1EBP

COMPLEX BETWEEN THE EXTRACELLULAR DOMAIN OF ERYTHROPOIETIN (EPO) RECEPTOR [EBP] AND AN AGONIST PEPTIDE [EMP1]

1EBP の概要

• エントリーDOI: 10.2210/pdb1ebp/pdb
• 分子名称: EPO RECEPTOR, EPO MIMETICS PEPTIDE 1 (2 entities in total)
• 機能のキーワード: erythropoietin receptor, signal transduction, protein minimization, drug design, cytokine receptor class 1, complex (cytokine receptor-peptide), complex (cytokine receptor-peptide) complex, complex (cytokine receptor/peptide)
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cell membrane; Single-pass type I membrane protein. Isoform EPOR-S: Secreted: P19235
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 50849.69

構造登録者

Livnah, O.,Stura, E.A.,Wilson, I.A. (登録日: 1996-05-07, 公開日: 1997-07-29, 最終更新日: 2024-10-30)

主引用文献

Livnah, O.,Stura, E.A.,Johnson, D.L.,Middleton, S.A.,Mulcahy, L.S.,Wrighton, N.C.,Dower, W.J.,Jolliffe, L.K.,Wilson, I.A.
Functional mimicry of a protein hormone by a peptide agonist: the EPO receptor complex at 2.8 A.
Science, 273:464-471, 1996

PubMed Abstract: The functional mimicry of a protein by an unrelated small molecule has been a formidable challenge. Now, however, the biological activity of a 166-residue hematopoietic growth hormone, erythropoietin (EPO), with its class 1 cytokine receptor has been mimicked by a 20-residue cyclic peptide unrelated in sequence to the natural ligand. The crystal structure at 2.8 A resolution of a complex of this agonist peptide with the extracellular domain of EPO receptor reveals that a peptide dimer induces an almost perfect twofold dimerization of the receptor. The dimer assembly differs from that of the human growth hormone (hGH) receptor complex and suggests that more than one mode of dimerization may be able to induce signal transduction and cell proliferation. The EPO receptor binding site, defined by peptide interaction, corresponds to the smaller functional epitope identified for hGH receptor. Similarly, the EPO mimetic peptide ligand can be considered as a minimal hormone, and suggests the design of nonpeptidic small molecule mimetics for EPO and other cytokines may indeed be achievable.

PubMed: 8662530

実験手法

X-RAY DIFFRACTION (2.8 Å)