PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

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Catalytic in vivo protein knockdown by small-molecule PROTACs

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Drugging the ‘undruggable’ cancer targets

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Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

Bondeson, D. P., Smith, B. E., Burslem, G. M., Buhimschi, A. D., Hines, J., Jaime-Figueroa, S., Wang, J., Hamman, B. D., Ishchenko, A., & Crews, C. M. (2018) · Cell Chemical Biology · doi:10.1016/j.chembiol.2017.09.010 · Cited by 923 · see citing works

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

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Small‐Molecule PROTACS: New Approaches to Protein Degradation

Toure, M., & Crews, C. M. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201507978 · Cited by 674 · see citing works

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

Churcher, I. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01272 · Cited by 491 · see citing works

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

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An unstructured initiation site is required for efficient proteasome-mediated degradation

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

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Drugging the undruggables: exploring the ubiquitin system for drug development

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

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

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

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Ibrutinib for previously untreated and relapsed or refractory chronic lymphocytic leukaemia with TP53 aberrations: a phase 2, single-arm trial

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

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Multiplexed Proteome Dynamics Profiling Reveals Mechanisms Controlling Protein Homeostasis

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Non–T Cell Activation Linker (NTAL)

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Ability of Bruton’s Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling

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Small Molecules Destabilize cIAP1 by Activating Auto-ubiquitylation

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A Novel SH2-Containing Phosphatidylinositol 3,4,5-Trisphosphate 5-Phosphatase (SHIP2) Is Constitutively Tyrosine Phosphorylated and Associated With src Homologous and Collagen Gene (SHC) in Chronic Myelogenous Leukemia Progenitor Cells

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CD19 regulation of human B cell responses. B cell proliferation and antibody secretion are inhibited or enhanced by ligation of the CD19 surface glycoprotein depending on the stimulating signal used

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Efficient protein knockdown of HaloTag-fused proteins using hybrid molecules consisting of IAP antagonist and HaloTag ligand

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In situ detection of activated Bruton’s tyrosine kinase in the Ig signaling complex by phosphopeptide-specific monoclonal antibodies

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Differential Kinobeads Profiling for Target Identification of Irreversible Kinase Inhibitors

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Small molecule-mediated protein knockdown as a new approach to drug discovery

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Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: a comparative study

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CD19 differentially regulates BCR signalling through the recruitment of PI3K

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PROTAC targeted protein degraders: the past is prologue

Békés, M., Langley, D. R., & Crews, C. M. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00371-6 · Cited by 3,395 · see citing works

Targeted protein degradation: expanding the toolbox

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Chemistries of bifunctional PROTAC degraders

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Exploring Targeted Degradation Strategy for Oncogenic KRASG12C

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Recent Developments in PROTAC‐Mediated Protein Degradation: From Bench to Clinic

Hu, Z., & Crews, C. M. (2022) · ChemBioChem · doi:10.1002/cbic.202100270 · Cited by 231 · see citing works

Efficient targeted degradation via reversible and irreversible covalent PROTACs

Gabizon, R., Shraga, A., Gehrtz, P., Livnah, E., Gurwicz, N., Avram, L., Unger, T., Albeck, S., Shulman, Z., & London, N. (2020) · doi:10.26434/chemrxiv.11494398.v1 · Cited by 213 · see citing works

PROTACs: A novel strategy for cancer therapy

Liu, J., Ma, J., Liu, Y., Xia, J., Li, Y., Wang, Z. P., & Wei, W. (2020) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2020.02.006 · Cited by 186 · see citing works

Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation

Zhang, T., Hatcher, J. M., Teng, M., Gray, N. S., & Kostic, M. (2019) · Cell Chemical Biology · doi:10.1016/j.chembiol.2019.09.012 · Cited by 178 · see citing works

Improved Accuracy for Modeling PROTAC-Mediated Ternary Complex Formation and Targeted Protein Degradation <i>via</i> New <i>In Silico</i> Methodologies

Drummond, M. L., Henry, A., Li, H., & Williams, C. I. (2020) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.0c00897 · Cited by 166 · see citing works

Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta

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Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

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Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC

Yang, F., Wen, Y., Wang, C., Zhou, Y., Zhou, Y., Zhang, Z.-M., Liu, T., & Lu, X. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.114088 · Cited by 109 · see citing works

PROTAC degraders as chemical probes for studying target biology and target validation

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Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-X _L

Zhang, X., Thummuri, D., He, Y., Liu, X., Zhang, P., Zhou, D., & Zheng, G. (2019) · Chemical Communications · doi:10.1039/c9cc07217a · Cited by 86 · see citing works

PROTAC Cell Permeability and Oral Bioavailability: A Journey Into Uncharted Territory

Poongavanam, V., & Kihlberg, J. (2022) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0208 · Cited by 72 · see citing works

Monomeric Targeted Protein Degraders

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Assessing IRAK4 Functions in ABC DLBCL by IRAK4 Kinase Inhibition and Protein Degradation

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Development of covalent inhibitors: Principle, design, and application in cancer

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Development of NanoLuc-targeting protein degraders and a universal reporter system to benchmark tag-targeted degradation platforms

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Potential applications of Bruton’s tyrosine kinase inhibitors for the prevention of allergic reactions

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Development of btk Transgenic Mice

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Bruton’s tyrosine kinase (BTK) function is important to the development and expansion of chronic lymphocytic leukemia (CLL)

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Molecular studies on Burton's tyrosine kinase

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