A novel cereblon modulator for targeted protein degradation

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

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Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

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The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins

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Structural basis of PROTAC cooperative recognition for selective protein degradation

Gadd, M. S., Testa, A., Lucas, X., Chan, K.-H., Chen, W., Lamont, D. J., Zengerle, M., & Ciulli, A. (2017) · Nature Chemical Biology · doi:10.1038/nchembio.2329 · Cited by 1,242 · see citing works

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

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Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

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Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

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PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

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The evolution of thalidomide and its IMiD derivatives as anticancer agents

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Bromodomain: an acetyl‐lysine binding domain

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BET domain co-regulators in obesity, inflammation and cancer

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The double bromodomain protein Brd4 binds to acetylated chromatin during interphase and mitosis

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Apoptotic signaling induced by immunomodulatory thalidomide analogs in human multiple myeloma cells: therapeutic implications

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Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

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Modular PROTAC design for the degradation of oncogenic BCR-ABL

Lai, A. C., Toure, M., Hellerschmied, D., Salami, J., Jaime‐Figueroa, S., Ko, E., Hines, J., & Crews, C. M. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201507634 · Cited by 618 · see citing works

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Zhou, B. N., Hu, J., Xu, F., Chen, Z., Bai, L., Fernández‐Salas, E., Lin, M., Liu, L., Yang, C., Zhao, Y., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01816 · Cited by 373 · see citing works

Growth and Early Postimplantation Defects in Mice Deficient for the Bromodomain-Containing Protein Brd4

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Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway

Lu, M., Liu, T., Jiao, Q., Ji, J., Tao, M., Liu, Y., You, Q., & Jiang, Z. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.01.063 · Cited by 310 · see citing works

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 · see citing works

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

Qin, C., Hu, Y., Zhou, B., Fernandez-Salas, E., Yang, C.-Y., Liu, L., McEachern, D., Przybranowski, S., Wang, M., Stuckey, J., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00506 · Cited by 281 · see citing works

The bromodomain revisited

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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 227 · see citing works

Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)

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Identification of cereblon-binding proteins and relationship with response and survival after IMiDs in multiple myeloma

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Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer

Bai, L., Zhou, B., Yang, C.-Y., Ji, J., McEachern, D., Przybranowski, S., Jiang, H., Hu, J., Xu, F., Zhao, Y., et al. (2017) · Cancer Research · doi:10.1158/0008-5472.can-16-2622 · Cited by 199 · see citing works

Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells

Saenz, D. T., Fiskus, W. C., Qian, Y., Manshouri, T., Rajapakshe, K., Raina, K., Coleman, K. G., Crew, A. P. A., Shen, A., Mill, C. P., et al. (2017) · Leukemia · doi:10.1038/leu.2016.393 · Cited by 184 · see citing works

Progress in the Development and Application of Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions

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THALIDOMIDE AND CONGENITAL ABNORMALITIES

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Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation

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Prime time for PROTACs

Deshaies, R. J. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1887 · Cited by 162 · see citing works

Neuropathy After Intake of Thalidomide (Distaval)

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Thalidomide as an emerging immunotherapeutic agent

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Hijacking the host ubiquitin pathway: structural strategies of bacterial E3 ubiquitin ligases

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Therapeutic targeting of BET bromodomain protein, Brd4, delays cyst growth in ADPKD

Zhou, X., Fan, L. X., Peters, D. J. M., Trudel, M., Bradner, J. E., & Li, X. (2015) · Human Molecular Genetics · doi:10.1093/hmg/ddv136 · Cited by 62 · see citing works

Two‐Headed PROTAC: An Effective New Tool for Targeted Protein Degradation

Cyrus, K., Wehenkel, M., Choi, E., Swanson, H. I., & Kim, K. (2010) · ChemBioChem · doi:10.1002/cbic.201000222 · Cited by 59 · see citing works

Absence of mutations in cereblon (CRBN) and DNA damage-binding protein 1 (DDB1) genes and significance for IMiD therapy

Thakurta, A., Gandhi, A. K., Waldman, M. F., Bjorklund, C., Ning, Y., Mendy, D., Schafer, P., Lopez-Girona, A., Lentzsch, S., Schey, S. A., et al. (2014) · Leukemia · doi:10.1038/leu.2013.315 · Cited by 56 · see citing works

First thalidomide clinical trial in multiple myeloma: a decade

van Rhee, F., Dhodapkar, M. V., Shaughnessy, J. D., Anaissie, E. J., Siegel, D. S. D., Hoering, A., Zeldis, J. B., Jenkins, B., Singhal, S., Mehta, J., et al. (2008) · Blood · doi:10.1182/blood-2008-02-140954 · Cited by 44 · see citing works

PROTAC-Induced Proteolytic Targeting

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Pharmacological Inhibition of Bromodomain-Containing Proteins in InflammationPreprint

Schaefer, U. (2014) · Cold Spring Harbor Perspectives in Biology · doi:10.1101/cshperspect.a018671 · Cited by 21 · see citing works

A third-generation IMiD for MM

Cavo, M. (2011) · Blood · doi:10.1182/blood-2011-07-364315 · Cited by 12 · see citing works

Chemistries of bifunctional PROTAC degraders

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

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PROTACs: A novel strategy for cancer therapy

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

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Cereblon vs VHL: Hijacking E3 Ligases Against Each Other Using PROTACsPreprint

Girardini, M., Maniaci, C., Hughes, S. J., et al. (2019) · ChemRxiv · doi:10.26434/chemrxiv.7698185.v1

Cereblon versus VHL: Hijacking E3 Ligases Against Each Other Using PROTACsPreprint

Girardini, M., Maniaci, C., Hughes, S. J., et al. (2019) · ChemRxiv · doi:10.26434/chemrxiv.7698185

Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs

Girardini, M., Maniaci, C., Hughes, S. J., Testa, A., & Ciulli, A. (2019) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2019.02.048 · Cited by 157 · see citing works

Cereblon versus VHL: Hijacking E3 Ligases Against Each Other Using PROTACsPreprint

Girardini, M., Maniaci, C., Hughes, S. J., et al. (2019) · ChemRxiv · doi:10.26434/chemrxiv.7698185.v2 · Cited by 3 · see citing works

A Cell-Based Target Engagement Assay for the Identification of Cereblon E3 Ubiquitin Ligase Ligands and Their Application in HDAC6 Degraders

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