Research output per year
Research output per year
- 26 results
Search results
-
2022
Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
Diehl, C. J. & Ciulli, A. (Lead / Corresponding author), 19 Aug 2022, In: Chemical Society Reviews. 51, 19, p. 8216-8257 42 p.Research output: Contribution to journal › Review article › peer-review
Open AccessFile99 Citations (Scopus)276 Downloads (Pure) -
2020
Targeting epigenetic reader domains by chemical biology
Cipriano, A., Sbardella, G. (Lead / Corresponding author) & Ciulli, A. (Lead / Corresponding author), Aug 2020, In: Current Opinion in Chemical Biology. 57, p. 82-94 13 p.Research output: Contribution to journal › Review article › peer-review
22 Citations (Scopus) -
2018
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)
Soares, P., Gadd, M., Frost, J., Galdeano, C., Ellis, L., Epemolu, R., Rocha, S., Read, K. & Ciulli, A. (Lead / Corresponding author), 25 Jan 2018, In: Journal of Medicinal Chemistry. 61, p. 599-618 19 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile119 Citations (Scopus)356 Downloads (Pure) -
Optimization of a “Bump-and-Hole” Approach to Allele-Selective BET Bromodomain Inhibition
Runcie, A., Zengerle, M., Chan, K. H., Testa, A., Van Beurden, L., Baud, M., Epemolu, R., Ellis, L., Read, K., Coulthard, V., Brien, A. & Ciulli, A. (Lead / Corresponding author), 7 Mar 2018, In: Chemical Science. 9, 9, p. 2452-2468 17 p., 2452.Research output: Contribution to journal › Article › peer-review
Open AccessFile35 Citations (Scopus)252 Downloads (Pure) -
2017
Allosteric targeting of the Fanconi anemia ubiquitin-conjugating enzyme Ube2T by fragment screening
Morreale, F., Bortoluzzi, A., Chaugule, V., Arkinson, C., Walden, H. & Ciulli, A. (Lead / Corresponding author), 11 May 2017, In: Journal of Medicinal Chemistry. 60, 9, p. 4093-4098 6 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile27 Citations (Scopus)231 Downloads (Pure) -
Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand
Khan, R., Marsh, G., Felix, R., Kemmitt, P. D., Baud, M. G. J., Ciulli, A. & Spencer, J. (Lead / Corresponding author), Aug 2017, In: ACS Omega. 2, 8, p. 4328-4332 5 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile3 Citations (Scopus)179 Downloads (Pure) -
Mind the metal: a fragment library-derived zinc impurity binds the E2 ubiquitin-conjugating enzyme Ube2T and induces structural rearrangements
Morreale, F., Testa, A., Chaugule, V., Bortoluzzi, A., Ciulli, A. & Walden, H. (Lead / Corresponding author), 12 Oct 2017, In: Journal of Medicinal Chemistry. 60, 19, p. 8183-8191 9 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile20 Citations (Scopus)318 Downloads (Pure) -
Structural Basis of Molecular Recognition of Helical Histone H3 Tail by PHD Finger Domains
Bortoluzzi, A., Amato, A., Lucas, X., Blank, M. & Ciulli, A. (Lead / Corresponding author), 4 May 2017, In: Biochemical Journal. 474, 10, p. 1633-1651 19 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile26 Citations (Scopus)270 Downloads (Pure) -
2016
Chemical genetics approaches for selective intervention in epigenetics
Runcie, A. C., Chan, K. H., Zengerle, M. & Ciulli, A. (Lead / Corresponding author), Aug 2016, In: Current Opinion in Chemical Biology. 33, p. 186-194 9 p.Research output: Contribution to journal › Review article › peer-review
Open AccessFile24 Citations (Scopus)275 Downloads (Pure) -
Cyclic and macrocyclic peptides as chemical tools to recognise protein surfaces and probe protein-protein interactions
Cardote, T. A. F. & Ciulli, A. (Lead / Corresponding author), 19 Apr 2016, In: ChemMedChem. 11, 8, p. 787-794 8 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile147 Citations (Scopus)244 Downloads (Pure) -
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
Baud, M. G. J., Lin-Shiao, E., Zengerle, M., Tallant, C. & Ciulli, A. (Lead / Corresponding author), 25 Feb 2016, In: Journal of Medicinal Chemistry. 59, 4, p. 1492-1500 9 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile46 Citations (Scopus)533 Downloads (Pure) -
Potent and selective chemical probe of hypoxic signaling downstream of HIF-α hydroxylation via VHL inhibition
Frost, J., Galdeano, C., Soares, P., Gadd, M. S., Grzes, K. M., Ellis, L., Epemolu, O., Shimamura, S., Bantscheff, M., Grandi, P., Read, K. D., Cantrell, D. A., Rocha, S. & Ciulli, A. (Lead / Corresponding author), 4 Nov 2016, In: Nature Communications. 7, p. 1-12 12 p., 13312.Research output: Contribution to journal › Article › peer-review
Open AccessFile172 Citations (Scopus)328 Downloads (Pure) -
Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology
Galdeano, C. & Ciulli, A. (Lead / Corresponding author), Sept 2016, In: Future Medicinal Chemistry. 8, 13, p. 1655-1680 26 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile50 Citations (Scopus)718 Downloads (Pure) -
