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Coot : model-building tools for molecular graphics

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Multiplex Genome Engineering Using CRISPR/Cas Systems

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The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity

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Selective inhibition of BET bromodomains

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An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer

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Phthalimide conjugation as a strategy for in vivo target protein degradation

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The tripartite motif family identifies cell compartments

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Catalytic in vivo protein knockdown by small-molecule PROTACs

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The roles and targeting options of TRIM family proteins in tumor

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High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Riching, K. M., Mahan, S. D., Urh, M., & Daniels, D. L. (2020) · Journal of Visualized Experiments · doi:10.3791/61787 · Cited by 30

T herapeutic targeting of chromatin: status and opportunities

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

Fan, L., Tong, W., Wei, A., & Mu, X. (2024) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2024.133680 · Cited by 30

The application of ubiquitin ligases in the PROTAC drug design

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Emerging modes-of-action in drug discovery

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Improved methods for targeting epigenetic reader domains of acetylated and methylated lysine

Engelberg, I. A., Foley, C. A., James, L. I., & Frye, S. V. (2021) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2021.03.002 · Cited by 26

Selective degradation-inducing probes for studying cereblon (CRBN) biology

Powell, C. E., Du, G., Bushman, J. W., He, Z., Zhang, T., Fischer, E. S., & Gray, N. S. (2021) · RSC Medicinal Chemistry · doi:10.1039/d0md00382d · Cited by 29

Tissue and host species-specific transcriptional changes in models of experimental visceral leishmaniasis

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Elucidation of genome-wide understudied proteins targeted by PROTAC-induced degradation using interpretable machine learning

Xie, L., & Xie, L. (2023) · PLOS Computational Biology · doi:10.1371/journal.pcbi.1010974 · Cited by 26

Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders

Bouvier, C., Lawrence, R., Cavallo, F., Xolalpa, W., Jordan, A. M., Hjerpe, R., & Rodríguez, M. S. (2024) · Cells · doi:10.3390/cells13070578 · Cited by 28

Roles of Cullin-RING Ubiquitin Ligases in Cardiovascular Diseases

Diaz, S., Wang, K., Sjögren, B., & Liu, X. (2022) · Biomolecules · doi:10.3390/biom12030416 · Cited by 27

Ubiquitination, Biotech Startups, and the Future of TRIM Family Proteins: A TRIM-Endous Opportunity

Bhaduri, U., & Merla, G. (2021) · Cells · doi:10.3390/cells10051015 · Cited by 25

ELIOT : A platform to navigate the E3 pocketome and aid the design of new PROTACs

Palomba, T., Baroni, M., Cross, S., Cruciani, G., & Siragusa, L. (2022) · Chemical Biology & Drug Design · doi:10.1111/cbdd.14123 · Cited by 26

Discovery and optimization of novel N-benzyl-3,6-dimethylbenzo[d]isoxazol-5-amine derivatives as potent and selective TRIM24 bromodomain inhibitors with potential anti-cancer activities

Hu, Q., Wang, C., Xiang, Q., Wang, R., Zhang, C. L., Zhang, M., Xue, X., Luo, G., Liu, X., Wu, X., et al. (2019) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2019.103424 · Cited by 25

Design, Synthesis and In Vitro Investigation of Cabozantinib-Based PROTACs to Target c-Met Kinase

Sachkova, A. A., Andreeva, D. V., Tikhomirov, A. S., Scherbakov, A. M., Salnikova, D. I., Sorokin, D. V., Bogdanov, F. B., Rysina, Y. D., Shchekotikhin, A. E., Shchegravina, E. S., et al. (2022) · Pharmaceutics · doi:10.3390/pharmaceutics14122829 · Cited by 24

Bifunctional Molecules beyond PROTACs

Conway, S. J. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00293 · Cited by 23

SPOP-mutant prostate cancer: Translating fundamental biology into patient care

Bernasocchi, T., & Theurillat, J.-P. P. (2021) · Cancer Letters · doi:10.1016/j.canlet.2021.12.024 · Cited by 22

