2YJA

Stapled Peptides binding to Estrogen Receptor alpha.

Summary for 2YJA

• Entry DOI: 10.2210/pdb2yja/pdb
• Related: 1A52 1AKF 1ERE 1ERR 1G50 1GWQ 1GWR 1HCP 1HCQ 1L2I 1PCG 1QKT 1QKU 1R5K 1SJ0 1UOM 1X7E 1X7R 1XP1 1XP6 1XP9 1XPC 1XQC 1YIM 1YIN 1ZKY 2AYR 2B1V 2BJ4 2FAI 2JF9 2JFA 2LDA 2LDC 2LDD 2YAT 2YJD 3ERD 3ERT
• Descriptor: STAPLED PEPTIDE, ESTROGEN RECEPTOR, ESTRADIOL, ... (4 entities in total)
• Functional Keywords: hormone receptor-peptide complex, hormone receptor/peptide
• Biological source: HOMO SAPIENS (HUMAN); More
• Cellular location: Isoform 1: Nucleus. Isoform 3: Nucleus: P03372
• Total number of polymer chains: 2
• Total formula weight: 30780.33

Authors

Phillips, C.,Roberts, L.R.,Schade, M.,Bazin, R.,Bent, A.,Davies, N.L.,Irving, S.L.,Moore, R.,Pannifer, A.D.,Brown, D.G.,Pickford, A.R.,Scott, A.,Xu, B. (deposition date: 2011-05-19, release date: 2011-08-03)

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 (1.82 Å)