Plasticity in designing PROTACs for selective and potent degradation of HDAC6

Development and Applications of CRISPR-Cas9 for Genome Engineering

Hsu, P. D., Lander, E. S., & Zhang, F. (2014) · Cell · doi:10.1016/j.cell.2014.05.010 · Cited by 5,762

Erasers of Histone Acetylation: The Histone Deacetylase EnzymesPreprint

Seto, E., & Yoshida, M. (2014) · Cold Spring Harbor Perspectives in Biology · doi:10.1101/cshperspect.a018713 · Cited by 2,105

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Lu, J., Qian, Y., Altieri, M., Dong, H., Wang, J., Raina, K., Hines, J., Winkler, J. D., Crew, A. P., Coleman, K., et al. (2015) · Chemistry & Biology · doi:10.1016/j.chembiol.2015.05.009 · Cited by 1,140

Targeted protein degradation by PROTACs

Neklesa, T. K., Winkler, J. D., & Crews, C. M. (2017) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2017.02.027 · Cited by 599

Choosing the Right Tool for the Job: RNAi, TALEN, or CRISPR

Boettcher, M., & McManus, M. T. (2015) · Molecular Cell · doi:10.1016/j.molcel.2015.04.028 · Cited by 539

HDAC6: a key regulator of cytoskeleton, cell migration and cell–cell interactions

Valenzuela-Fernández, A., Cabrero, J. R., Serrador, J. M., & Sánchez‐Madrid, F. (2008) · Trends in Cell Biology · doi:10.1016/j.tcb.2008.04.003 · Cited by 510

Histone deacetylases and cancer

Barneda‐Zahonero, B., & Parra, M. (2012) · Molecular Oncology · doi:10.1016/j.molonc.2012.07.003 · Cited by 449

Histone deacetylase 6 plays a role as a distinct regulator of diverse cellular processes

Li, Y., Shin, D., & Kwon, S. H. (2012) · FEBS Journal · doi:10.1111/febs.12079 · Cited by 351

Structural insights into HDAC6 tubulin deacetylation and its selective inhibition

Miyake, Y., Keusch, J. J., Wang, L., Saito, M., Hess, D., Wang, X., Melancon, B. J., Helquist, P., Gut, H., & Matthias, P. (2016) · Nature Chemical Biology · doi:10.1038/nchembio.2140 · Cited by 315

PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

Sun, Y., Zhao, X., Ding, N., Gao, H., Wu, Y., Yang, Y., Zhao, M., Hwang, J., Song, Y., Liu, W., et al. (2018) · Cell Research · doi:10.1038/s41422-018-0055-1 · Cited by 295

Current strategies for the design of PROTAC linkers: a critical review

Troup, R. I., Fallan, C., & Baud, M. G. J. (2020) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2020.00018 · Cited by 424

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Li, X., Pu, W., Zheng, Q., Ai, M., Chen, S., & Peng, Y. (2022) · Molecular Cancer · doi:10.1186/s12943-021-01434-3 · Cited by 389

Targeted protein degradation: advances in drug discovery and clinical practice

Zhong, G., Chang, X., Xie, W., & Zhou, X. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-02004-x · Cited by 326

PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy

Qi, S., Dong, J., Xu, Z., Cheng, X., Zhang, W., & Qin, J. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.692574 · Cited by 306

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

He, M., Cao, C., Ni, Z., Liu, Y., Song, P., Hao, S., He, Y., Sun, X., & Rao, Y. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00999-9 · Cited by 283

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

Khan, S., He, Y., Zhang, X., Yuan, Y., Pu, S., Kong, Q., Zheng, G., & Zhou, D. (2020) · Oncogene · doi:10.1038/s41388-020-1336-y · Cited by 252

Targeting histone deacetylases for cancer therapy: Trends and challenges

Liang, T., Wang, F., Elhassan, R. M., Cheng, Y., Tang, X., Chen, W., Fang, H., & Hou, X. (2023) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2023.02.007 · Cited by 222

