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Master Transcription Factors and Mediator Establish Super-Enhancers at Key Cell Identity Genes

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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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High-fidelity CRISPR-Cas9 nucleases with no detectable genome-wide off-target effects

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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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Identification of a Primary Target of Thalidomide Teratogenicity

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Believe it or not: how much can we rely on published data on potential drug targets?

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

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RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

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Phthalimide conjugation as a strategy for in vivo target protein degradation

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Mechanism of auxin perception by the TIR1 ubiquitin ligase

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An auxin-based degron system for the rapid depletion of proteins in nonplant cells

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

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Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

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Proteomic and bioinformatic analysis of mammalian SWI/SNF complexes identifies extensive roles in human malignancy

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Auxin regulates SCFTIR1-dependent degradation of AUX/IAA proteins

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Catalytic in vivo protein knockdown by small-molecule PROTACs

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Structural basis of PROTAC cooperative recognition for selective protein degradation

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Recruitment of P-TEFb for Stimulation of Transcriptional Elongation by the Bromodomain Protein Brd4

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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

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The dTAG system for immediate and target-specific protein degradation

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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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A Rapid, Reversible, and Tunable Method to Regulate Protein Function in Living Cells Using Synthetic Small Molecules

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The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

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

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The promise and peril of chemical probes

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Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15

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An Optimized microRNA Backbone for Effective Single-Copy RNAi

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A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

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The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

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Rapid protein depletion in human cells by auxin-inducible degron tagging with short homology donors

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

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Plasticity in binding confers selectivity in ligand-induced protein degradation

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Redesigning an FKBP–ligand interface to generate chemical dimerizers with novel specificity

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Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

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Defining the human C2H2 zinc finger degrome targeted by thalidomide analogs through CRBN

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Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome

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Differences in promiscuity for antibody–FcRn interactions across species: implications for therapeutic antibodies

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Chemical Genetic Control of Protein Levels: Selective in Vivo Targeted Degradation

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HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

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Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

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BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment

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A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader

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TRIM24 links a non-canonical histone signature to breast cancer

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Harnessing the anti-cancer natural product nimbolide for targeted protein degradation

Spradlin, J. N., Hu, X., Ward, C. C., Brittain, S. M., Jones, M. D., Ou, L., To, M., Proudfoot, A., Ornelas, E., Woldegiorgis, M., et al. (2019) · Nature Chemical Biology · doi:10.1038/s41589-019-0304-8 · Cited by 432 · see citing works

A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation

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Delineating the role of cooperativity in the design of potent PROTACs for BTK

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CRISPR knockout screening outperforms shRNA and CRISPRi in identifying essential genes

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Protein Knockdown Using Methyl Bestatin−Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins

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Selective degradation of splicing factor CAPERα by anticancer sulfonamides

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BRD4 is an atypical kinase that phosphorylates Serine2 of the RNA Polymerase II carboxy-terminal domain

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SLAM-seq defines direct gene-regulatory functions of the BRD4-MYC axis

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MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

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SALL4 mediates teratogenicity as a thalidomide-dependent cereblon substrate

Matyskiela, M. E., Couto, S., Zheng, X., Lu, G., Hui, J., Stamp, K., Drew, C., Ren, Y., Wang, M., Carpenter, A., et al. (2018) · Nature Chemical Biology · doi:10.1038/s41589-018-0129-x · Cited by 338 · see citing works

Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications

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BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia

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Transcription control by the ENL YEATS domain in acute leukaemia

Erb, M. A., Scott, T. G., Li, B. E., Xie, H., Paulk, J., Seo, H., Souza, A., Roberts, J. M., Dastjerdi, S., Buckley, D. L., et al. (2017) · Nature · doi:10.1038/nature21688 · Cited by 313 · see citing works

An open investigation of the reproducibility of cancer biology research

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Small‐Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

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Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands

Remillard, D., Buckley, D. L., Paulk, J., Brien, G. L., Sonnett, M., Seo, H., Dastjerdi, S., Wühr, M., Dhe‐Paganon, S., Armstrong, S. A., et al. (2017) · Angewandte Chemie International Edition · doi:10.1002/anie.201611281 · Cited by 294 · see citing works

ENL links histone acetylation to oncogenic gene expression in acute myeloid leukaemia

Wan, L., Wen, H., Li, Y., Lyu, J., Xi, Y., Hoshii, T., Joseph, J. K., Wang, X., Loh, Y. E., Erb, M. A., et al. (2017) · Nature · doi:10.1038/nature21687 · Cited by 293 · see citing works

TRIM24 Is an Oncogenic Transcriptional Activator in Prostate Cancer

Groner, A. C., Cato, L., de Tribolet-Hardy, J., Bernasocchi, T., Janoušková, H., Melchers, D., Houtman, R., Cato, A. C. B., Tschopp, P., Gu, L., et al. (2016) · Cancer Cell · doi:10.1016/j.ccell.2016.04.012 · Cited by 267 · see citing works

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

Crew, A. P., Raina, K., Dong, H., Qian, Y., Wang, J., Vigil, D., Serebrenik, Y. V., Hamman, B. D., Morgan, A., Ferraro, C., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00635 · Cited by 257 · see citing works

In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

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Tunable and reversible drug control of protein production via a self-excising degron

Chung, H. K., Jacobs, C. L., Huo, Y., Yang, J., Krumm, S. A., Plemper, R. K., Tsien, R. Y., & Lin, M. Z. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1869 · Cited by 233 · see citing works

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

Martin, L. J., Koegl, M., Bader, G., Cockcroft, X. F., Fedorov, O., Fiegen, D., Gerstberger, T., Hofmann, M. H., Hohmann, A. F., Kessler, D., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01865 · Cited by 228 · see citing works

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

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Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma

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Small-molecule displacement of a cryptic degron causes conditional protein degradation

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The Super Elongation Complex Family of RNA Polymerase II Elongation Factors: Gene Target Specificity and Transcriptional Output

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Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition

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MELK is not necessary for the proliferation of basal-like breast cancer cells

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

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