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Structural Basis for Recruitment of DAPK1 to the KLHL20 E3 Ligase.

  • Read more about Structural Basis for Recruitment of DAPK1 to the KLHL20 E3 Ligase.

Chen, Z., Picaud, S., Filippakopoulos, P., D'Angiolella, V., & Bullock, A. N. (2019). Structural Basis for Recruitment of DAPK1 to the KLHL20 E3 Ligase. Structure (London, England : 1993), 27(9), 1395–1404.e4.

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).

  • Read more about Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).

Xiong, Y., Greschik, H., Johansson, C., Seifert, L., Bacher, J., Park, K, ... Jin J. (2019). Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1). Journal Of Medicinal Chemistry, 62(20), 8996-9007.

A genetics-led approach defines the drug target landscape of 30 immune-related traits.

  • Read more about A genetics-led approach defines the drug target landscape of 30 immune-related traits.

Fang, H., De Wolf, H., Knezevic, B., Burnham, K., Osgood, J., Sanniti, A., ... Knight, J. (2019). A genetics-led approach defines the drug target landscape of 30 immune-related traits. Nature Genetics, 51(7), 1082-1091.

Structural basis of HMCES interactions with abasic DNA and multivalent substrate recognition.

  • Read more about Structural basis of HMCES interactions with abasic DNA and multivalent substrate recognition.

Halabelian, L., Ravichandran, M., Li, Y., Zeng, H., Rao, A., Aravind, L., & Arrowsmith, C. H. (2019). Structural basis of HMCES interactions with abasic DNA and multivalent substrate recognition. Nature structural & molecular biology, 26(7), 607–612.

Structure-guided fragment-based drug discovery at the synchrotron: screening binding sites and correlations with hotspot mapping.

  • Read more about Structure-guided fragment-based drug discovery at the synchrotron: screening binding sites and correlations with hotspot mapping.

Thomas, S. E., Collins, P., James, R. H., Mendes, V., Charoensutthivarakul, S., Radoux, C., … Blundell, T. L. (2019). Structure-guided fragment-based drug discovery at the synchrotron: screening binding sites and correlations with hotspot mapping. Philosophical transactions. Series A, Mathematical, physical, and engineering sciences, 377(2147), 20180422.

Synthesis and structure-activity relationships of 3,5-disubstituted-pyrrolo[2,3- b]pyridines as inhibitors of adaptor associated kinase 1 (AAK1) with antiviral activity.

  • Read more about Synthesis and structure-activity relationships of 3,5-disubstituted-pyrrolo[2,3- b]pyridines as inhibitors of adaptor associated kinase 1 (AAK1) with antiviral activity.

Verdonck, S., Pu, S., Sorrell, F., Elkins, J., Froeyen, M., Gao, L., ...  De Jonghe, S. (2019). Synthesis and Structure–Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3-b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity. Journal Of Medicinal Chemistry, 62(12), 5810-5831.

Targeting protein methylation: from chemical tools to precision medicines.

  • Read more about Targeting protein methylation: from chemical tools to precision medicines.

Dilworth, D., Barsyte-Lovejoy, D. (2019). Targeting protein methylation: from chemical tools to precision medicines. Cellular And Molecular Life Sciences, 76(15), 2967-2985.

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.

  • Read more about C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.

Le Bihan, Y. V., Lanigan, R. M., Atrash, B., McLaughlin, M. G., Velupillai, S., Malcolm, A. G., … Bavetsias, V. (2019). C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays. European journal of medicinal chemistry, 177, 316–337.

Structure of the human frataxin-bound iron-sulfur cluster assembly complex provides insight into its activation mechanism.

  • Read more about Structure of the human frataxin-bound iron-sulfur cluster assembly complex provides insight into its activation mechanism.

Fox, N. G., Yu, X., Feng, X., Bailey, H. J., Martelli, A., Nabhan, J. F., … Han, S. (2019). Structure of the human frataxin-bound iron-sulfur cluster assembly complex provides insight into its activation mechanism. Nature communications, 10(1), 2210.

The dynamic conformational landscape of the protein methyltransferase SETD8.

  • Read more about The dynamic conformational landscape of the protein methyltransferase SETD8.

Chen, S., Wiewiora, R. P., Meng, F., Babault, N., Ma, A., Yu, W., … Luo, M. (2019). The dynamic conformational landscape of the protein methyltransferase SETD8. eLife, 8, e45403.

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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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