Harnessing the Power of Proteolysis for Targeted Protein Inactivation

Mechanism and medical implications of mammalian autophagy

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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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JAZ repressor proteins are targets of the SCFCOI1 complex during jasmonate signalling

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The HPV-16 E6 and E6-AP complex functions as a ubiquitin-protein ligase in the ubiquitination of p53

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Identification of a Primary Target of Thalidomide Teratogenicity

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The F-box protein TIR1 is an auxin receptor

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Cohesin Loss Eliminates All Loop Domains

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

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Phthalimide conjugation as a strategy for in vivo target protein degradation

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The Arabidopsis F-box protein TIR1 is an auxin receptor

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Targeted Degradation of CTCF Decouples Local Insulation of Chromosome Domains from Genomic Compartmentalization

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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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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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Induction of APOBEC3G Ubiquitination and Degradation by an HIV-1 Vif-Cul5-SCF Complex

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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

Zengerle, M., Chan, K.-H., & Ciulli, A. (2015) · ACS Chemical Biology · doi:10.1021/acschembio.5b00216 · Cited by 1,056 · see citing works

The SCFbeta -TRCP-ubiquitin ligase complex associates specifically with phosphorylated destruction motifs in Ikappa Balpha and beta -catenin and stimulates Ikappa Balpha ubiquitination in vitroPreprint

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Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

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Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS

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Chaperone-mediated autophagy: a unique way to enter the lysosome world

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Targeting IAP proteins for therapeutic intervention in cancer

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Structure and Function of the 26S Proteasome

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Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide

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Structure of an HIF-1α-pVHL Complex: Hydroxyproline Recognition in Signaling

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

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Structural basis for the recognition of hydroxyproline in HIF-1α by pVHL

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A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

Matyskiela, M. E., Lu, G., Ito, T., Pagarigan, B., Lu, C.-C., Miller, K., Fang, W., Wang, N.-Y., Nguyen, D., Houston, J., et al. (2016) · Nature · doi:10.1038/nature18611 · Cited by 701 · see citing works

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

Burslem, G. M., Smith, B. E., Lai, A. C., Jaime-Figueroa, S., McQuaid, D. C., Bondeson, D. P., Toure, M., Dong, H., Qian, Y., Wang, J., et al. (2018) · Cell Chemical Biology · doi:10.1016/j.chembiol.2017.09.009 · Cited by 686 · see citing works

AUTACs: Cargo-Specific Degraders Using Selective Autophagy

Takahashi, D., Moriyama, J., Nakamura, T., Miki, E., Takahashi, E., Sato, A., Akaike, T., Itto-Nakama, K., & Arimoto, H. (2019) · Molecular Cell · doi:10.1016/j.molcel.2019.09.009 · Cited by 675 · see citing works

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

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A Novel Human WD Protein, h-βTrCP, that Interacts with HIV-1 Vpu Connects CD4 to the ER Degradation Pathway through an F-Box Motif

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Identification of the receptor component of the IκBα–ubiquitin ligase

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

Schneekloth, A. R., Pucheault, M., Tae, H. S., & Crews, C. M. (2008) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2008.07.114 · Cited by 635 · see citing works

Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

Petzold, G., Fischer, E. S., & Thomä, N. H. (2016) · Nature · doi:10.1038/nature16979 · Cited by 620 · see citing works

Immunomodulatory agents lenalidomide and pomalidomide co‐stimulate <scp>T</scp> cells by inducing degradation of <scp>T</scp> cell repressors <scp>I</scp> karos and <scp>A</scp> iolos via modulation of the <scp>E</scp> 3 ubiquitin ligase complex <scp>CRL</scp> 4 <scp> ^CRBN </scp>

Gandhi, A. K., Kang, J., Havens, C. G., Conklin, T., Ning, Y., Wu, L., Ito, T., Ando, H., Waldman, M. F., Thakurta, A., et al. (2014) · British Journal of Haematology · doi:10.1111/bjh.12708 · Cited by 619 · see citing works

