| Year |
Citation |
Score |
| 2023 |
Ramachandran S, Makukhin N, Haubrich K, Nagala M, Forrester B, Lynch DM, Casement R, Testa A, Bruno E, Gitto R, Ciulli A. Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2. Nature Communications. 14: 6345. PMID 37816714 DOI: 10.1038/s41467-023-41894-3 |
0.728 |
|
| 2023 |
Vu LP, Diehl CJ, Casement R, Bond AG, Steinebach C, Strašek N, Bricelj A, Perdih A, Schnakenburg G, Sosič I, Ciulli A, Gütschow M. 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. Journal of Medicinal Chemistry. 66: 12776-12811. PMID 37708384 DOI: 10.1021/acs.jmedchem.3c00434 |
0.321 |
|
| 2023 |
Liu X, Ciulli A. Proximity-Based Modalities for Biology and Medicine. Acs Central Science. 9: 1269-1284. PMID 37521793 DOI: 10.1021/acscentsci.3c00395 |
0.314 |
|
| 2023 |
Haubrich K, Spiteri VA, Farnaby W, Sobott F, Ciulli A. Breaking free from the crystal lattice: Structural biology in solution to study protein degraders. Current Opinion in Structural Biology. 79: 102534. PMID 36804675 DOI: 10.1016/j.sbi.2023.102534 |
0.315 |
|
| 2023 |
Wijaya AJ, Farnaby W, Ciulli A. Crystallization of VHL-based PROTAC-induced ternary complexes. Methods in Enzymology. 681: 241-263. PMID 36764760 DOI: 10.1016/bs.mie.2022.10.005 |
0.302 |
|
| 2022 |
Kofink C, Trainor N, Mair B, Wöhrle S, Wurm M, Mischerikow N, Roy MJ, Bader G, Greb P, Garavel G, Diers E, McLennan R, Whitworth C, Vetma V, Rumpel K, ... ... Ciulli A, et al. A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo. Nature Communications. 13: 5969. PMID 36216795 DOI: 10.1038/s41467-022-33430-6 |
0.346 |
|
| 2022 |
Liu X, Kalogeropulou AF, Domingos S, Makukhin N, Nirujogi RS, Singh F, Shpiro N, Saalfrank A, Sammler E, Ganley IG, Moreira R, Alessi DR, Ciulli A. Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood-Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2. Journal of the American Chemical Society. PMID 36007011 DOI: 10.1021/jacs.2c05499 |
0.338 |
|
| 2022 |
Diehl CJ, Ciulli A. Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders. Chemical Society Reviews. PMID 35983982 DOI: 10.1039/d2cs00387b |
0.441 |
|
| 2022 |
Grohmann C, Magtoto CM, Walker JR, Chua NK, Gabrielyan A, Hall M, Cobbold SA, Mieruszynski S, Brzozowski M, Simpson DS, Dong H, Dorizzi B, Jacobsen AV, Morrish E, Silke N, ... ... Ciulli A, et al. Development of NanoLuc-targeting protein degraders and a universal reporter system to benchmark tag-targeted degradation platforms. Nature Communications. 13: 2073. PMID 35440107 DOI: 10.1038/s41467-022-29670-1 |
0.336 |
|
| 2022 |
Cowan AD, Ciulli A. Driving E3 Ligase Substrate Specificity for Targeted Protein Degradation: Lessons from Nature and the Laboratory. Annual Review of Biochemistry. PMID 35320687 DOI: 10.1146/annurev-biochem-032620-104421 |
0.416 |
|
| 2022 |
Webb T, Craigon C, Ciulli A. Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective. Bioorganic & Medicinal Chemistry Letters. 63: 128653. PMID 35257896 DOI: 10.1016/j.bmcl.2022.128653 |
0.321 |
|
| 2021 |
Tarantelli C, Cannas E, Ekeh H, Moscatello C, Gaudio E, Cascione L, Napoli S, Rech C, Testa A, Maniaci C, Rinaldi A, Zucca E, Stathis A, Ciulli A, Bertoni F. The bromodomain and extra-terminal domain degrader MZ1 exhibits preclinical anti-tumoral activity in diffuse large B-cell lymphoma of the activated B cell-like type. Exploration of Targeted Anti-Tumor Therapy. 2: 586-601. PMID 36046113 DOI: 10.37349/etat.2021.00065 |
0.314 |
|
| 2021 |
Müller S, Ackloo S, Al Chawaf A, Al-Lazikani B, Antolin A, Baell JB, Beck H, Beedie S, Betz UAK, Bezerra GA, Brennan PE, Brown D, Brown PJ, Bullock AN, Carter AJ, ... ... Ciulli A, et al. Target 2035 - update on the quest for a probe for every protein. Rsc Medicinal Chemistry. 13: 13-21. PMID 35211674 DOI: 10.1039/d1md00228g |
0.55 |
|
| 2021 |
