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Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis

  • Read more about Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis

Myrianthopoulos, V., Gaboriaud-Kolar, N., Tallant, C., Hall, M.-L., Grigoriou, S., Brownlee, P. M., … Mikros, E. (2016). Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis. Journal of Medicinal Chemistry, 59(19), 8787–8803.

Advances and challenges in understanding histone demethylase biology

  • Read more about Advances and challenges in understanding histone demethylase biology

Nowak, R., Tumber, A., Johansson, C., Che, K., Brennan, P., Owen, D., Oppermann, U. (2016). Advances and challenges in understanding histone demethylase biology. Current Opinion In Chemical Biology, 33, 151-159.

Protein-Protein Interaction Inhibition (2P2I)-Oriented Chemical Library Accelerates Hit Discovery

  • Read more about Protein-Protein Interaction Inhibition (2P2I)-Oriented Chemical Library Accelerates Hit Discovery

Milhas, S., Raux, B., Betzi, S., Derviaux, C., Roche, P., Restouin, A., … Morelli, X. (2016). Protein–Protein Interaction Inhibition (2P2I)-Oriented Chemical Library Accelerates Hit Discovery. ACS Chemical Biology, 11(8), 2140-2148.

BET inhibition as a new strategy for the treatment of gastric cancer

  • Read more about BET inhibition as a new strategy for the treatment of gastric cancer

Montenegro, R. C., Clark, P. G. K., Howarth, A., Wan, X., Ceroni, A., Siejka, P., … Müller, S. (2016). BET inhibition as a new strategy for the treatment of gastric cancer. Oncotarget, 7(28), 43997–44012.

Structural analysis of human KDM5B guides histone demethylase inhibitor development

  • Read more about Structural analysis of human KDM5B guides histone demethylase inhibitor development

Johansson, C., Velupillai, S., Tumber, A., Szykowska, A., Hookway, E. S., Nowak, R. P., … Oppermann, U. (2016). Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nature Chemical Biology, 12(7), 539-545.

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex

  • Read more about Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex

Sutherell, C. L., Tallant, C., Monteiro, O. P., Yapp, C., Fuchs, J. E., Fedorov, O., … Ley, S. V. (2016). Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex. Journal of Medicinal Chemistry, 59(10), 5095–5101.

Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk

  • Read more about Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk

Sdelci, S., Lardeau, C., Tallant, C., Klepsch, F., Klaiber, B., Bennett, J., … Kubicek, S. (2016). Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk. Nature Chemical Biology, 12(7), 504-510.

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

  • Read more about Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

Gerstenberger, B. S., Trzupek, J. D., Tallant, C., Fedorov, O., Filippakopoulos, P., Brennan, P. E., … Owen, D. R. (2016). Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit. Journal of Medicinal Chemistry, 59(10), 4800–4811.

Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib

  • Read more about Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib

Mathea, S., Abdul Azeez, K. R., Salah, E., Tallant, C., Wolfreys, F., Konietzny, R., … Knapp, S. (2016). Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib. ACS Chemical Biology, 11(6), 1595–1602.

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

  • Read more about Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

Martin, L. J., Koegl, M., Bader, G., Cockcroft, X.-L., Fedorov, O., Fiegen, D., … McConnell, D. (2016). Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. Journal of Medicinal Chemistry, 59(10), 4462–4475.

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The ULTRA-DD project is supported by the Innovative Medicines Initiative Joint Undertaking (IMI JU) under grant agreement n° [115766], resources of which are composed of financial contribution from the European Union's Seventh Framework Programme (FP7/2007-2013) and EFPIA companies’ in kind contribution. This website reflects only the author’s views and neither IMI nor the European Commission is liable for any use that may be made of the information contained therein.
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