Modular PROTAC design for the degradation of oncogenic BCR-ABL

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Plasticity in binding confers selectivity in ligand-induced protein degradation

Nowak, R. P., DeAngelo, S. L., Buckley, D., He, Z., Donovan, K. A., An, J., Safaee, N., Jedrychowski, M. P., Ponthier, C. M., Ishoey, M., et al. (2018) · Nature Chemical Biology · doi:10.1038/s41589-018-0055-y · Cited by 615 · see citing works

Cereblon expression is required for the antimyeloma activity of lenalidomide and pomalidomide

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The auxin-inducible degradation (AID) system enables versatile conditional protein depletion in C. elegans

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Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction

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BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

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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

Sievers, Q. L., Petzold, G., Bunker, R. D., Renneville, A., Słabicki, M., Liddicoat, B. J., Abdulrahman, W., Mikkelsen, T., Ebert, B. L., & Thomä, N. H. (2018) · Science · doi:10.1126/science.aat0572 · Cited by 537 · see citing works

A Method for the Acute and Rapid Degradation of Endogenous Proteins

Clift, D., McEwan, W. A., Labzin, L. I., Konieczny, V., Mogessie, B., James, L. C., & Schuh, M. (2017) · Cell · doi:10.1016/j.cell.2017.10.033 · Cited by 531 · see citing works

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

Smith, B. E., Wang, S. L., Jaime-Figueroa, S., Harbin, A., Wang, J., Hamman, B. D., & Crews, C. M. (2019) · Nature Communications · doi:10.1038/s41467-018-08027-7 · Cited by 517 · see citing works

Fluorescent fusion protein knockout mediated by anti-GFP nanobody

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

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

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Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

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

Buckley, D. L., Raina, K., Darricarrere, N., Hines, J., Gustafson, J. L., Smith, I. E., Miah, A. H., Harling, J. D., & Crews, C. M. (2015) · ACS Chemical Biology · doi:10.1021/acschembio.5b00442 · Cited by 488 · see citing works

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

Zhang, X., Crowley, V. M., Wucherpfennig, T. G., Dix, M. M., & Cravatt, B. F. (2019) · Nature Chemical Biology · doi:10.1038/s41589-019-0279-5 · Cited by 487 · see citing works

The Molecular Basis of CRL4DDB2/CSA Ubiquitin Ligase Architecture, Targeting, and Activation

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

Huang, H.-T., Dobrovolsky, D., Paulk, J., Yang, G., Weisberg, E. L., Doctor, Z. M., Buckley, D. L., Cho, J.-H., Ko, E., Jang, J., et al. (2018) · Cell Chemical Biology · doi:10.1016/j.chembiol.2017.10.005 · Cited by 437 · see citing works

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

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Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteins

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Development of Protacs to Target Cancer-promoting Proteins for Ubiquitination and Degradation

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Targeted Protein Degradation: from Chemical Biology to Drug Discovery

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

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An expanded tool kit for the auxin‐inducible degron system in budding yeast

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Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

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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

Uehara, T., Minoshima, Y., Sagane, K., Sugi, N. H., Mitsuhashi, K. O., Yamamoto, N., Kamiyama, H., Takahashi, K., Kotake, Y., Uesugi, M., et al. (2017) · Nature Chemical Biology · doi:10.1038/nchembio.2363 · Cited by 396 · see citing works

Targeting the C481S ibrutinib-resistance mutation in Bruton’s tyrosine kinase using PROTAC-mediated degradation

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Structural basis for PRYSPRY-mediated tripartite motif (TRIM) protein function

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SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate

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

Hines, J., Lartigue, S., Dong, H., Qian, Y., & Crews, C. M. (2019) · Cancer Research · doi:10.1158/0008-5472.can-18-2918 · Cited by 348 · see citing works

SALL4 mediates teratogenicity as a thalidomide-dependent cereblon substrate

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Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7

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

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Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

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Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action

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