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Plasticity in binding confers selectivity in ligand-induced protein degradation

Nature chemical biology, 2018-07, Vol.14 (7), p.706-714

2018

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Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15

Nature chemical biology, 2020-01, Vol.16 (1), p.7-14

2020

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Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)

Journal of medicinal chemistry, 2018-05, Vol.61 (9), p.4249-4255

2018

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Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2

Angewandte Chemie International Edition, 2021-07, Vol.60 (29), p.15905-15911

International ed. in English, 2021

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Development of Dual and Selective Degraders of Cyclin‐Dependent Kinases 4 and 6

Angewandte Chemie International Edition, 2019-05, Vol.58 (19), p.6321-6326

International ed. in English, 2019

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The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K

Nature (London), 2020-09, Vol.585 (7824), p.293-297

2020

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Small-molecule-induced polymerization triggers degradation of BCL6

Nature (London), 2020-12, Vol.588 (7836), p.164-168

2020

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Development of CDK2 and CDK5 Dual Degrader TMX‐2172

Angewandte Chemie International Edition, 2020-08, Vol.59 (33), p.13865-13870

International ed. in English, 2020

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Acute pharmacological degradation of Helios destabilizes regulatory T cells

Nature chemical biology, 2021-06, Vol.17 (6), p.711-717

2021

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Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library

ACS chemical biology, 2020-10, Vol.15 (10), p.2722-2730

2020

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Structure-Guided Design of a “Bump-and-Hole” Bromodomain-Based Degradation Tag

Journal of medicinal chemistry, 2021-08, Vol.64 (15), p.11637-11650

2021

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Design principles for cyclin K molecular glue degraders

Nature chemical biology, 2024-01, Vol.20 (1), p.93-102

2024

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Proteolysis-targeting chimeras with reduced off-targets

Nature chemistry, 2024-02, Vol.16 (2), p.218

2024

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Chemical Specification of E3 Ubiquitin Ligase Engagement by Cysteine-Reactive Chemistry

Journal of the American Chemical Society, 2023-10, Vol.145 (40), p.21937-21944

2023

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Targeted Degradation of the Oncogenic Phosphatase SHP2

Biochemistry (Easton), 2021-08, Vol.60 (34), p.2593-2609

2021

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Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216

Journal of medicinal chemistry, 2022-01, Vol.65 (1), p.747-756

2022

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Ubiquitin-specific proximity labeling for the identification of E3 ligase substrates

Nature chemical biology, 2024-09, Vol.20 (9), p.1227-1236

2024

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Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions

Journal of medicinal chemistry, 2023-04, Vol.66 (8), p.5524-5535

2023

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Development and Utility of a PAK1-Selective Degrader

Journal of medicinal chemistry, 2022-12, Vol.65 (23), p.15627-15641

2022

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Proteomics-Based Discovery of First-in-Class Chemical Probes for Programmed Cell Death Protein 2 (PDCD2)

Angewandte Chemie International Edition, 2023-10, Vol.62 (43), p.e202308292

International ed. in English, 2023

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Heterobifunctional Ligase Recruiters Enable pan-Degradation of Inhibitor of Apoptosis Proteins

Journal of medicinal chemistry, 2023-04, Vol.66 (7), p.4703-4733

2023

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Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity

Chembiochem : a European journal of chemical biology, 2023-10, Vol.24 (19), p.e202300141-e202300141

2023

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Development of potent and selective degraders of PI5P4Kγ

European journal of medicinal chemistry, 2023-02, Vol.247, p.115027-115027, Article 115027

2023

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A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders

European journal of medicinal chemistry, 2021-07, Vol.219, p.113435-113435, Article 113435

2021

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Multiomic profiling of breast cancer cells uncovers stress MAPK-associated sensitivity to AKT degradation

Science signaling, 2024-02, Vol.17 (825), p.eadf2670

2024

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Plasticity in binding confers selectivity in ligand-induced protein degradation

Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)

Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2

Development of Dual and Selective Degraders of Cyclin‐Dependent Kinases 4 and 6

The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K

Small-molecule-induced polymerization triggers degradation of BCL6

Development of CDK2 and CDK5 Dual Degrader TMX‐2172

Acute pharmacological degradation of Helios destabilizes regulatory T cells

Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library

Structure-Guided Design of a “Bump-and-Hole” Bromodomain-Based Degradation Tag

Design principles for cyclin K molecular glue degraders

Proteolysis-targeting chimeras with reduced off-targets

Chemical Specification of E3 Ubiquitin Ligase Engagement by Cysteine-Reactive Chemistry

Targeted Degradation of the Oncogenic Phosphatase SHP2

Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216

Ubiquitin-specific proximity labeling for the identification of E3 ligase substrates

Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions

Development and Utility of a PAK1-Selective Degrader

Proteomics-Based Discovery of First-in-Class Chemical Probes for Programmed Cell Death Protein 2 (PDCD2)

Heterobifunctional Ligase Recruiters Enable pan-Degradation of Inhibitor of Apoptosis Proteins

Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity

Development of potent and selective degraders of PI5P4Kγ

A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders

Multiomic profiling of breast cancer cells uncovers stress MAPK-associated sensitivity to AKT degradation

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