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Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel–Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1α Stabilizers

[Image: see text] Hypoxia-inducible factor-1α (HIF-1α) constitutes the principal mediator of cellular adaptation to hypoxia in humans. The HIF-1α protein level and activity are tightly regulated by the ubiquitin E3 ligase von Hippel–Lindau (VHL). Here, we performed a structure-guided and bioactivity...

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Detalles Bibliográficos
Autores principales: Vu, Lan Phuong, Diehl, Claudia J., Casement, Ryan, Bond, Adam G., Steinebach, Christian, Strašek, Nika, Bricelj, Aleša, Perdih, Andrej, Schnakenburg, Gregor, Sosič, Izidor, Ciulli, Alessio, Gütschow, Michael
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2023
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10544018/
https://www.ncbi.nlm.nih.gov/pubmed/37708384
http://dx.doi.org/10.1021/acs.jmedchem.3c00434