Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain
Michael Brand, James Clayton, Mustafa Moroglu, Matthias Schiedel, S. Picaud, Joseph P. Bluck, Anna Skwarska, Hannah R. Bolland, Anthony Chan, Corentine M. C. Laurin, Amy R. Scorah, Larissa See, Timothy P. C. Rooney, Katrina H. Andrews, Oleg Fedorov, Gabriella Perell, Prakriti Kalra, Kayla B. Vinh, Wilian A. Cortopassi, Pascal Heitel, Kirsten E. Christensen, Richard I. Cooper, Robert S. Paton, William C. K. Pomerantz, Philip C. Biggin, Ester M. Hammond, P. Filippakopoulos, Stuart J. Conway
Abstract
), the inhibition of the CREBBP/EP300 bromodomain results in the enhanced stabilization of HIF-1α.
Topics & Concepts
BromodomainCREB-binding proteinChemistryAcetylationBRD4BiochemistryHistoneCell biologyTranscription factorBiologyGeneCREBProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysPeptidase Inhibition and Analysis