Anticancer Therapy with HDAC Inhibitors: Mechanism-Based Combination Strategies and Future Perspectives

Jenke, R., Reßing, N., Hansen, F. K., Aigner, A. M., & Büch, T. (2021) · Cancers · doi:10.3390/cancers13040634 · Cited by 198

Developments of CRBN-based PROTACs as potential therapeutic agents

Wang, C., Zhang, Y., Wu, Y., & Xing, D. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113749 · Cited by 158

Characteristic roadmap of linker governs the rational design of PROTACs

Dong, Y., Ma, T., Xu, T., Feng, Z., Li, Y., Song, L., Yao, X., Ashby, C. R., & Hao, G.-F. (2024) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2024.04.007 · Cited by 146

Epigenetic regulation in hematopoiesis and its implications in the targeted therapy of hematologic malignancies

Zhao, A., Zhou, H., Yang, J., Li, M., & Niu, T. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01342-6 · Cited by 153

Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs

Xiao, Y., Wang, J., Zhao, L., Chen, X., Zheng, G., Zhang, X., & Liao, D. (2020) · Chemical Communications · doi:10.1039/d0cc03243c · Cited by 131

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies

He, Y., Khan, S., Huo, Z., Lv, D., Zhang, X., Liu, X., Yuan, Y., Hromas, R., Xu, M., Zheng, G., et al. (2020) · Journal of Hematology & Oncology · doi:10.1186/s13045-020-00924-z · Cited by 126

Strategies for designing proteolysis targeting chimaeras (PROTACs)

He, S., Dong, G., Cheng, J., Wu, Y., & Sheng, C. (2022) · Medicinal Research Reviews · doi:10.1002/med.21877 · Cited by 120

A bibliometric analysis of PROTAC from 2001 to 2021

Li, D., Yu, D., Li, Y., & Yang, R. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114838 · Cited by 125

Development of Selective Histone Deacetylase 6 (HDAC6) Degraders Recruiting Von Hippel–Lindau (VHL) E3 Ubiquitin Ligase

Yang, K., Wu, H., Zhang, Z., Leisten, E. D., Nie, X., Liu, B., Wen, Z., Zhang, J., Cunningham, M. D., & Tang, W. (2020) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.0c00046 · Cited by 124

Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1

Hu, M., Zhou, W., Wang, Y., Yao, D., Ye, T., Yao, Y., Chen, B., Liu, G., Yang, X., Wang, W., et al. (2020) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2020.02.010 · Cited by 117

HDAC-targeting epigenetic modulators for cancer immunotherapy

Cheng, B., Pan, W., Xiao, Y., Ding, Z., Zhou, Y., Fei, X., Liu, J., Su, Z., Peng, X., & Chen, J. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116129 · Cited by 116

Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo

Luo, G., Li, Z., Lin, X., Li, X., Chen, Y., Xi, K., Xiao, M., Wei, H., Zhu, L., & Xiang, H. (2020) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2020.11.001 · Cited by 84

Overview of epigenetic degraders based on PROTAC, molecular glue, and hydrophobic tagging technologies

Peng, X., Hu, Z., Zeng, L., Zhang, M., Xu, C., Lu, B., Tao, C., Chen, W., Hou, W., Cheng, K., et al. (2023) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2023.09.003 · Cited by 87

Targeting the Ubiquitin-Proteasome System for Cancer Therapeutics by Small-Molecule Inhibitors

LaPlante, G., & Zhang, W. (2021) · Cancers · doi:10.3390/cancers13123079 · Cited by 88

HDAC Inhibitors: Innovative Strategies for Their Design and Applications

Daśko, M., de Pascual‐Teresa, B., Ortín, I., & Ramos, A. (2022) · Molecules · doi:10.3390/molecules27030715 · Cited by 80

Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity

Sinatra, L., Yang, J. C., Schliehe‐Diecks, J., Dienstbier, N., Vogt, M., Gebing, P., Bachmann, L. M., Sönnichsen, M., Lenz, T., Stühler, K., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01659 · Cited by 74

Attenuation of NLRP3 Inflammasome Activation by Indirubin-Derived PROTAC Targeting HDAC6

Cao, Z., Gu, Z., Lin, S., Chen, D., Wang, J., Zhao, Y., Li, Y., Liu, T., Li, Y., Wang, Y., et al. (2021) · ACS Chemical Biology · doi:10.1021/acschembio.1c00681 · Cited by 71

PROTACs: A novel strategy for cancer drug discovery and development

Han, X., & Sun, Y. (2023) · MedComm · doi:10.1002/mco2.290 · Cited by 69

Targeting Histone Deacetylases: Opportunities for Cancer Treatment and Chemoprevention

Ružić, D., Djoković, N., Srdić‐Rajić, T., Echeverría, C., Nikolic, K. M., & Santibanez, J. F. (2022) · Pharmaceutics · doi:10.3390/pharmaceutics14010209 · Cited by 69

Recent Advances of Degradation Technologies Based on PROTAC Mechanism

Xiao, M., Zhao, J., Wang, Q., Liu, J., & Ma, L. (2022) · Biomolecules · doi:10.3390/biom12091257 · Cited by 69

Journey of PROTAC: From Bench to Clinical Trial and Beyond

Berkley, K., Zalejski, J., Sharma, N., & Sharma, A. K. (2025) · Biochemistry · doi:10.1021/acs.biochem.4c00577 · Cited by 62

Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation

He, M., Lv, W., & Rao, Y. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.685106 · Cited by 63

Discovery of a PROTAC targeting ALK with in vivo activity

Yan, G., Zhong, X.-X., Lin, Y., Pu, C., Shan, H., Lan, S., Zhou, M., Hou, X., Yang, J., & Li, R. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.113150 · Cited by 59

Development of the first non-hydroxamate selective HDAC6 degraders

Keuler, T., König, B., Bückreiß, N., Kraft, F. B., König, P., Schäker‐Hübner, L., Steinebach, C., Bendas, G., Gütschow, M., & Hansen, F. K. (2022) · Chemical Communications · doi:10.1039/d2cc03712b · Cited by 54

HDAC3 and HDAC8 PROTAC dual degrader reveals roles of histone acetylation in gene regulation

Xiao, Y., Hale, S. M., Awasthee, N., Meng, C., Zhang, X., Liu, Y., Ding, H., Huo, Z., Lv, D., Zhang, W., et al. (2023) · Cell chemical biology · doi:10.1016/j.chembiol.2023.07.010 · Cited by 54

Selective degradation of PARP2 by PROTACs via recruiting DCAF16 for triple-negative breast cancer

Pu, C., Tong, Y., Liu, Y., Lan, S., Wang, S., Yan, G., Zhang, H., Luo, D., Ma, X., Yu, S., et al. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114321 · Cited by 54

Discovery of pomalidomide-based PROTACs for selective degradation of histone deacetylase 8

Sun, Z., Deng, B., Yang, Z., Mai, R., Huang, J., Ma, Z., Chen, T., & Chen, J. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114544 · Cited by 46

Bifunctional HDAC Therapeutics: One Drug to Rule Them All?

