Research output per year
Research output per year
- 22 results
Search results
-
2022
Discovery of benzo[d]imidazole-6-sulfonamides as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain
Cipriano, A., Milite, C., Feoli, A., Viviano, M., Pepe, G., Campiglia, P., Sarno, G., Picaud, S., Imaide, S., Makukhin, N., Filippakopoulos, P., Ciulli, A., Castellano, S. (Lead / Corresponding author) & Sbardella, G., 19 Oct 2022, In: ChemMedChem. 17, 20, 14 p., e202200343.Research output: Contribution to journal › Article › peer-review
Open AccessFile8 Citations (Scopus)132 Downloads (Pure) -
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) -
2021
Targeting non-canonical activation of GLI1 by the SOX2-BRD4 transcriptional complex improves the efficacy of HEDGEHOG pathway inhibition in melanoma
Pietrobono, S. (Lead / Corresponding author), Gaudio, E., Gagliardi, S., Zitani, M., Carrassa, L., Migliorini, F., Petricci, E., Manetti, F., Makukhin, N., Bond, A. G., Paradise, B. D., Ciulli, A., Fernandez-Zapico, M. E., Bertoni, F. & Stecca, B. (Lead / Corresponding author), 3 Jun 2021, In: Oncogene. 40, p. 3799-3814 16 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile34 Citations (Scopus)116 Downloads (Pure) -
2020
Stereoselective synthesis of allele-specific BET inhibitors
Bond, A., Testa, A. & Ciulli, A. (Lead / Corresponding author), 14 Oct 2020, In: Organic and Biomolecular Chemistry. 18, 38, p. 7533-7539 7 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile6 Citations (Scopus)103 Downloads (Pure) -
Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor
Hassell-Hart, S., Runcie, A., Krojer, T., Doyle, J., Lineham, E., Ocasio, C. A., Neto, B. A. D., Fedorov, O., Marsh, G., Maple, H., Felix, R., Banks, R., Ciulli, A., Picaud, S., Filippakopoulos, P., Von Delft, F., Brennan, P., Stewart, H. J. S., Chevassut, T. J. & Walker, M. & 3 others, , 10 Feb 2020, In: Organometallics. 39, 3Research output: Contribution to journal › Article › peer-review
9 Citations (Scopus) -
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) -
Understanding and Improving the Membrane Permeability of VH032-Based PROTACs
Klein, V. G., Townsend, C. E., Testa, A., Zengerle, M., Maniaci, C., Hughes, S. J., Chan, K.-H., Ciulli, A. & Lokey, R. S. (Lead / Corresponding author), 10 Sept 2020, In: ACS Medicinal Chemistry Letters. 11, 9, p. 1732-1738 7 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile90 Citations (Scopus)303 Downloads (Pure) -
2018
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
Chan, K. H., Zengerle, M., Testa, A. & Ciulli, A. (Lead / Corresponding author), 25 Jan 2018, In: Journal of Medicinal Chemistry. 61, 2, p. 504-513 10 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile173 Citations (Scopus)381 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
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) -
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) -
Structural basis of PROTAC cooperative recognition for selective protein degradation
Gadd, M., Testa, A., Lucas, X., Chan, K. H., Chen, W., Lamont, D., Zengerle, M. & Ciulli, A. (Lead / Corresponding author), May 2017, In: Nature Chemical Biology. 13, 5, p. 514-521 11 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile839 Citations (Scopus)697 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) -
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) -
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
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) -
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) -
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)211 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)