Download MendeleyDesign and Structure of Stapled Peptides Binding to Estrogen Receptors.
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.(2011) J Am Chem Soc 133: 9696
- PubMed: 21612236
- DOI: https://doi.org/10.1021/ja202946k
- Primary Citation of Related Structures:
2LDA, 2LDC, 2LDD, 2YJA, 2YJD - 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.
Organizational Affiliation:
Department of Chemistry, Pfizer, Sandwich CT13 9NJ, UK. [email protected]