Smalley, J. P., Cowley, S. M., & Hodgkinson, J. T. (2020) · Molecules · doi:10.3390/molecules25194394 · Cited by 48

Small molecules targeting HDAC6 for cancer treatment: Current progress and novel strategies

Huang, Z., Li, L., Cheng, B., & Li, D. (2024) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2024.117218 · Cited by 46

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

Degraders in epigenetic therapy: PROTACs and beyond

Dai, X., Ji, S., Fu, M., Liu, G.-Z., Liu, H., Wang, S., Shen, L., Wang, N., Herdewijn, P. A., Zheng, Y., et al. (2024) · Theranostics · doi:10.7150/thno.92526 · Cited by 45

Advancements in Hydrazide-Based HDAC Inhibitors: A Review of Recent Developments and Therapeutic Potential

Raucci, A., Zwergel, C., Valente, S., & Mai, A. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c01677 · Cited by 43

Pharmacological inhibition of HDAC6 suppresses NLRP3 inflammasome-mediated IL-1β release

Bockstiegel, J., Wurnig, S. L., Engelhardt, J., Enns, J., Hansen, F. K., & Weindl, G. (2023) · Biochemical Pharmacology · doi:10.1016/j.bcp.2023.115693 · Cited by 40

PROTACs in Epigenetic Cancer Therapy: Current Status and Future Opportunities

Liu, X., Wang, A., Shi, Y., Dai, M., Liu, M., & Cai, H. (2023) · Molecules · doi:10.3390/molecules28031217 · 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

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

HDAC6—An Emerging Target Against Chronic Myeloid Leukemia?

Losson, H., Schnekenburger, M., Dicato, M. A., & Diederich, M. F. (2020) · Cancers · doi:10.3390/cancers12020318 · Cited by 36

Designing an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells

Liu, Y., Zhen, Y., Wang, G., Yang, G., Fu, L., Liu, B., & Ouyang, L. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112505 · Cited by 34

Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer’s disease

Li, Y., Lin, S., Gu, Z., Chen, L., & He, B. (2022) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2022.129015 · Cited by 34

Histone Deacetylases as Epigenetic Targets for Treating Parkinson’s Disease

Li, Y., Gu, Z., Lin, S., Chen, L., Dzreyan, V., Eid, M., Demyanenko, S. V., & He, B. (2022) · Brain Sciences · doi:10.3390/brainsci12050672 · Cited by 31

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

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 novel anti-angiogenesis agents. Part 11: Development of PROTACs based on active molecules with potency of promoting vascular normalization

Shan, Y., Si, R., Wang, J., Zhang, Q., Li, J., Ma, Y., & Zhang, J. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112654 · 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

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

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

Degradation of histone deacetylase 6 alleviates ROS-mediated apoptosis in renal ischemia-reperfusion injury

Xia, K., Qiu, T., Jian, Y., Liu, H., Chen, H., Liu, X., Chen, Z., & Wang, L. (2023) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2023.115128 · Cited by 25

PROTAC chemical probes for histone deacetylase enzymes

Patel, U., Smalley, J. P., & Hodgkinson, J. T. (2023) · RSC Chemical Biology · doi:10.1039/d3cb00105a · Cited by 25

Development of a Bestatin-SAHA Hybrid with Dual Inhibitory Activity against APN and HDAC

Cao, J., Zhao, W., Zhao, C., Liu, Q., Li, S., Zhang, G., Chou, C. J., & Zhang, Y. (2020) · Molecules · doi:10.3390/molecules25214991 · Cited by 25

Role of Histone Deacetylase 6 and Histone Deacetylase 6 Inhibition in Colorectal Cancer

Vuletić, A. M., Martinović, K. M., & Spasić, J. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics16010054 · Cited by 24

Rational Proteolysis Targeting Chimera Design Driven by Molecular Modeling and Machine Learning

Tan, S., Chen, Z., Lu, R., Liu, H., & Yao, X. (2025) · Wiley Interdisciplinary Reviews Computational Molecular Science · doi:10.1002/wcms.70013 · Cited by 24

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

Identification of mercaptoacetamide-based HDAC6 inhibitors via a lean inhibitor strategy: screening, synthesis, and biological evaluation

Geurs, S., Clarisse, D., Baele, F., Franceus, J., Desmet, T., Bosscher, K. D., & D’hooghe, M. (2022) · Chemical Communications · doi:10.1039/d2cc01550a · Cited by 20