Advances and Opportunities in Epigenetic Chemical Biology

Beyer, J. N., Raniszewski, N. R., & Burslem, G. M. (2020) · ChemBioChem · doi:10.1002/cbic.202000459 · Cited by 23

Kinetic Detection of E3:PROTAC:Target Ternary Complexes Using NanoBRET Technology in Live Cells

Mahan, S. D., Riching, K. M., Urh, M., & Daniels, D. L. (2021) · Methods in molecular biology · doi:10.1007/978-1-0716-1665-9_8 · Cited by 20

Identification of Histone Peptide Binding Specificity and Small-Molecule Ligands for the TRIM33α and TRIM33β Bromodomains

Sekirnik, A. R., Reynolds, J. K., See, L., Bluck, J. P., Scorah, A. R., Tallant, C., Lee, B., Leszczyńska, K. B., Grimley, R. L., Storer, R. I., et al. (2022) · ACS Chemical Biology · doi:10.1021/acschembio.2c00266 · Cited by 23

Light-Activating PROTACs in Cancer: Chemical Design, Challenges, and Applications

Negi, A., Kesari, K. K., & Voisin‐Chiret, A. S. (2022) · Applied Sciences · doi:10.3390/app12199674 · Cited by 21

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

Shibata, N., Ohoka, N., Hattori, T., & Naito, M. (2019) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.c18-00703 · Cited by 21

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

Tomaselli, D., Mautone, N., Mai, A., & Rotili, D. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112750 · Cited by 21

A strategy to assess the cellular activity of E3 ligase components against neo-substrates using electrophilic probes

Pinch, B. J., Buckley, D. L., Gleim, S., Brittain, S. M., Tandeske, L., D'Alessandro, P. L., Hauseman, Z. J., Lipps, J., Xu, L., Harvey, E. P., et al. (2022) · Cell Chemical Biology · doi:10.1016/j.chembiol.2021.08.007 · Cited by 20

Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors

Xiang, Q., Luo, G., Zhang, C. L., Hu, Q., Wang, C., Wu, T., Xu, H., Hu, J., Zhuang, X., Zhang, M., et al. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114311 · Cited by 21

Application of PROTACs in target identification and validation

Liu, Y., Liang, J. Y., Zhu, R., Yang, Y., Wang, Y., Wei, W., Li, H., & Chen, L. (2024) · Acta Materia Medica · doi:10.15212/amm-2024-0010 · Cited by 21

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

Lv, M., Hu, W., Zhang, S., He, L., Hu, C., & Yang, S. (2022) · Cancer Letters · doi:10.1016/j.canlet.2022.215716 · Cited by 19

Azobenzene Photoswitches in Proteolysis Targeting Chimeras: Photochemical Control Strategies and Therapeutic Benefits

Negi, A., Kieffer, C., & Voisin‐Chiret, A. S. (2022) · ChemistrySelect · doi:10.1002/slct.202200981 · Cited by 19

The tripartite motif-containing 24 is a multifunctional player in human cancer

Yao, Y., Zhou, S., Yue, Y., Fu, K., & Xiao, S. (2024) · Cell & Bioscience · doi:10.1186/s13578-024-01289-3 · Cited by 20

TRIMming Down Hormone-Driven Cancers: The Biological Impact of TRIM Proteins on Tumor Development, Progression and Prognostication

Pauletto, E., Eickhoff, N., Padrão, N., Blattner, C., & Zwart, W. T. (2021) · Cells · doi:10.3390/cells10061517 · Cited by 19

Allostery in Disease: Anticancer Drugs, Pockets, and the Tumor Heterogeneity Challenge

Nussinov, R., Yavuz, B. R., & Jang, H. (2025) · Journal of Molecular Biology · doi:10.1016/j.jmb.2025.169050 · Cited by 19

Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold

Remillard, D., Buckley, D. L., Seo, H., Ferguson, F. M., Dhe‐Paganon, S., Bradner, J. E., & Gray, N. S. (2019) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.9b00243 · Cited by 18

Design and pharmaceutical applications of proteolysis-targeting chimeric molecules