Laveglia V, Giachetti A, Cerofolini L, Haubrich K, Fragai M, Ciulli A, Rosato A. Automated Determination of Nuclear Magnetic Resonance Chemical Shift Perturbations in Ligand Screening Experiments: The PICASSO Web Server. Journal of Chemical Information and Modeling. 61: 5726-5733. PMID 34843238 DOI: 10.1021/acs.jcim.1c00871 |
0.317 |
|
| 2021 |
Imaide S, Riching KM, Makukhin N, Vetma V, Whitworth C, Hughes SJ, Trainor N, Mahan SD, Murphy N, Cowan AD, Chan KH, Craigon C, Testa A, Maniaci C, Urh M, ... ... Ciulli A, et al. Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity. Nature Chemical Biology. 17: 1157-1167. PMID 34675414 DOI: 10.1038/s41589-021-00878-4 |
0.422 |
|
| 2021 |
Bond AG, Craigon C, Chan KH, Testa A, Karapetsas A, Fasimoye R, Macartney T, Blow JJ, Alessi DR, Ciulli A. Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. Journal of Medicinal Chemistry. PMID 34652918 DOI: 10.1021/acs.jmedchem.1c01532 |
0.339 |
|
| 2021 |
Bartoschik T, Zoephel A, Rumpel K, Ciulli A, Heffern C. MST and TRIC Technology to Reliably Study PROTAC Binary and Ternary Binding in Drug Development. Methods in Molecular Biology (Clifton, N.J.). 2365: 115-133. PMID 34432241 DOI: 10.1007/978-1-0716-1665-9_6 |
0.42 |
|
| 2021 |
Casement R, Bond A, Craigon C, Ciulli A. Mechanistic and Structural Features of PROTAC Ternary Complexes. Methods in Molecular Biology (Clifton, N.J.). 2365: 79-113. PMID 34432240 DOI: 10.1007/978-1-0716-1665-9_5 |
0.353 |
|
| 2021 |
Frost J, Rocha S, Ciulli A. Von Hippel-Lindau (VHL) small molecule inhibitor binding increases stability and intracellular levels of VHL protein. The Journal of Biological Chemistry. 100910. PMID 34174286 DOI: 10.1016/j.jbc.2021.100910 |
0.375 |
|
| 2021 |
Ishida T, Ciulli A. E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones. Slas Discovery : Advancing Life Sciences R & D. 26: 484-502. PMID 33143537 DOI: 10.1177/2472555220965528 |
0.388 |
|
| 2020 |
Makukhin N, Ciulli A. Recent advances in synthetic and medicinal chemistry of phosphotyrosine and phosphonate-based phosphotyrosine analogues. Rsc Medicinal Chemistry. 12: 8-23. PMID 34041480 DOI: 10.1039/d0md00272k |
0.347 |
|
| 2020 |
Ramachandran S, Ciulli A. Building ubiquitination machineries: E3 ligase multi-subunit assembly and substrate targeting by PROTACs and molecular glues. Current Opinion in Structural Biology. 67: 110-119. PMID 33271439 DOI: 10.1016/j.sbi.2020.10.009 |
0.376 |
|
| 2020 |
Klein VG, Townsend CE, Testa A, Zengerle M, Maniaci C, Hughes SJ, Chan KH, Ciulli A, Lokey RS. Understanding and Improving the Membrane Permeability of VH032-Based PROTACs. Acs Medicinal Chemistry Letters. 11: 1732-1738. PMID 32939229 DOI: 10.1021/Acsmedchemlett.0C00265 |
0.379 |
|
| 2020 |
Bond AG, Testa A, Ciulli A. Stereoselective synthesis of allele-specific BET inhibitors. Organic & Biomolecular Chemistry. PMID 32756710 DOI: 10.1039/D0Ob01165G |
0.402 |
|
| 2020 |
Cipriano A, Sbardella G, Ciulli A. Targeting epigenetic reader domains by chemical biology Current Opinion in Chemical Biology. 57: 82-94. PMID 32739717 DOI: 10.1016/J.Cbpa.2020.05.006 |
0.456 |
|
| 2020 |
Whitworth C, Ciulli A. New class of molecule targets proteins outside cells for degradation Nature. 584: 193-194. PMID 32728153 DOI: 10.1038/D41586-020-02211-W |
0.413 |
|
| 2020 |
Simpson LM, Macartney TJ, Nardin A, Fulcher LJ, Röth S, Testa A, Maniaci C, Ciulli A, Ganley IG, Sapkota GP. Inducible Degradation of Target Proteins through a Tractable Affinity-Directed Protein Missile System. Cell Chemical Biology. PMID 32668203 DOI: 10.1016/J.Chembiol.2020.06.013 |
0.416 |
|
| 2019 |
Ciulli A, Testa A, Hughes SJ, Lucas X, Wright JE. Structure-Based Design of a Macrocyclic PROTAC. Angewandte Chemie (International Ed. in English). PMID 31746102 DOI: 10.1002/Anie.201914396 |
0.511 |
|
| 2019 |
Tovell H, Testa A, Zhou H, Shpiro N, Crafter C, Ciulli A, Alessi DR. Design and characterization of SGK3-PROTAC1, an isoform specific SGK3 kinase PROTAC degrader. Acs Chemical Biology. PMID 31461270 DOI: 10.1021/Acschembio.9B00505 |
