4RWD

XFEL structure of the human delta opioid receptor in complex with a bifunctional peptide

4RWD の概要

• エントリーDOI: 10.2210/pdb4rwd/pdb
• 関連するPDBエントリー: 4EJ4 4N6H 4RWA
• 関連するBIRD辞書のPRD_ID: PRD_001256
• 分子名称: Soluble cytochrome b562,Delta-type opioid receptor, bifunctional peptide, OLEIC ACID, ... (6 entities in total)
• 機能のキーワード: human opioid receptor, bifunctional peptide, gpcr signaling, gpcr network, membrane protein, psi-biology, structural genomics, gpcr, membrane, lipidic cubic phase, x-ray free-electron laser, serial femtosecond crystallography, bril
• 由来する生物種: Escherichia coli; 詳細
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 95688.01

構造登録者

Fenalti, G.,Zatsepin, N.A.,Betti, C.,Giguere, P.,Han, G.W.,Ishchenko, A.,Liu, W.,Guillemyn, K.,Zhang, H.,James, D.,Wang, D.,Weierstall, U.,Spence, J.C.H.,Boutet, S.,Messerschmidt, M.,Williams, G.J.,Gati, C.,Yefanov, O.M.,White, T.A.,Oberthuer, D.,Metz, M.,Yoon, C.H.,Barty, A.,Chapman, H.N.,Basu, S.,Coe, J.,Conrad, C.E.,Fromme, R.,Fromme, P.,Tourwe, D.,Schiller, P.W.,Roth, B.L.,Ballet, S.,Katritch, V.,Stevens, R.C.,Cherezov, V.,GPCR Network (GPCR) (登録日: 2014-12-02, 公開日: 2015-01-14, 最終更新日: 2024-11-20)

主引用文献

Fenalti, G.,Zatsepin, N.A.,Betti, C.,Giguere, P.,Han, G.W.,Ishchenko, A.,Liu, W.,Guillemyn, K.,Zhang, H.,James, D.,Wang, D.,Weierstall, U.,Spence, J.C.,Boutet, S.,Messerschmidt, M.,Williams, G.J.,Gati, C.,Yefanov, O.M.,White, T.A.,Oberthuer, D.,Metz, M.,Yoon, C.H.,Barty, A.,Chapman, H.N.,Basu, S.,Coe, J.,Conrad, C.E.,Fromme, R.,Fromme, P.,Tourwe, D.,Schiller, P.W.,Roth, B.L.,Ballet, S.,Katritch, V.,Stevens, R.C.,Cherezov, V.
Structural basis for bifunctional peptide recognition at human delta-opioid receptor.
Nat.Struct.Mol.Biol., 22:265-268, 2015

PubMed Abstract: Bifunctional μ- and δ-opioid receptor (OR) ligands are potential therapeutic alternatives, with diminished side effects, to alkaloid opiate analgesics. We solved the structure of human δ-OR bound to the bifunctional δ-OR antagonist and μ-OR agonist tetrapeptide H-Dmt-Tic-Phe-Phe-NH2 (DIPP-NH2) by serial femtosecond crystallography, revealing a cis-peptide bond between H-Dmt and Tic. The observed receptor-peptide interactions are critical for understanding of the pharmacological profiles of opioid peptides and for development of improved analgesics.

PubMed: 25686086
DOI: 10.1038/nsmb.2965

実験手法

X-RAY DIFFRACTION (2.7 Å)