8E1O

Crystal structure of hTEAD2 bound to a methoxypyridine lipid pocket binder

Summary for 8E1O

• Entry DOI: 10.2210/pdb8e1o/pdb
• Descriptor: Transcriptional enhancer factor TEF-4, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 5-methoxy-N-({3-[2-(methylamino)-2-oxoethyl]phenyl}methyl)-4-{(E)-2-[trans-4-(trifluoromethyl)cyclohexyl]ethenyl}pyridine-2-carboxamide, ... (4 entities in total)
• Functional Keywords: transcription factor inhibitor complex, transcription-inhibitor complex, transcription/inhibitor
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 2
• Total formula weight: 58131.44

Authors

Noland, C.L.,Dey, A.,Zbieg, J.,Crawford, J. (deposition date: 2022-08-10, release date: 2023-08-16, Last modification date: 2024-02-28)

• Primary citation: Pham, T.,Pahuja, K.,Hagenbeek, T.,Zbieg, Z.,Noland, C.L.,Pham, V.C.,Yao, X.,Rose, C.,Browder, K.,Lee, H.J.,Yu, M.,Chu, M.L.,Martin, S.,Verschueren, E.,Li, J.,Kubala, M.,Fong, R.,Lorenzo, M.,Beroza, P.,Hsu, P.,Paul, S.,Villemure, E.,Lee, W.,Cheung, T.,Clausen, S.,Lacap, J.,Liang, Y.,Schmidt, S.,Modrusan, Z.,Cohen, M.,Crawford, J.,Jasper, H.,Ashworth, A.,Lill, J.R.,Malek, S.,Rudolph, J.,Wertz, I.,Chang, M.,Ye, X.,Dey, A.; Targeting the Hippo pathway in cancers via ubiquitination dependent TEAD degradation; Biorxiv, 2024; DOI: 10.1101/2023.10.03.560675

Experimental method

X-RAY DIFFRACTION (2.25 Å)