7JUO

CBP bromodomain complexed with YF2-23

Summary for 7JUO

• Entry DOI: 10.2210/pdb7juo/pdb
• Descriptor: CREB-binding protein, N-{1-[1,1-di(pyridin-2-yl)ethyl]-6-(1-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-3-yl)-1H-indol-4-yl}ethanesulfonamide (3 entities in total)
• Functional Keywords: dual bet/cbp inhibitor, transcription
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 8
• Total formula weight: 116357.26

Authors

Ratia, K.M.,Xiong, R.,Principe, D.,Li, Y.,Huang, F.,Rana, A.,Thatcher, G. (deposition date: 2020-08-20, release date: 2021-09-01, Last modification date: 2023-10-18)

• Primary citation: Principe, D.R.,Xiong, R.,Li, Y.,Pham, T.N.D.,Kamath, S.D.,Dubrovskyi, O.,Ratia, K.,Huang, F.,Zhao, J.,Shen, Z.,Thummuri, D.,Daohong, Z.,Underwood, P.W.,Trevino, J.,Munshi, H.G.,Thatcher, G.R.J.,Rana, A.; XP-524 is a dual-BET/EP300 inhibitor that represses oncogenic KRAS and potentiates immune checkpoint inhibition in pancreatic cancer.; Proc.Natl.Acad.Sci.USA, 119:-, 2022; PubMed: 35064087; DOI: 10.1073/pnas.2116764119

Experimental method

X-RAY DIFFRACTION (2.2 Å)