5WGD

Estrogen Receptor Alpha Ligand Binding Domain in Complex with Estradiol and SRC2-LP1

Summary for 5WGD

Entry DOI	10.2210/pdb5wgd/pdb
Descriptor	Estrogen receptor, (ACE)HKILHKLLQDS(NH2), (ACE)AILHKLLQDS(NH2), ... (5 entities in total)
Functional Keywords	breast cancer, stapled peptides, synthetic peptides, hormone, transcription
Biological source	Homo sapiens (Human) More
Total number of polymer chains	4
Total formula weight	62616.04
Authors	Fanning, S.W.,Speltz, T.E.,Mayne, C.G.,Siddiqui, Z.,Greene, G.L.,Tajkhorshid, E.,Moore, T.W. (deposition date: 2017-07-14, release date: 2018-06-13, Last modification date: 2024-10-23)
Primary citation	Speltz, T.E.,Mayne, C.G.,Fanning, S.W.,Siddiqui, Z.,Tajkhorshid, E.,Greene, G.L.,Moore, T.W. A "cross-stitched" peptide with improved helicity and proteolytic stability. Org. Biomol. Chem., 16:3702-3706, 2018 Cited by PubMed Abstract: A new computational approach to obtain quantitative energy profiles for helix folding was used in the design of orthogonal hydrocarbon and lactam bicyclic peptides. The proteolytically stable, "cross-stitched" peptide SRC2-BCP1 shows nanomolar affinity for estrogen receptor α and X-ray crystallography confirms a helical binding pose. PubMed: 29725689 DOI: 10.1039/c8ob00790j PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.8 Å)

Structure validation