0.42 |
|
| 2019 |
Maniaci C, Ciulli A. Bifunctional chemical probes inducing protein-protein interactions. Current Opinion in Chemical Biology. 52: 145-156. PMID 31419624 DOI: 10.1016/J.Cbpa.2019.07.003 |
0.482 |
|
| 2019 |
Farnaby W, Koegl M, Roy MJ, Whitworth C, Diers E, Trainor N, Zollman D, Steurer S, Karolyi-Oezguer J, Riedmueller C, Gmaschitz T, Wachter J, Dank C, Galant M, Sharps B, ... ... Ciulli A, et al. Publisher Correction: BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design. Nature Chemical Biology. PMID 31267096 DOI: 10.1038/S41589-019-0329-Z |
0.384 |
|
| 2019 |
Ciulli A, Farnaby W. Protein degradation for drug discovery Drug Discovery Today: Technologies. 31: 1-3. PMID 31200853 DOI: 10.1016/J.Ddtec.2019.04.002 |
0.325 |
|
| 2019 |
Kung WW, Ramachandran S, Makukhin N, Bruno E, Ciulli A. Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase. Nature Communications. 10: 2534. PMID 31182716 DOI: 10.1038/s41467-019-10190-4 |
0.346 |
|
| 2019 |
Farnaby W, Koegl M, Roy MJ, Whitworth C, Diers E, Trainor N, Zollman D, Steurer S, Karolyi-Oezguer J, Riedmueller C, Gmaschitz T, Wachter J, Dank C, Galant M, Sharps B, ... ... Ciulli A, et al. BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design. Nature Chemical Biology. PMID 31178587 DOI: 10.1038/S41589-019-0294-6 |
0.444 |
|
| 2019 |
Testa A, Lucas X, Castro GV, Chan KH, Wright JE, Runcie AC, Gadd MS, Harrison WTA, Ko EJ, Fletcher D, Ciulli A. Correction to "3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation". Journal of the American Chemical Society. PMID 31017404 DOI: 10.1021/jacs.9b03833 |
0.792 |
|
| 2019 |
Tovell H, Testa A, Maniaci C, Zhou H, Prescott AR, Macartney T, Ciulli A, Alessi DR. Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader. Acs Chemical Biology. PMID 30978004 DOI: 10.1021/Acschembio.8B01016 |
0.443 |
|
| 2019 |
Girardini M, Maniaci C, Hughes SJ, Testa A, Ciulli A. Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs. Bioorganic & Medicinal Chemistry. PMID 30826187 DOI: 10.1016/J.Bmc.2019.02.048 |
0.433 |
|
| 2019 |
Popow J, Arnhof H, Bader G, Berger H, Ciulli A, Covini D, Dank C, Gmaschitz T, Greb P, Karolyi-Oezguer J, Koegl M, McConnell D, Pearson M, Rieger M, Rinnenthal J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras (PROTACs) to Probe Focal Adhesion Kinase Scaffolding Functions. Journal of Medicinal Chemistry. PMID 30739444 DOI: 10.1021/Acs.Jmedchem.8B01826 |
0.34 |
|
| 2019 |
Roy M, Winkler S, Hughes SJ, Whitworth C, Galant M, Farnaby W, Rumpel K, Ciulli A. SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate. Acs Chemical Biology. PMID 30721025 DOI: 10.1021/Acschembio.9B00092 |
0.453 |
|
| 2019 |
Castro GVd, Ciulli A. Spy vs. spy: selecting the best reporter for 19F NMR competition experiments Chemical Communications. 55: 1482-1485. PMID 30644956 DOI: 10.1039/C8Cc09790A |
0.362 |
|
| 2019 |
Ciulli A. Targeted Protein Degradation with Small Molecules: How PROTACs Work Proceedings. 22: 115. DOI: 10.3390/proceedings2019022115 |
0.432 |
|
| 2019 |
Kung W, Ramachandran S, Makukhin N, Bruno E, Ciulli A. Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase. Nature Communications. 10: 2534-2534. DOI: 10.2210/Pdb6I5N/Pdb |
0.437 |
|
| 2019 |
Zoppi V, Hughes SJ, Maniaci C, Testa A, Gmaschitz T, Wieshofer C, Koegl M, Riching KM, Daniels DL, Spallarossa A, Ciulli A. Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7 Journal of Medicinal Chemistry. 62: 699-726. DOI: 10.2210/Pdb6Hm0/Pdb |
0.485 |
|
| 2019 |
Hassell-Hart S, Runcie A, Krojer T, Doyle J, Lineham E, Ocasio CA, Neto BAD, Fedorov O, Marsh G, Maple H, Felix R, Banks R, Ciulli A, Picaud S, Filippakopoulos P, et al. Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor Organometallics. 39: 408-416. DOI: 10.1021/Acs.Organomet.9B00750 |
0.453 |