Recent Advances in Small Molecular Modulators Targeting Histone Deacetylase 6

Xiao, Y., & Zhang, X. (2020) · Future Drug Discovery · doi:10.4155/fdd-2020-0023 · Cited by 20

Design, Synthesis, and Biological Evaluation of HDAC Degraders with CRBN E3 Ligase Ligands

Lu, Y., Sun, D., Xiao, D., Shao, Y.-Y., Su, M., Zhou, Y., Li, J. X., Zhu, S., & Lu, W. P. (2021) · Molecules · doi:10.3390/molecules26237241 · Cited by 21

Targeting micro-environmental pathways by PROTACs as a therapeutic strategy

Liu, J., Peng, Y., Inuzuka, H., & Wei, W. (2022) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2022.07.001 · Cited by 20

Development of the First-in-Class FEM1B-Recruiting Histone Deacetylase Degraders

Feller, F., Honin, I., Miranda, M., Weber, H. B., Henze, S., Hanl, M., & Hansen, F. K. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c02569 · Cited by 19

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

Exploring the landscape of post-translational modification in drug discovery

Cao, Y., Yu, T., Zhu, Z., Zhang, Y., Sun, S., Li, N., Gu, C., & Yang, Y. (2024) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2024.108749 · Cited by 17

Discovery of Novel Proteolysis-Targeting Chimera Molecules as Degraders of Programmed Cell Death-Ligand 1 for Breast Cancer Therapy

Zhang, H., Zhang, Y., Feng, Z., Shuai, M., Ma, X., Wang, S., Yu, S., Deng, R., Luo, D., Shi, J., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c02259 · Cited by 15

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

Discovery of the cereblon-recruiting tubulin PROTACs effective in overcoming Taxol resistance in vitro and in vivo

Yang, H., Qin, J., Pei, Y., Guan, S., Zhao, M., Wang, Y., Yao, Y., Duan, Y., & Sun, M. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.116067 · Cited by 14

Cereblon: promise and challenges for combating human diseases

Kim, H. K., Seol, J. E., Ahn, S. W., Jeon, S., Park, C., & Han, J. (2021) · Pflügers Archiv - European Journal of Physiology · doi:10.1007/s00424-021-02624-0 · Cited by 14

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

Proteolysis-Targeting Chimeras (PROTACs) Based on Macrocyclic Tetrapeptides Selectively Degrade Class I Histone Deacetylases 1–3Preprint

Roatsch, M., Vogelmann, A., Herp, D., Jung, M., & Olsen, C. A. (2020) · ChemRxiv · doi:10.26434/chemrxiv.12416303.v1 · Cited by 14

Targeting intracellular proteins with cell type-specific functions for cancer immunotherapy

Carelock, M. E., Master, R. P., Kim, M., Jin, Z., Wang, L. A., Maharjan, C. K., Hua, N., De, U., Kolb, R. H., Xiao, Y., et al. (2023) · Life Medicine · doi:10.1093/lifemedi/lnad019 · Cited by 13

The Role of HDAC6 in Glioblastoma Multiforme: A New Avenue to Therapeutic Interventions?

Spallotta, F., & Illi, B. (2024) · Biomedicines · doi:10.3390/biomedicines12112631 · Cited by 13

Development and Characterization of the First Selective Class IIb Histone Deacetylase Degraders

Zhai, S., Honin, I., Schäker‐Hübner, L., Hanl, M., Jacobi, L., Dressler, F., Pieńkowska, D. E., König, P., Gerhartz, J., Voget, R., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00674 · 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

Epigenetic therapy meets targeted protein degradation: HDAC-PROTACs in cancer treatment

Hussain, M. S., Zhang, L., Rana, A. J., Maqbool, M., Ashique, S., Khan, Y., Jakhmola, V., Hanbashi, A., Mawkili, W., & Khan, G. (2025) · Future Medicinal Chemistry · doi:10.1080/17568919.2025.2533113 · Cited by 10

