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

[Image: see text] CREBBP (CBP/KAT3A) and its paralogue EP300 (KAT3B) are lysine acetyltransferases (KATs) that are essential for human development. They each comprise 10 domains through which they interact with >400 proteins, making them important transcriptional co-activators and key nodes in th...

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Udgivet i:J Med Chem
Main Authors: 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.
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2021
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC8311651/
https://ncbi.nlm.nih.gov/pubmed/34255515
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.1c00348
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