxin-inducible degradation system for rapid protein depletion in mammalian cells

Lambrus, B. G., Moyer, T. C., & Holland, A. J. (2018) · Methods in cell biology · doi:10.1016/bs.mcb.2018.03.004 · Cited by 31

Prime Editing Efficiency and Fidelity are Enhanced in the Absence of Mismatch RepairPreprint

da Silva, J. F., Oliveira, G., Arasa-Verge, E. A., Kagiou, C., Moretton, A., Timelthaler, G., Jiricny, J., & Loizou, J. (2021) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2021.09.30.462548 · Cited by 32

Effects of super-enhancers in cancer metastasis: mechanisms and therapeutic targets

Liu, S., Dai, W., Jin, B., Jiang, F., Huang, H., Hou, W., Lan, J., Jin, Y., Peng, W., & Pan, J. (2024) · Molecular Cancer · doi:10.1186/s12943-024-02033-8 · Cited by 35

The efflux pump ABCC1/MRP1 constitutively restricts PROTAC sensitivity in cancer cells

Wolf, G., Craigon, C., Teoh, S. T., Essletzbichler, P., Onstein, S., Cassidy, D. M., Uijttewaal, E. C. H., Dvorak, V., Cao, Y., Bensimon, A., et al. (2025) · Cell chemical biology · doi:10.1016/j.chembiol.2024.11.009 · Cited by 34

Small-molecule PROTACs: Novel Agents for Cancer Therapy

Wan, Y., Yan, C., Gao, H. J., & Liu, T. (2020) · Future Medicinal Chemistry · doi:10.4155/fmc-2019-0340 · Cited by 32

Targeting epigenetic reader domains by chemical biology

Cipriano, A., Sbardella, G., & Ciulli, A. (2020) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2020.05.006 · Cited by 30

HaloTag‐Targeted Sirtuin‐Rearranging Ligand (SirReal) for the Development of Proteolysis‐Targeting Chimeras (PROTACs) against the Lysine Deacetylase Sirtuin 2 (Sirt2)**

Schiedel, M., Lehotzky, A., Szunyogh, S., Oláh, J., Hammelmann, S., Wössner, N., Robaa, D., Einsle, O., Sippl, W., Ovádi, J., et al. (2020) · ChemBioChem · doi:10.1002/cbic.202000351 · Cited by 30

PROTACs technology for targeting non-oncoproteins: Advances and perspectives

Wang, C., Zhang, Y., Xing, D., & Zhang, R. (2021) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.105109 · Cited by 32

Targeted Degradation of PRC1 Components, BMI1 and RING1B, via a Novel Protein Complex Degrader Strategy

Park, K., Qin, L., Kabir, M., Luo, K., Dale, B., Zhong, Y., Kim, A., Wang, G. G., Kanıskan, H. Ü., & Jin, J. J. (2023) · Advanced Science · doi:10.1002/advs.202205573 · Cited by 30

mRNA export factors store nascent transcripts within nuclear speckles as an adaptive response to transient global inhibition of transcription

Williams, T. D., Michalak, E. M., Carey, K. T., Lam, E. Y. N., Anderson, A., Griesbach, E., Chan, Y.-C., Papasaikas, P., Tan, V. W. T., Ngo, L., et al. (2025) · Molecular Cell · doi:10.1016/j.molcel.2024.12.008 · Cited by 35

High-throughput ligand diversification to discover chemical inducers of proximity

Shaum, J. B., Ordoño, M. M. I., Steen, E. A., Wenge, D. V., Cheong, H., Janowski, J., Hunkeler, M., Bilotta, E. M., Rutter, Z. J., Barta, P. A., et al. (2026) · Nature Chemical Biology · doi:10.1038/s41589-025-02137-2 · Cited by 41

A small-molecule ARTS mimetic promotes apoptosis through degradation of both XIAP and Bcl-2

Mamriev, D., Abbas, R., Klingler, F., Kagan, J., Kfir, N., Donald, A., Weidenfeld, K., Sheppard, D. W., Barkan, D., & Larisch, S. (2020) · Cell Death and Disease · doi:10.1038/s41419-020-2670-2 · Cited by 31

Construction of an IMiD-based azide library as a kit for PROTAC research

Liu, H., Sun, R., Ren, C., Qiu, X., Yang, X., & Jiang, B. (2020) · Organic & Biomolecular Chemistry · doi:10.1039/d0ob02120b · Cited by 30

The testis-specific E3 ubiquitin ligase RNF133 is required for fecundity in mice

Nozawa, K., Fujihara, Y., Devlin, D. J., Deras, R. E., Kent, K., Larina, I. V., Umezu, K., Yu, Z., Sutton, C. M., Ye, Q., et al. (2022) · BMC Biology · doi:10.1186/s12915-022-01368-2 · Cited by 30

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

Generation of tau dephosphorylation-targeting chimeras for the treatment of Alzheimer’s disease and related tauopathies

Su, J., Xiao, Y., Wei, L., Lei, H., Sun, F., Wang, W., Yin, J., Xiong, R., Li, S., Zhang, P., et al. (2024) · 中国科学通报：英文版 · doi:10.1016/j.scib.2024.01.019 · Cited by 30

