A Systems Approach for the Fragment-based Development of Selective Chemical Probes of Bromodomain Function (joint with University of Oxford)

Research Output

  • 12 Article
  • 1 Chapter (peer-reviewed)
  • 1 Short survey
  • 1 Review article
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Article
2018
Open Access
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54 Citations (Scopus)
167 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., 7 Mar 2018, In : Chemical Science. 9, 9, p. 2452-2468 17 p., 2452.

Research output: Contribution to journalArticle

Open Access
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9 Citations (Scopus)
187 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., Aug 2017, In : ACS Omega. 2, 8, p. 4328-4332 5 p.

Research output: Contribution to journalArticle

Open Access
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2 Citations (Scopus)
115 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., 4 May 2017, In : Biochemical Journal. 474, 10, p. 1633-1651 19 p.

Research output: Contribution to journalArticle

Open Access
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9 Citations (Scopus)
185 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., May 2017, In : Nature Chemical Biology. 13, 5, p. 514-521 11 p.

Research output: Contribution to journalArticle

Open Access
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197 Citations (Scopus)
363 Downloads (Pure)
2016

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., 25 Feb 2016, In : Journal of Medicinal Chemistry. 59, 4, p. 1492-1500 9 p.

Research output: Contribution to journalArticle

Open Access
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22 Citations (Scopus)
280 Downloads (Pure)

Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology

Galdeano, C. & Ciulli, A., Sep 2016, In : Future Medicinal Chemistry. 8, 13, p. 1655-1680 26 p.

Research output: Contribution to journalArticle

Open Access
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32 Citations (Scopus)
576 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., 6 Jan 2015, In : Structure. 23, 1, p. 80-92 13 p.

Research output: Contribution to journalArticle

31 Citations (Scopus)

Selective small molecule induced degradation of the BET bromodomain protein BRD4

Zengerle, M., Chan, K-H. & Ciulli, A., 21 Aug 2015, In : ACS Chemical Biology. 10, 8, p. 1770-1777 8 p.

Research output: Contribution to journalArticle

Open Access
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273 Citations (Scopus)
215 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., 31 Oct 2014, In : Science. 346, 6209, p. 638-641 4 p.

Research output: Contribution to journalArticle

79 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., 28 Oct 2014, In : Biochemistry. 53, 42, p. 6706-6716 11 p.

Research output: Contribution to journalArticle

Open Access
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10 Citations (Scopus)
234 Downloads (Pure)
Open Access
File
32 Citations (Scopus)
144 Downloads (Pure)