2018
69. Lucas, X., Van Molle, I., Ciulli, A.*
Surface probing by fragment-based screening and computational methods identifies ligandable pockets on the von Hippel-Lindau (VHL) E3 ubiquitin ligase
J. Med. Chem. 2018, 61 (16), 7387-7393
- See Figures here
- The coordinates and structure factors of our co-crystal structures are available in the PDB. Accession codes of VCB (pVHL:ElonginC:ElonginB complex) in complex with MB235 (PDB 6GMN), MB756 (PDB 6GMQ), MB1200 (PDB 6GMX), and VCBH (pVHL:ElonginC:ElonginB:HIF-1alpha complex) in complex with MB756 (PDB 6GMR)
- Listed amongst the Most Read Articles in the journal (Aug 2018)
- Highlighted in the Faculty of 1000 Prime
68. Testa, A., Lucas, X., Castro, G.V., Chan, K.-H., Wright, J.E., Runcie, A.C., Gadd, M.S., Harrison, W.T.A., Ko, E.-J., Fletcher, D., Ciulli, A.*
3-Fluoro-4-hydroxyprolines: Synthesis, conformational analysis and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation
J. Am. Chem. Soc. 2018, 140 (29), 9299-9313
- See Figures here
- The coordinates and structure factors of our co-crystal structures are available in the PDB, with accession codes: 6GFX, 6GFY and 6GFZ
- Addition/Correction published (Web): April 24, 2019. DOI: 10.1021/jacs.9b03833
67. Soares, P., Lucas, X., Ciulli, A.*
Thioamide substitution to probe the hydroxyproline recognition of VHL ligands
Bioorg. Med. Chem. 2018, 26 (11), 2992-2995
- See Figures here
- The article is a contribution to the journal’s Special Issue for the 2018 Tetrahedron Young Investigators Award for Matthew Fuchter
- The coordinates and structure factors of our co-crystal structures are available in the Protein DataBank, with accession codes: 6FMI, 6FMJ, and 6FMK
- 4th Most Downloaded Article in the journal (June 2018)
66. Amato, A., Lucas, X., Bortoluzzi, A., Wright, D., Ciulli, A.*
Targeting ligandable pockets on plant homeodomain (PHD) zinc finger domains by a fragment-based approach
ACS Chem. Biol. 2018, 13 (4), 915-921
- See Figures here
- The coordinates and structure factors of our co-crystal structures are available in the Protein DataBank, with accession codes: 6FHU, 6FKP, 6FI0, 6FAP, 6FHQ, and 6FI1
65. Runcie, A.C., Zengerle, M., Chan, K.-H., Testa, A., van Beurden, L., Baud, M.G.J., Epemolu, O., Ellis, L.C.J., Read, K.D., Coulthard, V., Brien, A. and Ciulli, A.*
Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition