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

Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation

Cromm, P. M., Samarasinghe, K. T. G., Hines, J., & Crews, C. M. (2018) · Journal of the American Chemical Society · doi:10.1021/jacs.8b08008 · Cited by 293

Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy

Ottis, P., & Crews, C. M. (2017) · ACS Chemical Biology · doi:10.1021/acschembio.6b01068 · Cited by 228

Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK)

Zhang, C., Han, X.-R., Yang, X., Jiang, B., Liu, J., Xiong, Y., & Jin, J. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.03.071 · Cited by 226

The ins and outs of tubulin acetylation: More than just a post-translational modification?

Perdiz, D., Mackeh, R., Poüs, C., & Baillet, A. (2010) · Cellular Signalling · doi:10.1016/j.cellsig.2010.10.014 · Cited by 224

Histone Deacetylase 6 in Health and Disease

Seidel, C., Schnekenburger, M., Dicato, M. A., & Diederich, M. F. (2015) · Epigenomics · doi:10.2217/epi.14.69 · Cited by 219

Selective Histone Deacetylase 6 Inhibitors Bearing Substituted Urea Linkers Inhibit Melanoma Cell Growth

Bergman, J. A., Woan, K. V., Perez-Villarroel, P., Villagra, A., Sotomayor, E. M., & Kozikowski, A. P. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm301098e · Cited by 200

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

Wu, H., Yang, K., Zhang, Z., Leisten, E. D., Li, Z., Xie, H., Liu, J., Smith, K. A., Novakova, Z., Barinka, C., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00516 · Cited by 180

Advances in CRISPR-Cas9 genome engineering: lessons learned from RNA interference

Barrangou, R., Birmingham, A., Wiemann, S., Beijersbergen, R. L., Hornung, V., & Smith, A. V. B. (2015) · Nucleic Acids Research · doi:10.1093/nar/gkv226 · Cited by 173

Design and Applications of Bifunctional Small Molecules: Why Two Heads Are Better Than One

Corson, T. W., Aberle, N. S., & Crews, C. M. (2008) · ACS Chemical Biology · doi:10.1021/cb8001792 · Cited by 171

HDAC6 α-tubulin deacetylase: A potential therapeutic target in neurodegenerative diseases

Li, G., Jiang, H., Chang, M., Xie, H., & Hu, L. (2011) · Journal of the Neurological Sciences · doi:10.1016/j.jns.2011.02.017 · Cited by 141

Developing potent PROTACs tools for selective degradation of HDAC6 protein

An, Z., Lv, W., Su, S., Wu, W., & Rao, Y. (2019) · Protein & Cell · doi:10.1007/s13238-018-0602-z · Cited by 133

Pretreatment advanced lung cancer inflammation index ( ALI ) for predicting early progression in nivolumab‐treated patients with advanced non–small cell lung cancer

Shiroyama, T., Suzuki, H., Tamiya, M., Tamiya, A., Tanaka, A., Okamoto, N., Nakahama, K., Taniguchi, Y., Isa, S., Inoue, T., et al. (2017) · Cancer Medicine · doi:10.1002/cam4.1234 · Cited by 115

Genomes in Focus: Development and Applications of CRISPR‐Cas9 Imaging Technologies

Knight, S. C., Tjian, R., & Doudna, J. A. (2017) · Angewandte Chemie International Edition · doi:10.1002/anie.201709201 · Cited by 86

Proteolysis-Targeting Chimeras: Harnessing the Ubiquitin-Proteasome System to Induce Degradation of Specific Target Proteins

Coleman, K. G., & Crews, C. M. (2017) · Annual Review of Cancer Biology · doi:10.1146/annurev-cancerbio-030617-050430 · Cited by 72

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

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