|
| 2018 |
Zoppi V, Hughes SJ, Maniaci C, Testa A, Gmaschitz T, Wieshofer C, Koegl M, Riching K, Daniels DL, Spallarossa A, Ciulli A. Iterative design and optimization of initially inactive Proteolysis Targeting Chimeras (PROTACs) identify VZ185 as a potent, fast and selective von Hippel-Lindau (VHL)-based dual degrader probe of BRD9 and BRD7. Journal of Medicinal Chemistry. PMID 30540463 DOI: 10.1021/acs.jmedchem.8b01413 |
0.402 |
|
| 2018 |
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. Journal of Medicinal Chemistry. PMID 30040896 DOI: 10.1021/Acs.Jmedchem.8B00842 |
0.476 |
|
| 2018 |
Testa A, Lucas X, Castro G, Chan KH, Wright J, Runcie A, Gadd M, Harrison WTA, Ko EJ, Fletcher D, Ciulli A. 3-Fluoro-4-hydroxyprolines: Synthesis, conformational analysis and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation. Journal of the American Chemical Society. PMID 29949369 DOI: 10.1021/Jacs.8B05807 |
0.802 |
|
| 2018 |
Runcie AC, Zengerle M, Chan KH, Testa A, van Beurden L, Baud MGJ, Epemolu O, Ellis LCJ, Read KD, Coulthard V, Brien A, Ciulli A. Optimization of a "bump-and-hole" approach to allele-selective BET bromodomain inhibition. Chemical Science. 9: 2452-2468. PMID 29732121 DOI: 10.1039/C7Sc02536J |
0.778 |
|
| 2018 |
Soares P, Lucas X, Ciulli A. Thioamide substitution to probe the hydroxyproline recognition of VHL ligands. Bioorganic & Medicinal Chemistry. PMID 29650462 DOI: 10.1016/J.Bmc.2018.03.034 |
0.419 |
|
| 2018 |
Amato A, Lucas X, Bortoluzzi A, Wright D, Ciulli A. Targeting ligandable pockets on PHD zinc finger domains by a fragment-based approach. Acs Chemical Biology. PMID 29529862 DOI: 10.1021/Acschembio.7B01093 |
0.494 |
|
| 2018 |
Tarantelli C, Ekeh H, Moscatello C, Gaudio E, Testa A, Zucca E, Stathis A, Ciulli A, Bertoni F. Abstract A179: The BRD4 degrader MZ1 exhibits potent antitumoral activity in diffuse large B cell lymphoma of the activated B cell-like type Molecular Cancer Therapeutics. 17. DOI: 10.1158/1535-7163.Targ-17-A179 |
0.337 |
|
| 2017 |
Khan R, Marsh G, Felix R, Kemmitt PD, Baud MGJ, Ciulli A, Spencer J. Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand. Acs Omega. 2: 4328-4332. PMID 31457724 DOI: 10.1021/acsomega.7b00780 |
0.702 |
|
| 2017 |
Hughes SJ, Ciulli A. Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders. Essays in Biochemistry. 61: 505-516. PMID 29118097 DOI: 10.1042/Ebc20170041 |
0.524 |
|
| 2017 |
Maniaci C, Hughes SJ, Testa A, Chen W, Lamont DJ, Rocha S, Alessi DR, Romeo R, Ciulli A. Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation. Nature Communications. 8: 830. PMID 29018234 DOI: 10.1038/S41467-017-00954-1 |
0.49 |
|
| 2017 |
Morreale FE, Testa A, Chaugule VK, Bortoluzzi A, Ciulli A, Walden H. Mind the metal: a fragment library-derived zinc impurity binds the E2 ubiquitin-conjugating enzyme Ube2T and induces structural rearrangements. Journal of Medicinal Chemistry. PMID 28933844 DOI: 10.1021/Acs.Jmedchem.7B01071 |
0.497 |
|
| 2017 |
Soares P, Gadd MS, Frost J, Galdeano C, Ellis LCJ, Epemolu O, Rocha S, Read KD, Ciulli A. Group-based optimization of potent and cell-active inhibitors of the von Hippel-Lindau (VHL) E3 ubiquitin ligase: structure-activity relationships leading to the chemical probe (2S,4R)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298). Journal of Medicinal Chemistry. PMID 28853884 DOI: 10.1021/Acs.Jmedchem.7B00675 |
0.828 |
|
| 2017 |
Cardote TAF, Ciulli A. Structure-Guided Design of Peptides as Tools to Probe the Protein-Protein Interaction between Cullin-2 and Elongin BC Substrate Adaptor in Cullin RING E3 Ubiquitin Ligases. Chemmedchem. 12: 1491-1496. PMID 28776949 DOI: 10.1002/Cmdc.201700359 |
0.516 |
|
| 2017 |
Chan KH, Zengerle M, Testa A, Ciulli A. Impact of target warhead and linkage vector on inducing protein degradation: comparison of Bromodomain and Extra-Terminal (BET) degraders derived from triazolodiazepine (JQ1) and tetrahydroquinoline (I-BET726) BET inhibitor scaffolds. Journal of Medicinal Chemistry. PMID 28595007 DOI: 10.1021/Acs.Jmedchem.6B01912 |
0.518 |
|
| 2017 |
Cardote TAF, Gadd MS, Ciulli A. Crystal Structure of the Cul2-Rbx1-EloBC-VHL Ubiquitin Ligase Complex Structure. 25: 901-911. PMID 28591624 DOI: 10.1016/J.Str.2017.04.009 |
0.833 |
|
| 2017 |
Fernandez-Alonso R, Davidson L, Hukelmann J, Zengerle M, Prescott AR, Lamond A, Ciulli A, Sapkota GP, Findlay GM. Brd4-Brd2 isoform switching coordinates pluripotent exit and Smad2-dependent lineage specification. Embo Reports. PMID 28588073 DOI: 10.15252/Embr.201643534 |
0.32 |
|
| 2017 |
Morreale FE, Bortoluzzi A, Chaugule VK, Arkinson C, Walden H, Ciulli A. Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening Journal of Medicinal Chemistry. 60: 4093-4098. PMID 28437106 DOI: 10.1021/Acs.Jmedchem.7B00147 |
0.485 |
|
| 2017 |
Ryan A, Polycarpou E, Lack NA, Evangelopoulos D, Sieg C, Halman A, Bhakta S, Eleftheriadou O, McHugh TD, Keany S, Lowe ED, Ballet R, Abuhammad A, Jacobs WR, Ciulli A, et al. Investigation of the mycobacterial enzyme HsaD as a potential novel target for anti-tubercular agents using a fragment-based drug design approach. British Journal of Pharmacology. PMID 28380256 DOI: 10.1111/Bph.13810 |
0.336 |
|
| 2017 |
Macaulay KM, Heath GA, Ciulli A, Murphy AM, Abell C, Carr JP, Smith AG. The biochemical properties of the two Arabidopsis thaliana isochorismate synthases. The Biochemical Journal. PMID 28356402 DOI: 10.1042/Bcj20161069 |
0.667 |
|
| 2017 |
Bortoluzzi A, Amato A, Lucas X, Blank M, Ciulli A. Structural Basis of Molecular Recognition of Helical Histone H3 Tail by PHD Finger Domains. The Biochemical Journal. PMID 28341809 DOI: 10.1042/Bcj20161053 |
0.398 |
|
| 2017 |
Gadd MS, Testa A, Lucas X, Chan KH, Chen W, Lamont DJ, Zengerle M, Ciulli A. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nature Chemical Biology. PMID 28288108 DOI: 10.1038/Nchembio.2329 |
0.832 |
|
| 2017 |
De Schutter JW, Morrison JP, Morrison MJ, Ciulli A, Imperiali B. Targeting Bacillosamine Biosynthesis in Bacterial Pathogens: Development of Inhibitors to a Bacterial Amino-Sugar Acetyltransferase from Campylobacter jejuni. Journal of Medicinal Chemistry. PMID 28182413 DOI: 10.1021/Acs.Jmedchem.6B01869 |
0.453 |
|
| 2017 |
Lucas X, Ciulli A. Recognition of substrate degrons by E3 ubiquitin ligases and modulation by small-molecule mimicry strategies. Current Opinion in Structural Biology. 44: 101-110. PMID 28130986 DOI: 10.1016/J.Sbi.2016.12.015 |
0.483 |
|
| 2016 |
Frost J, Galdeano C, Soares P, Gadd MS, Grzes KM, Ellis L, Epemolu O, Shimamura S, Bantscheff M, Grandi P, Read KD, Cantrell DA, Rocha S, Ciulli A. Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nature Communications. 7: 13312. PMID 27811928 DOI: 10.1038/Ncomms13312 |
0.801 |
|
| 2016 |
Ciulli A. Target validation: Switching domains Nature Chemical Biology. 12: 659-660. PMID 27538023 DOI: 10.1038/Nchembio.2154 |
0.414 |
|
| 2016 |
Runcie AC, Chan KH, Zengerle M, Ciulli A. Chemical genetics approaches for selective intervention in epigenetics. Current Opinion in Chemical Biology. 33: 186-194. PMID 27423045 DOI: 10.1016/J.Cbpa.2016.06.031 |
0.387 |
|
| 2016 |
Galdeano C, Ciulli A. Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology. Future Medicinal Chemistry. PMID 27193077 DOI: 10.4155/Fmc-2016-0059 |
0.782 |
|
| 2016 |
Cardote TAF, Ciulli A. Cyclic and Macrocyclic Peptides as Chemical Tools To Recognise Protein Surfaces and Probe Protein-Protein Interactions. Chemmedchem. 11: 787-794. PMID 26563831 DOI: 10.1002/Cmdc.201500450 |
0.414 |
|
| 2016 |
Baud MGJ, Lin-Shiao E, Zengerle M, Tallant C, Ciulli A. New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition. Journal of Medicinal Chemistry. 59: 1492-1500. PMID 26367539 DOI: 10.1021/Acs.Jmedchem.5B01135 |
