Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity

[Display omitted] Proteolysis targeting chimeras (PROTACs) are heterobifunctional small-molecule degraders made of a linker connecting a target-binding moiety to a ubiquitin E3 ligase-binding moiety. The linker unit is known to influence the physicochemical and pharmacokinetic properties of PROTACs,...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2024-09, Vol.110, p.129861, Article 129861
Hauptverfasser:	Pierri, Martina, Liu, Xingui, Kroupova, Alena, Rutter, Zoe, Hallatt, Alex J., Ciulli, Alessio
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding affinity Binding Sites Conformation Cyclohexanes - chemistry Humans Ligands Linker Models, Molecular Molecular Conformation PROTAC Protein Binding Proteolysis - drug effects Stereocenter Stereoisomerism Structure-Activity Relationship VHL Von Hippel-Lindau Tumor Suppressor Protein - chemistry Von Hippel-Lindau Tumor Suppressor Protein - metabolism
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