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

Authors: Le Bihan, Yann-Vaï, Lanigan, Rachel M., Atrash, Butrus, McLaughlin, Mark G., Velupillai, Srikannathasan, Malcolm, Andrew G., England, Katherine S., Ruda, Gian Filippo, Mok, N. Yi, Tumber, Anthony, Tomlin, Kathy, Saville, Harry, Shehu, Erald, McAndrew, Craig, Carmichael, LeAnne, Bennett, James M., Jeganathan, Fiona, Eve, Paul, Donovan, Adam, Hayes, Angela, Wood, Francesca, Raynaud, Florence I., Fedorov, Oleg, Brennan, Paul E., Burke, Rosemary, van Montfort, Rob L.M., Rossanese, Olivia W., Blagg, Julian, Bavetsias, Vassilios

Source: In European Journal of Medicinal Chemistry 1 September 2019 177:316-337

Deliberately Losing Control of C−H Activation Processes in the Design of Small‐Molecule‐Fragment Arrays Targeting Peroxisomal Metabolism.

Authors: Khan Tareque, Raysa, Hassell‐Hart, Storm, Krojer, Tobias, Bradley, Anthony, Velupillai, Srikannathasan, Talon, Romain, Fairhead, Michael, Day, Iain J., Bala, Kamlesh, Felix, Robert, Kemmitt, Paul D., Brennan, Paul, Delft, Frank, Díaz Sáez, Laura, Huber, Kilian, Spencer, John

Source: ChemMedChem; 12/15/2020, Vol. 15 Issue 24, p2513-2520, 8p

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.

Authors: Fagan, Vincent^1,2 (AUTHOR), Johansson, Catrine^1,3 (AUTHOR), Gileadi, Carina^1,3 (AUTHOR), Monteiro, Octovia^1,2 (AUTHOR), Dunford, James E.³ (AUTHOR), Nibhani, Reshma³ (AUTHOR), Philpott, Martin³ (AUTHOR), Malzahn, Jessica³ (AUTHOR), Wells, Graham³ (AUTHOR), Faram, Ruth³ (AUTHOR), Cribbs, Adam P.³ (AUTHOR), Halidi, Nadia^1,3 (AUTHOR), Li, Fengling⁴ (AUTHOR), Chau, Irene⁴ (AUTHOR), Greschik, Holger⁵ (AUTHOR), Velupillai, Srikannathasan¹ (AUTHOR), Allali-Hassani, Abdellah⁴ (AUTHOR), Bennett, James^1,2 (AUTHOR), Christott, Thomas^1,2 (AUTHOR), Giroud, Charline^1,2 (AUTHOR)

Source: Journal of Medicinal Chemistry. 10/24/2019, Vol. 62 Issue 20, p9008-9025. 18p.

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Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.

Authors: Vazquez‐Rodriguez, Saleta¹, Wright, Miranda^1,2, Rogers, Catherine M.¹, Cribbs, Adam P.³, Velupillai, Srikannathasan¹, Philpott, Martin³, Lee, Henry³, Dunford, James E.³, Huber, Kilian V. M.¹, Robers, Matthew B.⁴, Vasta, James D.⁴, Thezenas, Marie‐Laetitia⁵, Bonham, Sarah⁵, Kessler, Benedikt⁵, Bennett, James¹, Fedorov, Oleg¹, Raynaud, Florence⁶, Donovan, Adam⁶, Blagg, Julian⁶, Bavetsias, Vassilios⁶

Source: Angewandte Chemie International Edition; Jan2019, Vol. 58 Issue 2, p515-519, 5p

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Phosphorylation of Synaptic Vesicle Protein 2A at Thr84 by Casein Kinase 1 Family Kinases Controls the Specific Retrieval of Synaptotagmin-1.

Authors: Ning Zhang, Gordon, Sarah L., Fritsch, Maximilian J., Esoof, Noor, Campbell, David G., Gourlay, Robert, Velupillai, Srikannathasan, Macartney, Thomas, Peggie, Mark, van Aalten, Daan M. F., Cousin, Michael A., Alessi, Dario R.

Source: Journal of Neuroscience; 2/11/2015, Vol. 35 Issue 6, p2492-2507, 16p

Subject Terms: SYNAPTOTAGMINS, CASEIN kinase regulation, SYNAPTIC vesicles, NEUROTRANSMITTER receptors, CELLULAR signal transduction, ENDOCYTOSIS, EVOKED potentials (Electrophysiology)

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