Target validation: switching domains
Ciulli, A. (Lead / Corresponding author), Sept 2016, In: Nature Chemical Biology. 12, 9, p. 659-660 2 p.Research output: Contribution to journal › Short survey › peer-review
Open AccessFile293 Downloads (Pure) -
2015
Biophysical studies on interactions and assembly of full-size E3 ubiquitin ligase: suppressor of cytokine signaling 2 (SOCS2):ElonginBC:Cullin5:RING-box protein 2 (Rbx2)
Bulatov, E., Martin, E. M., Chatterjee, S., Knebel, A., Shimamura, S., Konijnenberg, A., Johnson, C., Zinn, N., Grandi, P., Sobott, F. & Ciulli, A. (Lead / Corresponding author), 13 Feb 2015, In: Journal of Biological Chemistry. 290, 7, p. 4178-4191 14 p.Research output: Contribution to journal › Article
Open Access26 Citations (Scopus) -
Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC
Tallant, C., Valentini, E., Fedorov, O., Overvoorde, L., Ferguson, F. M., Filippakopoulos, P., Svergun, D. I., Knapp, S. & Ciulli, A. (Lead / Corresponding author), 6 Jan 2015, In: Structure. 23, 1, p. 80-92 13 p.Research output: Contribution to journal › Article › peer-review
59 Citations (Scopus) -
Selective small molecule induced degradation of the BET bromodomain protein BRD4
Zengerle, M., Chan, K.-H. & Ciulli, A. (Lead / Corresponding author), 21 Aug 2015, In: ACS Chemical Biology. 10, 8, p. 1770-1777 8 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile783 Citations (Scopus)399 Downloads (Pure) -
Serendipitous SAD solution for DMSO-soaked SOCS2-ElonginC-ElonginB crystals using covalently incorporated Dimethylarsenic: insights into substrate receptor conformational flexibility in Cullin RING Llgases
Gadd, M. S., Bulatov, E. & Ciulli, A. (Lead / Corresponding author), 29 Jun 2015, In: PLoS ONE. 10, 6, 14 p., e0131218.Research output: Contribution to journal › Article › peer-review
19 Citations (Scopus) -
Targeting Cullin-RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation
Bulatov, E. & Ciulli, A. (Lead / Corresponding author), 1 May 2015, In: Biochemical Journal. 467, 3, p. 365-386 22 p.Research output: Contribution to journal › Article › peer-review
188 Citations (Scopus) -
2014
A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes
Baud, M. G. J., Lin-Shiao, E., Cardote, T., Tallant, C., Pschibul, A., Chan, K.-H., Zengerle, M., Garcia, J. R., Kwan, T.T.-L., Ferguson, F. M. & Ciulli, A. (Lead / Corresponding author), 31 Oct 2014, In: Science. 346, 6209, p. 638-641 4 p.Research output: Contribution to journal › Article › peer-review
123 Citations (Scopus) -
Binding hotspots of BAZ2B bromodomain: histone interaction revealed by solution NMR driven docking
Ferguson, F. M., Dias, D. M., Rodrigues, J. P. G. L. M., Wienk, H., Boelens, R., Bonvin, A. M. J. J., Abell, C. & Ciulli, A. (Lead / Corresponding author), 28 Oct 2014, In: Biochemistry. 53, 42, p. 6706-6716 11 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile21 Citations (Scopus)276 Downloads (Pure) -
Is NMR fragment screening fine-tuned to assess druggability of protein-protein interactions?
Dias, D. M., Van Molle, I., Baud, M. G. J., Galdeano, C., Geraldes, C. F. G. C. & Ciulli, A., 9 Jan 2014, In: ACS Medicinal Chemistry Letters. 5, 1, p. 23-28 6 p.Research output: Contribution to journal › Letter › peer-review
48 Citations (Scopus) -
NMR approaches in structure-based lead discovery: recent developments and new frontiers for targeting multi-protein complexes
Dias, D. M. & Ciulli, A. (Lead / Corresponding author), Nov 2014, In: Progress in Biophysics and Molecular Biology. 116, 2-3, p. 101-112 12 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile54 Citations (Scopus)212 Downloads (Pure) -
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
Galdeano , C., Gadd, M. S., Soares, P., Scaffidi, S., Van Molle, I., Birced, I., Hewitt, S., Dias, D. M. & Ciulli, A. (Lead / Corresponding author), 23 Oct 2014, In: Journal of Medicinal Chemistry. 57, 20, p. 8657-8663 7 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile310 Citations (Scopus)335 Downloads (Pure) -
2013
Biophysical screening for the discovery of small-molecule ligands
Ciulli, A., 2013, Protein-ligand interactions: methods and applications. Williams, M. A. & Daviter, T. (eds.). Humana Press, p. 357-388 32 p. (Methods in Molecular Biology; vol. 1008).Research output: Chapter in Book/Report/Conference proceeding › Chapter (peer-reviewed)
67 Citations (Scopus) -
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
Thomas, J. C., Matak-Vinkovic, D., Van Molle, I. & Ciulli, A., 25 Jul 2013, In: Biochemistry. 52, 31, p. 5236-5246 11 p.Research output: Contribution to journal › Article › peer-review
26 Citations (Scopus)