0.75 |
|
| 2015 |
Dias DM, Furtado J, Wasielewski E, Cruz R, Costello B, Cole L, Faria TQ, Baaske P, Brito RM, Ciulli A, Simões I, MacEdo-Ribeiro S, Faro C, Geraldes CF, Castanheira P. Biophysical characterization of laforin-carbohydrate interaction. The Biochemical Journal. PMID 26578817 DOI: 10.1042/Bj20141555 |
0.372 |
|
| 2015 |
Hung AW, Silvestre HL, Wen S, George GP, Boland J, Blundell TL, Ciulli A, Abell C. Optimization of Inhibitors of Mycobacterium tuberculosis Pantothenate Synthetase Based on Group Efficiency Analysis. Chemmedchem. PMID 26486566 DOI: 10.1002/Cmdc.201500414 |
0.767 |
|
| 2015 |
Gadd MS, Bulatov E, Ciulli A. Serendipitous SAD Solution for DMSO-Soaked SOCS2-ElonginC-ElonginB Crystals Using Covalently Incorporated Dimethylarsenic: Insights into Substrate Receptor Conformational Flexibility in Cullin RING Ligases. Plos One. 10: e0131218. PMID 26121586 DOI: 10.1371/Journal.Pone.0131218 |
0.803 |
|
| 2015 |
Zengerle M, Chan KH, Ciulli A. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. Acs Chemical Biology. PMID 26035625 DOI: 10.1021/Acschembio.5B00216 |
0.471 |
|
| 2015 |
Bulatov E, Ciulli A. Targeting Cullin-RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation. Biochemical Journal. 467: 365-386. PMID 25886174 DOI: 10.1042/Bj20141450 |
0.783 |
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| 2015 |
Tallant C, Valentini E, Fedorov O, Overvoorde L, Ferguson FM, Filippakopoulos P, Svergun DI, Knapp S, Ciulli A. Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC. Structure (London, England : 1993). 23: 80-92. PMID 25533489 DOI: 10.1016/J.Str.2014.10.017 |
0.781 |
|
| 2015 |
Bulatov E, Martin EM, Chatterjee S, Knebel A, Shimamura S, Konijnenberg A, Johnson C, Zinn N, Grandi P, Sobott F, Ciulli A. Biophysical studies on interactions and assembly of full-size E3 ubiquitin ligase: suppressor of cytokine signaling 2 (SOCS2)-elongin BC-cullin 5-ring box protein 2 (RBX2). The Journal of Biological Chemistry. 290: 4178-91. PMID 25505247 DOI: 10.1074/Jbc.M114.616664 |
0.744 |
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| 2014 |
Baud MG, Lin-Shiao E, Cardote T, Tallant C, Pschibul A, Chan KH, Zengerle M, Garcia JR, Kwan TT, Ferguson FM, Ciulli A. Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes. Science (New York, N.Y.). 346: 638-41. PMID 25323695 DOI: 10.1126/Science.1249830 |
0.814 |
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| 2014 |
Ferguson FM, Dias DM, Rodrigues JP, Wienk H, Boelens R, Bonvin AM, Abell C, Ciulli A. Binding hotspots of BAZ2B bromodomain: Histone interaction revealed by solution NMR driven docking. Biochemistry. 53: 6706-16. PMID 25266743 DOI: 10.1021/Bi500909D |
0.804 |
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| 2014 |
Dias DM, Ciulli A. NMR approaches in structure-based lead discovery: recent developments and new frontiers for targeting multi-protein complexes. Progress in Biophysics & Molecular Biology. 116: 101-112. PMID 25175337 DOI: 10.1016/J.Pbiomolbio.2014.08.012 |
0.483 |
|
| 2014 |
Galdeano C, Gadd MS, Soares P, Scaffidi S, Van Molle I, Birced I, Hewitt S, Dias DM, Ciulli A. 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. 57: 8657-63. PMID 25166285 DOI: 10.1021/Jm5011258 |
0.827 |
|
| 2014 |
Dias DM, Molle IV, Baud MGJ, Galdeano C, Geraldes CFGC, Ciulli A. Is NMR Fragment Screening Fine-Tuned to Assess Druggability of Protein-Protein Interactions? Acs Medicinal Chemistry Letters. 5: 23-28. PMID 24436777 DOI: 10.1021/Ml400296C |
0.818 |
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| 2013 |
Ferguson FM, Fedorov O, Chaikuad A, Philpott M, Muniz JR, Felletar I, von Delft F, Heightman T, Knapp S, Abell C, Ciulli A. Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain. Journal of Medicinal Chemistry. 56: 10183-7. PMID 24304323 DOI: 10.1021/Jm401582C |
0.807 |
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| 2013 |
