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Editor All books published by WILEY-VCH are carefully erm
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Preface xiii nline L
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1.2.4 Milestone 4: PROTACs on the Rise – Small-Molecule Degraders Achieve iley.com
in vivo PoC 8 /term
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1.2.7.1 Itrsa TnPscDr iJputsiot nthael MBeogdiinfinciantgio?n B ifu1n5ctional Modulators of Post- iley Online L
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2.3.1 Dtheeg Eraxdtraaticoenll ufrloamr S tphaec eP las3m4a Membrane (PM) and the Extracellular ragab - C
Space 35 ochrane G
2.3.1.1 Internalization at the PM and Endosomal Sorting 35 erm
2.3.1.2 Ubiquitination at the PM 37 any , W
2.3.2 Degradation from the Endoplasmic Reticulum (ER) 39 iley O
2.3.2.1 ER-Associated Protein Degradation (ERAD) – Proteoasomal Degradation nline L
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3.2.1 Regulating E3 Ligases Activity 66 iley.com
3.3 RING E3 Ligases 67 /term
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3.4.1 Definition and Discovery 73 iley O
3.4.2 Subgroups 73 nline L
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33..56. 2 I Cnosnigchlutss iionnto a Tndh eIinr sRigehgtusl aintitoon D arnudg FDuenvcetlioopnm e8n5t 86 Contents vii https://onlinelibrary.w
References 87 iley.com
4 ATe Srntraurcyt uCoraml palnedx BFioorpmhaytsiiocna l P1e0rs7pective of Degrader Activity Through /doi/ by ibrahim
4.1 M Inotrrgoadnu cSt. iGonad d 1a0n7d Marine C. Aublette ragab - C
4.1.1 Mechanism of Degraders Through Ternary Complexes 108 ochrane G
4.1.2 Ternary Complex Behavior 108 erm
4.1.2.1 Binding Pose 108 any , W
4.1.2.2 Affinity and Cooperativity 108 iley O
4.1.2.3 Stoichiometry 110 nline L
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4.2.2.2 Molecular Glues Recruiting Other E3 Ligases 136 iley.com
4.3 Future Perspective on the Importance of Ternary Complexes in PROTAC /term
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66..22..11..21 MMoolleeccuullaarr GGlluuee sD e1g7ra9ders 182 ragab - C
6.2.2 Synthetic Compounds 182 ochrane G
6.2.2.1 Molecular Glues 182 erm
6.2.2.2 Molecular Glue Degraders 183 any , W
6.3 Synthetic Molecular Glue Degraders: Serendipitous iley O
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6.4.5 Discovery of VHL-Binding Molecular Glue Degraders 193 iley.com
6.5 Conclusions and Outlook 193 /term
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7.1 Introduction 205 nline L
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8 IXniasiogyhut sZ haanndg Future Perspectives of Covalent Protein Degraders 2C1o5ntents ix https://onlinelibrary.w
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88..22..23 MKREATAS PG21 2aCnd B2T2K0 218 ragab - C
8.2.4 EGFR, ERK1/2, and ERRα 221 ochrane G
8.2.5 Monofunctional Protein Degraders 223 erm
8.3 Protein Degraders that Covalently Interact with E3 Ubiquitin any , W
Ligases 224 iley O
8.3.1 RNF4 224 nline L
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Andrei Ursu, Barbara Herdy and Hendrik Osadnik iley.com
9.1 Introduction 245 /term
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Regulation 251 iley O
9.3.2.1 Activating a Weak Splice Site in SMN2 to Increase Protein nline L
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9.4.3.3 RDIisBeOasTeAsC -M26e3diated Degradation of Pre-miR-21 via Targeted Recruitment ragab - C
of RNase L 263 ochrane G
9.5 Conclusions 265 erm
References 266 any , W
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10.11 Potential Applications of Heterobifunctional Compounds to Modulate iley.com
PTMS 283 /term
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Discovery 289 iley O
Paola Martinelli, Christiane Kofink, Georg Boeck, Harald Weinstabl and nline L
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1 1.5 T Raerfgereetendc ePsr ot3e0in8 Degradation: Here to Stay 307 ragab - C
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12 Taming the Beast: How to Optimize DMPK–PD Properties of Oral erm
Degraders 313 any , W
Caroline Rynn, Arthur Van De Vyver, Antje Walz, Carina Cantrill and iley O
Matthias Wittwer nline L
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12.2.3 Translational PK/PD and Human Dose Prediction for Targeted Protein iley.com
Degraders 330 /term
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Tools to Clinical Candidates 337 iley O
Erika M.V. Araujo and Keith R. Hornberger nline L
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