Journal Article

PUBDB-2016-00256

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Structural basis for bifunctional peptide recognition at human $\delta$-opioid receptor

Fenalti, G. ; Zatsepin, N. A. ; Betti, C. ; Giguere, P. ; Han, G. W. ; Ishchenko, A. ; Liu, W.Extern* ; Guillemyn, K. ; Zhang, H. ; James, D. ; Wang, D. ; