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Small Molecule Inhibitors Reveal an Indispensable Scaffolding Role of RIPK2 in NOD2 Signaling

  • Read more about Small Molecule Inhibitors Reveal an Indispensable Scaffolding Role of RIPK2 in NOD2 Signaling

Hrdinka, M., Schlicher, L., Dai, B., Pinkas, D. M., Bufton, J. C., Picaud, S., … Gyrd-Hansen, M. (2018). Small molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling.The EMBO journal, 37(17), e99372.

Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept

  • Read more about Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept

Hudson, L., Mui, J., Vázquez, S., Carvalho, D. M., Williams, E., Jones, C., … Hoelder, S. (2018). Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept. Journal of Medicinal Chemistry, 61(16), 7261–7272.

Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-Benzodiazipinones as Inhibitors of Kinases and Bromodomains

  • Read more about Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-Benzodiazipinones as Inhibitors of Kinases and Bromodomains

Wang, J., Erazo, T., Ferguson, F.M., Buckley, D.L., Gomez, N., Muñoz-Guardiola, P., ... Gray, N.S. (2018). Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-Benzodiazipinones as Inhibitors of Kinases and Bromodomains. ACS Chemical Biology, 13(9), 2438-2448.

Design, Synthesis and Biological Evaluation of 3-(Imidazo[1,2-a]pyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as Dual Inhibitors of Discoidin Domain Receptor 1 and 2 (DDR1/2).

  • Read more about Design, Synthesis and Biological Evaluation of 3-(Imidazo[1,2-a]pyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as Dual Inhibitors of Discoidin Domain Receptor 1 and 2 (DDR1/2).

Wang, Z., Zhang, Y., Pinkas, D. M., Fox, A. E., Luo, J., Huang, H., … Lu, X. (2018). Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2. Journal of medicinal chemistry, 61(17), 7977–7990.

Chemical Instability and Promiscuity of Arylmethylidenepyrazolinone-based MDMX Inhibitors.

  • Read more about Chemical Instability and Promiscuity of Arylmethylidenepyrazolinone-based MDMX Inhibitors.

Stefaniak, J., Lewis, A. M., Conole, D., Galan, S., Bataille, C., Wynne, G. M., … Huber, K. (2018). Chemical Instability and Promiscuity of Arylmethylidenepyrazolinone-Based MDMX Inhibitors. ACS Chemical Biology, 13(10), 2849–2854.

Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors.

  • Read more about Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors.

Santiago, A., Couñago, R. M., Ramos, P. Z., Godoi, P., Massirer, K. B., Gileadi, O., & Elkins, J. M. (2018). Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors. Scientific reports, 8(1), 14800.

Discovery of an MLLT1/3 YEATS Domain Chemical Probe

  • Read more about Discovery of an MLLT1/3 YEATS Domain Chemical Probe

Moustakim, M., Christott, T., Monteiro, O. P., Bennett, J., Giroud, C., Ward, J., … Fedorov, O. (2018). Discovery of an MLLT1/3 YEATS Domain Chemical Probe. Angewandte Chemie (International ed. in English), 57(50), 16302–16307.

Arginine Methylation of FOXP3 is Crucial for The Suppressive Function of Regulatory T Cells.

  • Read more about Arginine Methylation of FOXP3 is Crucial for The Suppressive Function of Regulatory T Cells.

Kagoya, Y., Saijo, H., Matsunaga, Y., Guo, T., Saso, K., Anczurowski, M., ... Hirano, N. (2018). Arginine Methylation of FOXP3 is Crucial for The Suppressive Function of Regulatory T Cells. Journal of Autoimmunity, 97, 10-21.

Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9.

  • Read more about Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9.

Christott, T., Bennett, J., Coxon, C., Monteiro, O., Giroud, C., Beke, V., ... Fedorov, O. (2018). Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9. SLAS Discovery, 24(2), 133-141.

Palladium-Mediated Enzyme Activation Suggests Multiphase Initiation of Glycogenesis.

  • Read more about Palladium-Mediated Enzyme Activation Suggests Multiphase Initiation of Glycogenesis.

Bilyard, MK., Bailey, HJ., Raich, L., Gafitescu, MA., Machida, T., Iglésias-Fernández, J., ... Davis, BG. (2018). Palladium-Mediated Enzyme Activation Suggests Multiphase Initiation of Glycogenesis. Nature, 563(7730), 235-240.

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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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