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Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1á Protein-Protein Interface

DOI: 10.1016/j.chembiol.2012.08.015 DOI Help
PMID: 23102223 PMID Help

Authors: Inge Van Molle (University of Cambridge) , Andreas Thomann (University of Cambridge) , Dennis l. Buckley (Yale University) , Ernest c. So (University of Cambridge) , Steffen Lang (University of Cambridge) , Craig m. Crews (Yale University) , Alessio Ciulli (University of Cambridge)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Chemistry & Biology , VOL 19 (10) , PAGES 1300 - 1312

State: Published (Approved)
Published: October 2012

Abstract: Inhibitors of pVHL:HIF-1á interaction are ligand-efficient and retain binding mode ► Ro3-compliant fragments of these inhibitors are not hits in biophysical screens ► Successful hit fragments break the Ro3 and target at least two subsites at the PPI ► Integration of GE and GLE analyses provide methodology to probe hot spots at a PPI

Journal Keywords: Crystallography; X-Ray; Drug; Drug; Preclinical; Hypoxia-Inducible; alpha; Models; Chemical; Protein; Tertiary; Recombinant; Small; Von Hippel-Lindau Tumor Suppressor Protein

Subject Areas: Biology and Bio-materials


Instruments: I24-Microfocus Macromolecular Crystallography

Other Facilities: ESRF Soleil