The rational design of ARUK2007145, a dual inhibitor of the α and γ isoforms of the lipid kinase phosphatidylinositol 5-phosphate 4-kinase (PI5P4K)

por Aldred, Gregory G., Rooney, Timothy P. C., Willems, Henriette M. G., Boffey, Helen K., Green, Christopher, Winpenny, David, Skidmore, John, Clarke, Jonathan H., Andrews, Stephen P.
Publicado 2023

Isoxazole‐Derived Amino Acids are Bromodomain‐Binding Acetyl‐Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3

por Sekirnik (née Measures), Angelina R., Hewings, David S., Theodoulou, Natalie H., Jursins, Lukass, Lewendon, Katie R., Jennings, Laura E., Rooney, Timothy P. C., Heightman, Tom D., Conway, Stuart J.
Publicado 2016

The Identification of Potent, Selective, and Brain Penetrant PI5P4Kγ Inhibitors as In Vivo-Ready Tool Molecules

por Rooney, Timothy P. C., Aldred, Gregory G., Boffey, Helen K., Willems, Henriëtte M. G., Edwards, Simon, Chawner, Stephen J., Scott, Duncan E., Green, Christopher, Winpenny, David, Skidmore, John, Clarke, Jonathan H., Andrews, Stephen P.
Publicado 2022

Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode

por Boffey, Helen K., Rooney, Timothy P. C., Willems, Henriette M. G., Edwards, Simon, Green, Christopher, Howard, Tina, Ogg, Derek, Romero, Tamara, Scott, Duncan E., Winpenny, David, Duce, James, Skidmore, John, Clarke, Jonathan H., Andrews, Stephen P.
Publicado 2022

Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains

por Hay, Duncan A., Fedorov, Oleg, Martin, Sarah, Singleton, Dean C., Tallant, Cynthia, Wells, Christopher, Picaud, Sarah, Philpott, Martin, Monteiro, Octovia P., Rogers, Catherine M., Conway, Stuart J., Rooney, Timothy P. C., Tumber, Anthony, Yapp, Clarence, Filippakopoulos, Panagis, Bunnage, Mark E., Müller, Susanne, Knapp, Stefan, Schofield, Christopher J., Brennan, Paul E.
Publicado 2014

A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation–π Interaction**

por Rooney, Timothy P C, Filippakopoulos, Panagis, Fedorov, Oleg, Picaud, Sarah, Cortopassi, Wilian A, Hay, Duncan A, Martin, Sarah, Tumber, Anthony, Rogers, Catherine M, Philpott, Martin, Wang, Minghua, Thompson, Amber L, Heightman, Tom D, Pryde, David C, Cook, Andrew, Paton, Robert S, Müller, Susanne, Knapp, Stefan, Brennan, Paul E, Conway, Stuart J
Publicado 2014

Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain

por Brand, Michael, Clayton, James, Moroglu, Mustafa, Schiedel, Matthias, Picaud, Sarah, Bluck, Joseph P., Skwarska, Anna, Bolland, Hannah, Chan, Anthony K. N., Laurin, Corentine M. C., Scorah, Amy R., See, Larissa, Rooney, Timothy P. C., Andrews, Katrina H., Fedorov, Oleg, Perell, Gabriella, Kalra, Prakriti, Vinh, Kayla B., Cortopassi, Wilian A., Heitel, Pascal, Christensen, Kirsten E., Cooper, Richard I., Paton, Robert S., Pomerantz, William C. K., Biggin, Philip C., Hammond, Ester M., Filippakopoulos, Panagis, Conway, Stuart J.
Publicado 2021