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Scheuermann, J.  et al.: 2024 Science of Synthesis, 2023/5: DNA-Encoded Libraries DOI: 10.1055/sos-SD-241-00252
DNA-Encoded Libraries

4.4 Selections of DNA-Encoded Libraries to Protein Targets within Living Cells

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Buch

Herausgeber: Scheuermann, J. ; Li, Y. 

Autoren: Barluenga, S. ; Bassi, G. ; Brunschweiger, A. ; Cai, B. ; Cazzamalli, S. ; Chheda, P. ; Cui, M. ; Cui, W. ; Fang, X. ; Farrera-Soler, L. ; Favalli, N. ; Feng, J.; Foley, T. L. ; Franzini, R. M. ; Georgiev, T. ; Gillingham, D. ; Gloger, A. ; Graham, J. S. ; Granados, A. ; Heiden, S.; Hou, W. ; Huang, Y. ; Keefe, A. D. ; Krusemark, C. J. ; Li, X. ; Li, Y. ; Lin, W. ; Litovchick, A.; Liu, G. ; Lu, X. ; Lucaroni, L. ; Ma, P. ; Migliorini, F. ; Molander, G. A. ; Neri, D. ; Nie, Q. ; Oehler, S. ; Prati, L. ; Puglioli, S. ; Reddavide, F. V. ; Satz, A. L. ; Sauter, B. ; Scheuermann, J. ; Schuman, D.; Simmons, N. ; Stanway-Gordon, H. A. ; Su, W. ; Sun, J. ; Thompson, M.; Vummidi, B. R.; Wang, X. ; Wang, Y. ; Wang, Z. ; Waring, M. J. ; Willems, S.; Winssinger, N. ; Xia, B. ; Xiong, F. ; Xu, H. ; Xu, L. ; Yang, G. ; Zhang, G. ; Zhang, Y. ; Zhou, Y. 

Titel: DNA-Encoded Libraries

Print ISBN: 9783132455221; Online ISBN: 9783132437357; Buch-DOI: 10.1055/b000000342

1st edition © 2024. Thieme. All rights reserved.
Georg Thieme Verlag KG, Stuttgart

Fachgebiete: Organische Chemie;Chemische Reaktionen, Katalyse;Organometallchemie;Chemische Labormethoden, Stöchiometrie

Science of Synthesis Reference Libraries



Übergeordnete Publikation

Titel: Science of Synthesis

DOI: 10.1055/b-00000101

Reihenherausgeber: Fürstner, A. (Editor-in-Chief); Carreira, E. M.; Faul, M.; Kobayashi, S.; Koch, G.; Molander, G. A.; Nevado, C.; Trost, B. M.; You, S.-L.

Typ: Mehrbändiges Werk

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B. Cai;   C. J. Krusemark 

Abstract

Selections of DNA-encoded libraries (DELs) have been largely limited to biochemically pure proteins that are immobilized on solid supports. This excludes many targets that cannot be purified or reconstituted biochemically in a fully active form. This chapter describes a method for the selection of DEL ligands against proteins within live cells. The approach relies on appending a cyclic cell-penetrating peptide to the DNA construct to deliver DELs across the cell membrane into the cytoplasm of live cells. Once inside the cell, affinity crosslinking is used to covalently trap protein–ligand interactions. The DEL ligands are isolated by subsequent purification of the target protein. This approach has demonstrated potential in selecting focused libraries against cytosolic targets that are challenging to express and purify.

Schlüsselwörter

DNA-encoded libraries - crosslinking - cyclic cell-penetrating peptides - drug discovery - selections
 
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