5WGQ

Estrogen Receptor Alpha Ligand Binding Domain in Complex with Estradiol and SRC2-BCP1

Summary for 5WGQ

Entry DOI	10.2210/pdb5wgq/pdb
Related PRD ID	PRD_002318
Descriptor	Estrogen receptor, SRC2-BCP1, ESTRADIOL, ... (4 entities in total)
Functional Keywords	breast cancer, stapled peptides, synthetic peptides, hormone., transcription, transcription-transcription inhibitor complex, transcription/transcription inhibitor
Biological source	Homo sapiens (Human) More
Total number of polymer chains	4
Total formula weight	62868.39
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: 2024-10-30)
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 (2.3 Å)

Structure validation