6SWN

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH iBET-BD1 (GSK778)

This is a non-PDB format compatible entry.

Summary for 6SWN

• Entry DOI: 10.2210/pdb6swn/pdb
• Descriptor: Bromodomain-containing protein 4, GLUTAMIC ACID, 4-[2-(methoxymethyl)-1-[(1~{R})-1-phenylethyl]-8-[[(3~{S})-pyrrolidin-3-yl]methoxy]imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole, ... (5 entities in total)
• Functional Keywords: inhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist, transcription
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 15820.19

Authors

Chung, C. (deposition date: 2019-09-22, release date: 2020-04-01, Last modification date: 2020-05-06)

• Primary citation: Gilan, O.,Rioja, I.,Knezevic, K.,Bell, M.J.,Yeung, M.M.,Harker, N.R.,Lam, E.Y.N.,Chung, C.W.,Bamborough, P.,Petretich, M.,Urh, M.,Atkinson, S.J.,Bassil, A.K.,Roberts, E.J.,Vassiliadis, D.,Burr, M.L.,Preston, A.G.S.,Wellaway, C.,Werner, T.,Gray, J.R.,Michon, A.M.,Gobbetti, T.,Kumar, V.,Soden, P.E.,Haynes, A.,Vappiani, J.,Tough, D.F.,Taylor, S.,Dawson, S.J.,Bantscheff, M.,Lindon, M.,Drewes, G.,Demont, E.H.,Daniels, D.L.,Grandi, P.,Prinjha, R.K.,Dawson, M.A.; Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation.; Science, 368:387-394, 2020; PubMed: 32193360; DOI: 10.1126/science.aaz8455

Experimental method

X-RAY DIFFRACTION (1.28 Å)