Intrinsic signaling pathways modulate targeted protein degradation

Yuki, M., Akizuki, Y., Honda, R., Takao, M., Tsuchimoto, A., Hashimoto, S., Iio, H., Kato, M., Kaiho-Soma, A., Saeki, Y., et al. (2024) · Nature Communications · doi:10.1038/s41467-024-49519-z · Cited by 30

Discovery of novel BCL6-Targeting PROTACs with effective antitumor activities against DLBCL in vitro and in vivo

Mi, D., Cheng, L., Li, Y., Yao, M., Li, Y., Hong, K., Xie, C., & Chen, Y. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116789 · Cited by 32

Tandem‐Activatable PROTAC Prodrug for Tumor Biomarker‐Driven Near‐Infrared Opto‐Proteolysis

Lu, X., Wang, X., Liao, H., Sha, B., Zhang, Y., & Li, J. (2025) · Angewandte Chemie International Edition · doi:10.1002/anie.202510641 · Cited by 31

Protein degradation: a validated therapeutic strategy with exciting prospects

Lebraud, H., & Heightman, T. D. (2017) · Essays in Biochemistry · doi:10.1042/ebc20170030 · Cited by 30

Hitting two oncogenic machineries in cancer cells: cooperative effects of the multi-kinase inhibitor ponatinib and the BET bromodomain blockers JQ1 or dBET1 on human carcinoma cells

Bauer, K., Berger, D., Zielinski, C. C., Valent, P., & Grunt, T. W. (2018) · Oncotarget · doi:10.18632/oncotarget.25474 · Cited by 29

Targeting Oncogenic Super Enhancers in MYC-Dependent AML Using a Small Molecule Activator of NR4A Nuclear Receptors

Call, S. G., Duren, R. P., Panigrahi, A. K., Nguyen, L., Freire, P. R., Grimm, S. L., Coarfa, C., & Conneely, O. M. (2020) · Scientific Reports · doi:10.1038/s41598-020-59469-3 · Cited by 31

Phenotypic screening with target identification and validation in the discovery and development of E3 ligase modulators

Ege, N., Bouguenina, H., Tatari, M. N., & Chopra, R. (2021) · Cell chemical biology · doi:10.1016/j.chembiol.2021.02.011 · Cited by 31

Progress toward B-Cell Lymphoma 6 BTB Domain Inhibitors for the Treatment of Diffuse Large B-Cell Lymphoma and Beyond

Ai, Y., Hwang, L., MacKerell, A. D., Melnick, A. M., & Xue, F. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01686 · Cited by 29

T herapeutic targeting of chromatin: status and opportunities

Siklos, M. I., & Kubicek, S. (2021) · FEBS Journal · doi:10.1111/febs.15966 · Cited by 28

BET protein degradation triggers DR5-mediated immunogenic cell death to suppress colorectal cancer and potentiate immune checkpoint blockade

Tong, J., Tan, X., Risnik, D., Gao, M., Song, X., Ermine, K., Shen, L., Wang, S., Yu, J., & Zhang, L. (2021) · Oncogene · doi:10.1038/s41388-021-02041-8 · Cited by 29

Cell cycle involvement in cancer therapy; WEE1 kinase, a potential target as therapeutic strategy

Vakili‐Samiani, S., Khanghah, O. J., Gholipour, E., Najafi, F., Zeinalzadeh, E., Samadi, P., Sarvarian, P., Pourvahdani, S., Kelaye, S. K., Hamblin, M. R., et al. (2022) · Mutation research. Fundamental and molecular mechanisms of mutagenesis · doi:10.1016/j.mrfmmm.2022.111776 · Cited by 30

Chemical Biology Tools for Protein Lysine Acylation

Xie, Y., Du, S., Liu, Z., Liu, M., Xu, Z., Wang, X., Kee, J. X., Yi, F., Sun, H., & Yao, S. Q. (2022) · Angewandte Chemie International Edition · doi:10.1002/anie.202200303 · Cited by 29

Abstract IA31: Phthalimide conjugation as a strategy for targeted protein degradation

Winter, G. E., Buckley, D. L., & Bradner, J. E. (2017) · Clinical Cancer Research · doi:10.1158/1557-3265.pmccavuln16-ia31

Selectively targeting proteins for degradation

Crunkhorn, S. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4670 · Cited by 14

A degrading game plan for cancer therapy

Kiberstis, P. A. (2015) · Science · doi:10.1126/science.348.6241.1327-h

Translation termination factor GSPT1 is a phenotypically relevant off-target of heterobifunctional phthalimide degraders

Ishoey, M., Chorn, S., Singh, N., Jaeger, M. G., Brand, M., Paulk, J., Bauer, S., Erb, M. A., Parapatics, K., Müller, A. C., et al. (2018) · ACS Chemical Biology · doi:10.1021/acschembio.7b00969 · Cited by 177

Abstract 1283: Discovery of selective and potent BRD4 protein degraders using Plexium's DELPhe platform

Parker, G. S., Toth, J., Leriche, G., Bailey, S., Chng, K., Fish, S., Jamborcic, A., Daniele, E., Green, E., Hocker, M., et al. (2021) · Cancer Research · doi:10.1158/1538-7445.am2021-1283