Controlling Intramolecular Interactions in the Design of Selective, High-Affinity, Ligands for the CREBBP Bromodomain Michael Brand,† James Clayton,† Mustafa Moroglu,† Matthias Schiedel,† Sarah Picaud,‡ Joseph P. Bluck,†,§ Anna Skwarska,ǁ Anthony K. N. Chan,† Corentine M. C. Laurin,† Amy R. Scorah,† K. F. Larissa See,† Timothy P. C. Rooney,† Oleg Fedorov,‡ Gabriella Perell,# Prakriti Kalra,# Wilian A. Cortopassi,† Kirsten E. Christensen,† Richard I. Cooper,† Robert S. Paton,†,∇ William C. K. Pomerantz,# Philip C. Biggin,§ Ester M. Hammond,ǁ Panagis Filippakopoulos,‡ Stuart J. Conway†,* †Department of Chemistry, Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford OX1 3TA, U.K. ‡Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 3TA, U.K. §Department of Biochemistry, University of Oxford, South ParKs Road, Oxford OX1 3QU, U.K. ǁOxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Oxford, OX3 7DQ, U.K. #Department of Chemistry, University of Minnesota, 207 Pleasant Street SE, Minneapolis, Minnesota 55455, U.S.A. ∇Department of Chemistry, Colorado State University, 1301 Center Ave, Ft. Collins, CO 80523- 1872, U.S.A. *To whom correspondence should be addressed:
[email protected] 1 Michael Brand 0000-0002-6998-0516 James Clayton 0000-0002-9126-4030 Mustafa Moroglu 0000-0003-4841-9241 Matthias Schiedel 0000-0001-7365-3617 Sarah Picaud 0000-0002-3803-4455 Anthony K. N. Chan 0000-0002-7091-1294 Corentine M.C. Laurin 0000-0001-8808-9406 Joseph P. Bluck 0000-0001-9170-5919 Amy R. Scorah 0000-0001-7327-4502 Larissa See 0000-0002-7192-9007 Timothy P.