2YJD

Stapled peptide bound to Estrogen Receptor Beta

Summary for 2YJD

• Entry DOI: 10.2210/pdb2yjd/pdb
• Related: 1L2J 1NDE 1QKM 1U3Q 1U3R 1U3S 1U9E 1X76 1X78 1X7B 1X7J 1YY4 1YYE 2FSZ 2JJ3 2LDA 2LDC 2LDD 2YJA 2YLY
• Descriptor: ESTROGEN RECEPTOR BETA, STAPLED PEPTIDE, 4-(2-PROPAN-2-YLOXYBENZIMIDAZOL-1-YL)PHENOL, ... (4 entities in total)
• Functional Keywords: hormone receptor-peptide complex, hormone receptor/peptide
• Biological source: HOMO SAPIENS (HUMAN); More
• Cellular location: Nucleus : Q92731
• Total number of polymer chains: 4
• Total formula weight: 57466.20

Authors

Phillips, C.,Roberts, L.R.,Schade, M.,Bent, A.,Davies, N.L.,Moore, R.,Pannifer, A.D.,Brown, D.G.,Pickford, A.R.,Irving, S.L. (deposition date: 2011-05-19, release date: 2011-08-03, Last modification date: 2024-11-20)

Primary citation

Phillips, C.,Roberts, L.R.,Schade, M.,Bazin, R.,Bent, A.,Davies, N.L.,Moore, R.,Pannifer, A.D.,Pickford, A.R.,Prior, S.H.,Read, C.M.,Scott, A.,Brown, D.G.,Xu, B.,Irving, S.L.
Design and Structure of Stapled Peptides Binding to Estrogen Receptors.
J.Am.Chem.Soc., 133:9696-, 2011

PubMed Abstract: Synthetic peptides that specifically bind nuclear hormone receptors offer an alternative approach to small molecules for the modulation of receptor signaling and subsequent gene expression. Here we describe the design of a series of novel stapled peptides that bind the coactivator peptide site of estrogen receptors. Using a number of biophysical techniques, including crystal structure analysis of receptor-stapled peptide complexes, we describe in detail the molecular interactions and demonstrate that all-hydrocarbon staples modulate molecular recognition events. The findings have implications for the design of stapled peptides in general.

PubMed: 21612236
DOI: 10.1021/JA202946K

Experimental method

X-RAY DIFFRACTION (1.93 Å)