Liang, Y., Nandakumar, K. S., & Cheng, K. (2020) · Biochemical Pharmacology · doi:10.1016/j.bcp.2020.114211 · Cited by 16

Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations

Jang, J., To, C., Clercq, D. J. H. D., Park, E., Ponthier, C. M., Shin, B. H., Mushajiang, M., Nowak, R. P., Fischer, E. S., Eck, M. J., et al. (2020) · Angewandte Chemie · doi:10.1002/ange.202003500 · 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

Chemoproteomics Enabled Discovery of Selective Probes for NuA4 Factor BRD8

Remillard, D., Savage, N. A., Kedves, A. T., Paulk, J., Chen, X., García, F., Romanowski, M. J., Horton, P. A., Murphy, J., Schirle, M., et al. (2021) · ACS Chemical Biology · doi:10.1021/acschembio.1c00256 · Cited by 16

Chromatin Ubiquitination Guides DNA Double Strand Break Signaling and Repair

Kolobynina, K. G., Rapp, A. W., & Cardoso, M. C. (2022) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2022.928113 · Cited by 17

KRAB domain of ZFP568 disrupts TRIM28-mediated abnormal interactions in cancer cells

Kumar, J., Kaur, G., Ren, R., Lu, Y., Lin, K., Li, J., Huang, Y., Patel, A. B., Barton, M. C., Macfarlan, T. S., et al. (2020) · NAR Cancer · doi:10.1093/narcan/zcaa007 · Cited by 16

Pharmacological targeting of Tripartite Motif Containing 24 for the treatment of glioblastoma

Han, M., & Sun, Y. (2021) · Journal of Translational Medicine · doi:10.1186/s12967-021-03158-w · Cited by 16

The Role and Mechanism of TRIM Proteins in Gastric Cancer

Wu, W., Yang, J., Tian, Y., Zou, Z., & Huang, X. (2024) · Cells · doi:10.3390/cells13242107 · Cited by 14

Targeting Cullin-RING Ubiquitin Ligases and the Applications in PROTACs

Gong, L., Cui, D., Xiong, X., & Zhao, Y. (2020) · Advances in experimental medicine and biology · doi:10.1007/978-981-15-1025-0_19 · Cited by 13

Targeting Cullin-RING E3 Ligases for Radiosensitization: From NEDDylation Inhibition to PROTACs

Zheng, S., & Tao, W. (2020) · Frontiers in Oncology · doi:10.3389/fonc.2020.01517 · Cited by 13

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

Ubiquitination of Nonhistone Proteins in Cancer Development and Treatment

Zhang, X., Meng, T., Cui, S., Feng, L., Liu, D., Pang, Q., & Wang, P. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2020.621294 · Cited by 14

Expression and purification of functional recombinant CUL2•RBX1 from E. coli

Diaz, S., Li, L., Wang, K., & Liu, X. (2021) · Scientific Reports · doi:10.1038/s41598-021-90770-x · Cited by 14

TRIM24 is critical for the cellular response to DNA double-strand breaks through regulating the recruitment of MRN complex

Wang, Y., Yao, Y., Wei, Q., Long, S., Chen, Y., Xie, J., Tan, R., Jiang, W., Zhang, Q., Wu, D., et al. (2022) · Oncogene · doi:10.1038/s41388-022-02580-8 · 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

Inhibition of the TRIM24 bromodomain reactivates latent HIV-1

Horvath, R. M., Brumme, Z. L., & Sadowski, I. (2023) · Scientific Reports · doi:10.1038/s41598-023-27765-3 · Cited by 12

Pharmacological Modulation of Transcriptional Coregulators in Cancer

Bishop, T. R., Zhang, Y., & Erb, M. A. (2019) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2019.04.004 · Cited by 11

Knockdown of TRIM24 suppresses growth and induces apoptosis in acute myeloid leukemia through downregulation of Wnt/GSK-3β/β-catenin signaling

Li, C., Xin, H., Shi, Y., & Mu, J. (2020) · Human & Experimental Toxicology · doi:10.1177/0960327120938845 · Cited by 12

