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ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma.

  • Read more about ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma.

Carvalho, D., Taylor, K., Olaciregui, N., Molinari, V., Clarke, M., Mackay, A., ... Jones, C., (2019). ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma. Communications Biology, 2(1).

Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.

  • Read more about Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.

Resnick, E., Bradley, A., Gan, J., Douangamath, A., Krojer, T., Sethi, R., … London, N. (2019). Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. Journal of the American Chemical Society, 141(22), 8951–8968.

A Perspective on Extreme Open Science: Companies Sharing Compounds without Restriction.

  • Read more about A Perspective on Extreme Open Science: Companies Sharing Compounds without Restriction.

Drewry, D., Wells, C., Zuercher, W., & Willson, T. (2019). A Perspective on Extreme Open Science: Companies Sharing Compounds without Restriction. SLAS Discovery: Advancing Life Sciences R&D, 24(5), 505-514.

Crystal structure of human RIOK2 bound to a specific inhibitor.

  • Read more about Crystal structure of human RIOK2 bound to a specific inhibitor.

Wang, J., Varin, T., Vieth, M., & Elkins, J. M. (2019). Crystal structure of human RIOK2 bound to a specific inhibitor. Open biology, 9(4), 190037.

Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase.

  • Read more about Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase.

Zhang, R., McIntyre, P., Collins, P., Foley, D., Arter, C., von Delft, F., ... Nelson, A. (2019). Construction of a Shape‐Diverse Fragment Set: Design, Synthesis and Screen against Aurora‐A Kinase. Chemistry – A European Journal, 25(27), 6831-6839.

Discovery of selective activators of PRC2 mutant EED-I363M.

  • Read more about Discovery of selective activators of PRC2 mutant EED-I363M.

Suh, J. L., Barnash, K. D., Abramyan, T. M., Li, F., The, J., Engelberg, I. A., … Frye, S. V. (2019). Discovery of selective activators of PRC2 mutant EED-I363M. Scientific reports, 9(1), 6524.

A chemical toolbox for the study of bromodomains and epigenetic signaling.

  • Read more about A chemical toolbox for the study of bromodomains and epigenetic signaling.

Wu, Q., Heidenreich, D., Zhou, S., Ackloo, S., Krämer, A., Nakka, K., … Knapp, S. (2019). A chemical toolbox for the study of bromodomains and epigenetic signaling. Nature communications, 10(1), 1915.

Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.

  • Read more about Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.

Asquith, C., Naegeli, K., East, M., Laitinen, T., Havener, T., Wells, C., ... Morris, D. (2019). Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. Journal Of Medicinal Chemistry, 62(9), 4772-4778.

Discovery of Pyrrolo[3,2-d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell Active Inhibitors of P300/CBP-Associated Factor Bromodomain.

  • Read more about Discovery of Pyrrolo[3,2-d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell Active Inhibitors of P300/CBP-Associated Factor Bromodomain.

Huang, L., Li, H., Li, L., Niu, L., Seupel, R., Wu, C., ... Yang, S. (2019). Discovery of Pyrrolo[3,2-d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain. Journal Of Medicinal Chemistry, 62(9), 4526-4542.

Structural analyses reveal that MBD3 is a methylated-CG binder.

  • Read more about Structural analyses reveal that MBD3 is a methylated-CG binder.

Liu, K., Lei, M., Wu, Z., Gan, B., Cheng, H., Li, Y., & Min, J. (2019). Structural analyses reveal that MBD 3 is a methylated CG binder. The FEBS Journal, 286(16), 3240-3254.

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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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