Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von hippel-lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities

Journal of Medicinal Chemistry

Volumn 57, Issue 20, 2014, Pages 8657-8663

  Galdeano, Carles ^a,b   Gadd, Morgan S ^a   Soares, Pedro ^a   Scaffidi, Salvatore ^a   Van Molle, Inge ^b,c   Birced, Ipek ^a   Hewitt, Sarah ^b,d   Dias, David M ^b   Ciulli, Alessio ^a,b  

^a UNIVERSITY OF DUNDEE   (United Kingdom)

^b UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^c VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

^d UNIVERSITY OF LEEDS   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

HYPOXIA INDUCIBLE FACTOR 1ALPHA; LIGAND; UBIQUITIN PROTEIN LIGASE E3; VON HIPPEL LINDAU PROTEIN; HIF1A PROTEIN, HUMAN; MOLECULAR LIBRARY; PROTEIN BINDING; VHL PROTEIN, HUMAN;

ARTICLE; CHEMICAL STRUCTURE; CHIMERA; CRYSTAL STRUCTURE; ELECTROSPRAY MASS SPECTROMETRY; IN VITRO STUDY; PROTEIN DEGRADATION; PROTEIN PROTEIN INTERACTION; STRUCTURE ANALYSIS; SYNTHESIS; CHEMISTRY; HUMAN; METABOLISM; MOLECULAR LIBRARY; MOLECULARLY TARGETED THERAPY; PHARMACOLOGY; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

CRYSTALLOGRAPHY, X-RAY; HUMANS; HYPOXIA-INDUCIBLE FACTOR 1, ALPHA SUBUNIT; LIGANDS; MODELS, MOLECULAR; MOLECULAR TARGETED THERAPY; PROTEIN BINDING; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; VON HIPPEL-LINDAU TUMOR SUPPRESSOR PROTEIN;

EID: 84908373179     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm5011258     Document Type: Article

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