7TD9

G-059 bound to the SMARCA4 (BRG1) Bromodomain

This is a non-PDB format compatible entry.

Summary for 7TD9

• Entry DOI: 10.2210/pdb7td9/pdb
• Related: 7TAB
• Descriptor: Isoform 4 of Transcription activator BRG1, 4-phenyl-5H-pyridazino[4,3-b]indol-3-amine (3 entities in total)
• Functional Keywords: bromodomain brg1 smarca4 inhibitor, protein binding, hydrolase, hydrolase-hydrolase inhibitor complex, hydrolase/hydrolase inhibitor
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 3
• Total formula weight: 46093.57

Authors

Tang, Y.,Poy, F.,Taylor, A.M.,Cochran, A.G.,Bellon, S.F. (deposition date: 2021-12-30, release date: 2022-08-17, Last modification date: 2023-10-18)

• Primary citation: Taylor, A.M.,Bailey, C.,Belmont, L.D.,Campbell, R.,Cantone, N.,Cote, A.,Crawford, T.D.,Cummings, R.,DeMent, K.,Duplessis, M.,Flynn, M.,Good, A.C.,Huang, H.R.,Joshi, S.,Leblanc, Y.,Murray, J.,Nasveschuk, C.G.,Neiss, A.,Poy, F.,Romero, F.A.,Sandy, P.,Tang, Y.,Tsui, V.,Zawadzke, L.,Sims 3rd, R.J.,Audia, J.E.,Bellon, S.F.,Magnuson, S.R.,Albrecht, B.K.,Cochran, A.G.; GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.; J.Med.Chem., 65:11177-11186, 2022; PubMed: 35930799; DOI: 10.1021/acs.jmedchem.2c00662

Experimental method

X-RAY DIFFRACTION (1.61 Å)