Developments and challenges in hit progression within fragment-based drug discovery

Grosjean, H., & Biggin, P. C. (2026) · Nature Communications · doi:10.1038/s41467-026-68941-z · Cited by 15

Extrapolating Lessons from Targeted Protein Degradation to Other Proximity-Inducing Drugs

Winter, G. E. (2024) · ACS Chemical Biology · doi:10.1021/acschembio.4c00191 · Cited by 13

TRIM24-mediated K27-linked ubiquitination of ULK1 alleviates energy stress-induced autophagy and promote prostate cancer growth in the context of SPOP mutation

Chen, S., Lin, J., Yang, Z., Wang, Y., Wang, Q., Wang, D., Qu, Y., Lin, Q., Liu, J., Shi, Y., et al. (2025) · Cell Death and Differentiation · doi:10.1038/s41418-025-01582-9 · Cited by 13

Proteasomal and lysosomal degradation for specific and durable suppression of immunotherapeutic targets

Wang, Y., Deng, S., & Xu, J. (2020) · Cancer Biology and Medicine · doi:10.20892/j.issn.2095-3941.2020.0066 · Cited by 10

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

Role of TRIM24 in the regulation of proteasome-autophagy crosstalk in bortezomib-resistant mantle cell lymphoma

Bouvier, C., Gonzalez-Santamarta, M., Profitós-Pelejà, N., Armengol, M., Quinet, G., Alasseur, Q., Ceccato, L., Xolalpa, W., Freire, R., Guillermet‐Guibert, J., et al. (2025) · Cell Death Discovery · doi:10.1038/s41420-025-02355-6 · Cited by 10

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

Emerging Roles of TRIM Family Proteins in Gliomas Pathogenesis

Giannopoulou, A.-I., Xanthopoulos, C., Piperi, C., & Kostareli, E. (2022) · Cancers · doi:10.3390/cancers14184536 · 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

TRIM24 as a therapeutic target in endocrine treatment–resistant breast cancer

Padrão, N., Gregoricchio, S., Eickhoff, N., Dong, J., Luzietti, L., Bossi, D., Severson, T., Siefert, J. C., Calcinotto, A., Buluwela, L., et al. (2025) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2507571122 · Cited by 9

Conformational Dynamics in the Cell Membrane Interactions of Bispecific Targeted Degrader Therapeutics

Inganäs, E., Lavén, H., Caraballo, R., Klingegård, F., Eklund, M., Andersson, L., Hilgendorf, C., & Matsson, P. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c01499 · Cited by 9

Preclinical and Clinical Advances of Targeted Protein Degradation as a Novel Cancer Therapeutic Strategy: An Oncologist Perspective

Yang, X., He, Y., Kim, R. D., Fleming, J. B., & Xie, H. (2020) · Targeted Oncology · doi:10.1007/s11523-020-00782-2 · Cited by 10

Progress on Small-Molecule Proteolysis-Targeting Chimeras

Huang, W., Wang, B., Zhang, Z., Zhang, C., Zeng, S., & Shen, Z. (2019) · Future Medicinal Chemistry · doi:10.4155/fmc-2019-0161 · Cited by 10

Simultaneous inhibition of TRIM24 and TRIM28 sensitises prostate cancer cells to antiandrogen therapy, decreasing VEGF signalling and angiogenesis

Leach, D. A., Chatterjee, N., Spahr, K., de Almeida, G. S., Varela‐Carver, A., Shah, T. T., Winkler, M. H., Ahmed, H. U., & Bevan, C. L. (2025) · Molecular Oncology · doi:10.1002/1878-0261.70065 · Cited by 8

Reviewing the toolbox for degrader development in oncology

Cresser-Brown, J. O., Marsh, G. P., & Maple, H. J. (2021) · Current Opinion in Pharmacology · doi:10.1016/j.coph.2021.04.009 · 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

miR-339-3p inhibits cell growth and epithelial–mesenchymal transition in nasopharyngeal carcinoma by modulating the KAT6A/TRIM24 axis

