7Y8G

Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with an Inhibitor 30a and GRIP Peptide

Summary for 7Y8G

• Entry DOI: 10.2210/pdb7y8g/pdb
• Descriptor: Estrogen receptor, Grip peptide, [4-(1,2,4-triazol-1-yl)phenyl] (1~{S},2~{R},4~{S})-5,6-bis(4-hydroxyphenyl)-7-oxabicyclo[2.2.1]hept-5-ene-2-sulfonate, ... (5 entities in total)
• Functional Keywords: complex, inhibitor, estrogen receptor alpha, transcription, transcription-inhibitor complex, transcription/inhibitor
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 4
• Total formula weight: 61311.90

Authors

Min, J.,Hu, H.B.,Yang, Y.,Dong, C.E.,Zhou, H.B.,Chen, C.-C.,Guo, R.-T. (deposition date: 2022-06-23, release date: 2023-04-26, Last modification date: 2023-11-29)

• Primary citation: Xin, L.,Min, J.,Hu, H.,Li, Y.,Du, C.,Xie, B.,Cheng, Y.,Deng, X.,Deng, X.,Shen, K.,Huang, J.,Chen, C.C.,Guo, R.T.,Dong, C.,Zhou, H.B.; Structure-guided identification of novel dual-targeting estrogen receptor alpha degraders with aromatase inhibitory activity for the treatment of endocrine-resistant breast cancer.; Eur.J.Med.Chem., 253:115328-115328, 2023; PubMed: 37037140; DOI: 10.1016/j.ejmech.2023.115328

Experimental method

X-RAY DIFFRACTION (2.14 Å)