Silvestre HL, Blundell TL, Abell C, Ciulli A. Integrated biophysical approach to fragment screening and validation for fragment-based lead discovery. Proceedings of the National Academy of Sciences of the United States of America. 110: 12984-9. PMID 23872845 DOI: 10.1073/Pnas.1304045110 |
0.757 |
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| 2013 |
Thomas JC, Matak-Vinkovic D, Van Molle I, Ciulli A. Multimeric complexes among ankyrin-repeat and SOCS-box protein 9 (ASB9), ElonginBC, and cullin 5: Insights into the structure and assembly of ECS-type Cullin-RING E3 ubiquitin ligases Biochemistry. 52: 5236-5246. PMID 23837592 DOI: 10.1021/Bi400758H |
0.438 |
|
| 2013 |
Ciulli A. Biophysical screening for the discovery of small-molecule ligands. Methods of Molecular Biology. 1008: 357-388. PMID 23729259 DOI: 10.1007/978-1-62703-398-5_13 |
0.483 |
|
| 2013 |
Ryan A, Eleftheriadou O, Halman A, Sieg C, Keany S, Ciulli A, Abell C, Lowe ED, Sim E. Fragment-based approaches for anti-tuberculosis drug discovery Acta Crystallographica Section a Foundations of Crystallography. 69: s349-s349. DOI: 10.1107/S0108767313096992 |
0.681 |
|
| 2012 |
Van Molle I, Thomann A, Buckley DL, So EC, Lang S, Crews CM, Ciulli A. Dissecting fragment-based lead discovery at the von Hippel-Lindau protein:hypoxia inducible factor 1α protein-protein interface. Chemistry & Biology. 19: 1300-12. PMID 23102223 DOI: 10.1016/J.Chembiol.2012.08.015 |
0.763 |
|
| 2012 |
Buckley DL, Gustafson JL, Van Molle I, Roth AG, Tae HS, Gareiss PC, Jorgensen WL, Ciulli A, Crews CM. Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α. Angewandte Chemie (International Ed. in English). 51: 11463-7. PMID 23065727 DOI: 10.1002/Anie.201206231 |
0.762 |
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| 2012 |
Hudson SA, McLean KJ, Surade S, Yang YQ, Leys D, Ciulli A, Munro AW, Abell C. Application of fragment screening and merging to the discovery of inhibitors of the Mycobacterium tuberculosis cytochrome P450 CYP121. Angewandte Chemie (International Ed. in English). 51: 9311-6. PMID 22890978 DOI: 10.1002/Anie.201202544 |
0.697 |
|
| 2012 |
Buckley DL, Van Molle I, Gareiss PC, Tae HS, Michel J, Noblin DJ, Jorgensen WL, Ciulli A, Crews CM. Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction. Journal of the American Chemical Society. 134: 4465-8. PMID 22369643 DOI: 10.1021/Ja209924V |
0.826 |
|
| 2012 |
Buckley DL, Gustafson JL, Van Molle I, Roth AG, Tae HS, Gareiss PC, Jorgensen WL, Ciulli A, Crews CM. Niedermolekulare Inhibitoren der Wechselwirkung zwischen der E3-Ligase VHL und HIF1α Angewandte Chemie. 124: 11630-11634. DOI: 10.1002/Ange.201206231 |
0.668 |
|
| 2012 |
Śledź P, Abell C, Ciulli A. Ligand-Observed NMR in Fragment-Based Approaches Nmr of Biomolecules: Towards Mechanistic Systems Biology. 264-280. DOI: 10.1002/9783527644506.ch15 |
0.67 |
|
| 2011 |
Philpott M, Yang J, Tumber T, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Keates T, Felletar I, Ciulli A, Knapp S, Heightman TD. Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery. Molecular Biosystems. 7: 2899-908. PMID 21804994 DOI: 10.1039/C1Mb05099K |
0.404 |
|
| 2011 |
Dias MV, Snee WC, Bromfield KM, Payne RJ, Palaninathan SK, Ciulli A, Howard NI, Abell C, Sacchettini JC, Blundell TL. Structural investigation of inhibitor designs targeting 3-dehydroquinate dehydratase from the shikimate pathway of Mycobacterium tuberculosis. The Biochemical Journal. 436: 729-39. PMID 21410435 DOI: 10.1042/Bj20110002 |
0.808 |
|
| 2010 |
Sledz P, Silvestre HL, Hung AW, Ciulli A, Blundell TL, Abell C. Optimization of the interligand Overhauser effect for fragment linking: application to inhibitor discovery against Mycobacterium tuberculosis pantothenate synthetase. Journal of the American Chemical Society. 132: 4544-5. PMID 20232910 DOI: 10.1021/Ja100595U |
0.8 |
|