PROTACs targeting epigenetic proteins

Zhang, C., He, Y., Sun, X., Wei, W., Liu, Y., & Rao, Y. (2023) · Acta Materia Medica · doi:10.15212/amm-2023-0039 · Cited by 13

PROTAC‐Based HDAC Degradation: A Paradigm Shift in Targeted Epigenetic Therapies

Himaja, A., Halder, D., Banerjee, S., Biswas, S., Adhikari, N., & Ghosh, B. (2025) · ChemMedChem · doi:10.1002/cmdc.202500203 · Cited by 9

Histone deacetylase 6: a potential therapeutic target for drug development

Li, Z., Zhu, H., Wang, X., Zhang, L., & Zhang, L. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.108932 · Cited by 7

Developing PROteolysis TArgeting Chimeras (PROTACs) for hematologic malignancies

Wu, Y., Zhang, J., Zhu, X., & Zhang, Y. (2022) · Cancer Letters · doi:10.1016/j.canlet.2022.215808 · Cited by 8

Proteasomal Degradation of Zn-Dependent Hdacs: The E3-Ligases Implicated and the Designed Protacs That Enable Degradation

Márquez-Cantudo, L., Ramos, A., Coderch, C., & de Pascual‐Teresa, B. (2021) · Molecules · doi:10.3390/molecules26185606 · Cited by 8

Proteolysis-Targeting Chimeras (PROTACs) Based on Macrocyclic Tetrapeptides Selectively Degrade Class I Histone Deacetylases 1–3Preprint

Roatsch, M., Vogelmann, A., Herp, D., Jung, M., & Olsen, C. A. (2020) · ChemRxiv · doi:10.26434/chemrxiv.12416303 · Cited by 6

Reversing TGF-β1-induced fibrotic phenotype in human lung fibroblasts using a PROTAC tool derived from an indoline-based HDAC6 inhibitor

Cursaro, I., Ciccone, V., Tudino, V., Papulino, C., Scalvini, L., Donnini, S., Morbidelli, L., Bini, L., Landi, C., Contri, C., et al. (2025) · European Journal of Medicinal Chemistry Reports · doi:10.1016/j.ejmcr.2025.100276 · Cited by 5

HDAC6 mediates tumorigenesis during mitosis and the development of targeted deactivating agents

Peng, J., Liu, H., Liu, Y., Liu, J., Zhao, Q., Liu, W., Niu, H., Xue, H., Sun, J., & Wu, J. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2024.107818 · Cited by 5

Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activityPreprint

Sinatra, L., Yang, J., Schliehe‐Diecks, J., Dienstbier, N., Vogt, M., Gebing, P., Bachmann, L. M., Sönnichsen, M., Lenz, T., Stühler, K., et al. (2022) · ChemRxiv · doi:10.26434/chemrxiv-2022-dntx4-v2 · Cited by 5

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

Prospects and advances of PROTAC in the treatment of hematologic malignancies

Wang, X., Zhang, M., & Mei, H. (2026) · Experimental Hematology and Oncology · doi:10.1186/s40164-026-00759-3 · Cited by 3

Unlocking the therapeutic potential of HDAC inhibitors in colorectal cancer: Mechanisms, efficacy, and future perspectives

Wen, Y., Yang, C., Ye, Y., Shen, Z., & Wang, C. (2025) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2025.104920 · Cited by 3

Recent Innovative Advances in the Discovery of Selective HDAC6 Inhibitors

Tavares, M. T., & Shen, S. (2021) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0040 · Cited by 3

Targeted Protein Degradation by Proteolysis Targeting Chimeras

Du, W. (2022) · Wiley eBooks · doi:10.1002/9781119627784.ch11 · Cited by 2

The Chicken HDAC4 Promoter and Its Regulation by MYC and HIF1A

Wang, Y., Kong, R., Xie, K., Wang, X., Wu, H., & Zhang, Y. (2024) · Genes · doi:10.3390/genes15121518 · Cited by 1