Gao, P., Zhao, K., Lu, W., Wang, L., & Zhang, P. (2022) · International Journal of Clinical Oncology · doi:10.1007/s10147-022-02231-8 · Cited by 7

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

E3 ubiquitin ligases in lung cancer: Emerging insights and therapeutic opportunities

Basu, B., Kal, S., Karmakar, S., Basu, M., & Ghosh, M. K. (2023) · Life Sciences · doi:10.1016/j.lfs.2023.122333 · Cited by 5

Exploration of bromodomain ligand-linker conjugation sites for efficient CBP/p300 heterobifunctional degrader activity

Tiwari, P. K., Doda, S. R., Vannam, R., Hudlikar, M. S., Harrison, D. A., Ojeda, S., Rai, S., Koglin, A.-S., Gilbert, A., & Ott, C. J. (2024) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2024.129676 · Cited by 6

Applied Biophysics for Bromodomain Drug Discovery

Pomerantz, W. C. K., Johnson, J. A., & Ycas, P. D. (2019) · Topics in medicinal chemistry · doi:10.1007/7355_2019_79 · Cited by 5

Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable photoPROTACsPreprint

Pfaff, P., Samarasinghe, K. T. G., Crews, C. M., & Carreira, E. M. (2019) · ChemRxiv · doi:10.26434/chemrxiv.8281469 · Cited by 7

Medicinal chemistry approaches to the discovery and development of p300/CBP inhibitors for cancer therapy

Wang, H., Song, D., Miao, M., Wu, S., Wang, J., Huang, Z., & Ding, H. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117959 · Cited by 5

Targeting E3 ubiquitin ligases to sensitize cancer radiation therapy

Chen, Z., & Xu, W. (2019) · Precision Radiation Oncology · doi:10.1002/pro6.1069 · Cited by 4

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Riching, K. M., Mahan, S. D., Urh, M., & Daniels, D. L. (2020) · Journal of Visualized Experiments · doi:10.3791/61787-v · Cited by 4

Myxoinflammatory Fibroblastic Sarcoma, Nodular-Necrotizing Variant With Two YAP1::MAML2 Fusions and TRIM24::BRAF Fusion

Harnisch, K. J., Bode‐Lesniewska, B., Chijioke, O., Hench, I. B., & Kazakov, D. V. (2025) · American Journal of Dermatopathology · doi:10.1097/dad.0000000000003107 · Cited by 3

Taking the Brakes Off Targeted Protein Degradation

Kozicka, Z., Petzold, G., & Thomä, N. H. (2020) · Cell chemical biology · doi:10.1016/j.chembiol.2019.12.010 · Cited by 3

Degradation of NSD3: What to Myc of it all?

Green, A. I., & Burslem, G. M. (2022) · Cell chemical biology · doi:10.1016/j.chembiol.2022.03.005 · Cited by 3

Targeting TRIM24 promotes neuroblastoma differentiation and decreases tumorigenicity via LSD1/CoREST complex

Shi, Q., Yu, B., Zhang, Y., Yang, Y. A., Xu, C., Zhang, M., Chen, G., Luo, F., Sun, B., Yang, R., et al. (2023) · Cellular Oncology · doi:10.1007/s13402-023-00843-4 · Cited by 3

Chemische Epigenetik: der Einfluss chemischer und chemo‐biologischer Techniken auf die Zielstruktur‐Validierung von Bromodomänen

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 · doi:10.1002/ange.201812164 · Cited by 3

Rewiring DNA repair with PARP-based chemical inducers of proximityPreprint

da Camara, B., Bilotta, E. M., Broderick, E., Premashankar, A., Barta, P. A., Carter, T. R., Hargis, L. M., Durocher, D., & Erb, M. A. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.07.26.666954 · Cited by 2

Insights into the protein domains of C-VI TRIM subfamily in viral infection

Patrick, B., Lo, Y.-C., & Su, W. (2025) · Frontiers in Cellular and Infection Microbiology · doi:10.3389/fcimb.2025.1573422 · Cited by 4

Unraveling the secrets of novel PROTACs to improve degradation efficacy

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Abstract 981: The design and characterization of a selective TRIM24 degrader

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