| 2009 |
Scott DE, Dawes GJ, Ando M, Abell C, Ciulli A. A fragment-based approach to probing adenosine recognition sites by using dynamic combinatorial chemistry. Chembiochem : a European Journal of Chemical Biology. 10: 2772-9. PMID 19827080 DOI: 10.1002/Cbic.200900537 |
0.767 |
|
| 2009 |
Hung AW, Silvestre HL, Wen S, Ciulli A, Blundell TL, Abell C. Application of fragment growing and fragment linking to the discovery of inhibitors of Mycobacterium tuberculosis pantothenate synthetase. Angewandte Chemie (International Ed. in English). 48: 8452-6. PMID 19780086 DOI: 10.1002/Anie.200903821 |
0.752 |
|
| 2009 |
Scott DE, Dawes GJ, Ando M, Abell C, Ciulli A. Inside Cover: A Fragment-Based Approach to Probing Adenosine Recognition Sites by Using Dynamic Combinatorial Chemistry (ChemBioChem 17/2009) Chembiochem. 10: 2678-2678. DOI: 10.1002/Cbic.200990077 |
0.679 |
|
| 2008 |
Ciulli A, Scott DE, Ando M, Reyes F, Saldanha SA, Tuck KL, Chirgadze DY, Blundell TL, Abell C. Inhibition of Mycobacterium tuberculosis pantothenate synthetase by analogues of the reaction intermediate. Chembiochem : a European Journal of Chemical Biology. 9: 2606-11. PMID 18821554 DOI: 10.1002/Cbic.200800437 |
0.802 |
|
| 2007 |
Ciulli A, Abell C. Fragment-based approaches to enzyme inhibition. Current Opinion in Biotechnology. 18: 489-96. PMID 17959370 DOI: 10.1016/J.Copbio.2007.09.003 |
0.733 |
|
| 2007 |
Scott DE, Ciulli A, Abell C. Coenzyme biosynthesis: enzyme mechanism, structure and inhibition. Natural Product Reports. 24: 1009-26. PMID 17898895 DOI: 10.1039/B703108B |
0.718 |
|
| 2007 |
Kerbarh O, Ciulli A, Chirgadze DY, Blundell TL, Abell C. Nucleophile selectivity of chorismate-utilizing enzymes. Chembiochem : a European Journal of Chemical Biology. 8: 622-4. PMID 17335098 DOI: 10.1002/Cbic.200700019 |
0.745 |
|
| 2007 |
Ciulli A, Lobley CM, Tuck KL, Smith AG, Blundell TL, Abell C. pH-tuneable binding of 2'-phospho-ADP-ribose to ketopantoate reductase: a structural and calorimetric study. Acta Crystallographica. Section D, Biological Crystallography. 63: 171-8. PMID 17242510 DOI: 10.1107/S0907444906044465 |
0.806 |
|
| 2007 |
Ciulli A, Chirgadze DY, Smith AG, Blundell TL, Abell C. Crystal structure of Escherichia coli ketopantoate reductase in a ternary complex with NADP+ and pantoate bound: Substrate recognition, conformational change, and cooperativity Journal of Biological Chemistry. 282: 8487-8497. PMID 17229734 DOI: 10.1074/Jbc.M611171200 |
0.772 |
|
| 2006 |
Ciulli A, Williams G, Smith AG, Blundell TL, Abell C. Probing hot spots at protein-ligand binding sites: A fragment-based approach using biophysical methods Journal of Medicinal Chemistry. 49: 4992-5000. PMID 16884311 DOI: 10.1021/Jm060490R |
0.771 |
|
| 2005 |
Ciulli A, Abell C. Biophysical tools to monitor enzyme-ligand interactions of enzymes involved in vitamin biosynthesis. Biochemical Society Transactions. 33: 767-71. PMID 16042595 DOI: 10.1042/Bst0330767 |
0.721 |
|
| 2005 |
Kerbarh O, Ciulli A, Howard NI, Abell C. Salicylate biosynthesis: overexpression, purification, and characterization of Irp9, a bifunctional salicylate synthase from Yersinia enterocolitica. Journal of Bacteriology. 187: 5061-6. PMID 16030197 DOI: 10.1128/Jb.187.15.5061-5066.2005 |
0.705 |
|
| 2005 |
Lobley CM, Ciulli A, Whitney HM, Williams G, Smith AG, Abell C, Blundell TL. The crystal structure of Escherichia coli ketopantoate reductase with NADP+ bound. Biochemistry. 44: 8930-9. PMID 15966718 DOI: 10.1021/Bi0502036 |
0.772 |
|
| 2003 |
Banci L, Bertini I, Ciulli A, Fragai M, Luchinat C, Terni B. Expression and high yield production of the catalytic domain of matrix metalloproteinase 12 and of an active mutant with increased solubility Journal of Molecular Catalysis a-Chemical. 204: 401-408. DOI: 10.1016/S1381-1169(03)00493-X |
0.46 |
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