PROTACs in cancer therapy: targeted degradation of GPX4, PARP and epigenetic regulators

Periyasamy, S., Jarrett, T., Truong, J., & Skouta, R. (2026) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2026.2636394 · Cited by 2

Bifunctional proximity-inducing strategies for targeted and programmable post-translational modifications

Tanga, S., Das, P., Samoi, T. B., Hota, A., Karmakar, A., & Maji, B. (2026) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2026.115874 · Cited by 1

Histone Deacetylase Meets Protein Degradation: Accelerating Anticancer Drug Discovery

Wang, J.-J., Gao, Y., Ji, X.-Q., Yin, J.-Y., Zhang, M., Wang, B., Liu, H., Feng, S., Wang, N., Lu, G., et al. (2026) · Medicinal Research Reviews · doi:10.1002/med.70052 · Cited by 2

Discovery of a Selective Histone Deacetylase 6 Degrader (HDAC6 PROTAC) with a Short and Rigid Linker Demonstrating Sustained Knockdown of HDAC6 In Vivo

Ripa, L., Cassani, C., Hughes, G. A., Ranieri, B., Ullah, V., Zambelloni, R., Andreasson, T., Collins, M., Lindberg, B., Llinàs, A., et al. (2026) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.6c00086 · Cited by 2

Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activityPreprint

Sinatra, L., Yang, J., Schliehe‐Diecks, J., Dienstbier, N., Voigt, M., Gebing, P., Bachmann, L. M., Sönnichsen, M., Lenz, T., Stühler, K., et al. (2022) · ChemRxiv · doi:10.26434/chemrxiv-2022-dntx4

Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activityPreprint

Sinatra, L., Yang, J., Schliehe‐Diecks, J., Dienstbier, N., Vogt, M., Gebing, P., Bachmann, L. M., Sönnichsen, M., Lenz, T., Stühler, K., et al. (2022) · ChemRxiv · doi:10.26434/chemrxiv-2022-dntx4-v3

Targeted Protein Degradation of Metalloenzymes

O’Herin, C., & Cohen, S. M. (2025) · Wiley eBooks · doi:10.1002/0471266949.bmc303

Rapid Two-Step Multicomponent Synthesis and Structure-degradation Relationships of Selective HDAC6 PROTAC Degraders

Tsymliakov, M., Hanl, M., Enns, J., Zhai, S., Ferretti, E., König, P., Kousa, R., Tu, J., Steinebach, C., Gütschow, M., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c02045 · Cited by 1

Development of Ethyl-Hydrazide-Based Selective Histone Deacetylase 6 (HDAC6) PROTACs

Stopper, D., Honin, I., Feller, F., & Hansen, F. K. (2025) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.5c00033 · Cited by 14

Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activityPreprint

Sinatra, L., Yang, J., Schliehe‐Diecks, J., Dienstbier, N., Vogt, M., Gebing, P., Bachmann, L. M., Sönnichsen, M., Lenz, T., Stühler, K., et al. (2022) · ChemRxiv · doi:10.26434/chemrxiv-2022-dntx4-v2 · Cited by 5

Target engagement studies and kinetic live-cell degradation assays enable the systematic characterization of HDAC6 PROTACsPreprint

Hanl, M., Feller, F., Honin, I., Tan, K., Miranda, M., Schäker-Hübner, L., Bückreiß, N., Schiedel, M., Gütschow, M., Bendas, G., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.03.31.646177

Discovery of a Selective Histone Deacetylase 6 Degrader (HDAC6 PROTAC) with a Short and Rigid Linker Demonstrating Sustained Knockdown of HDAC6 In Vivo

Ripa, L., Cassani, C., Hughes, G. A., Ranieri, B., Ullah, V., Zambelloni, R., Andreasson, T., Collins, M., Lindberg, B., Llinàs, A., et al. (2026) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.6c00086 · Cited by 2