Concepedia

Development of BromoTag: A “Bump-and-Hole”–PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins

Adam G. Bond, Conner Craigon, Kwok-Ho Chan, Andrea Testa, Athanasios Karapetsas, Rotimi Fasimoye, Thomas Macartney, J. Julian Blow, Dario R. Alessi, Alessio Ciulli

Journal of Medicinal Chemistry · 2021 · 110 citations · 33 references

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Selective inhibition of BET bromodomains

P. Filippakopoulos, Jun Qi, S. Picaud et al. · Nature · 2010 · 4.3K citations · Full text

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Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules

Kenneth L. Rock, Colette F. Gramm, Lisa Rothstein et al. · Cell · 1994 · 2.5K citations

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Structural basis of PROTAC cooperative recognition for selective protein degradation

Morgan S. Gadd, Andrea Testa, Xavier Lucas et al. · Nature Chemical Biology · 2017 · 1.2K citations · Full text

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The dTAG system for immediate and target-specific protein degradation

Behnam Nabet, Justin M. Roberts, Dennis L. Buckley et al. · Nature Chemical Biology · 2018 · 1.2K citations · Full text

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Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

Michael Zengerle, Kwok-Ho Chan, Alessio Ciulli · ACS Chemical Biology · 2015 · 1K citations · Full text

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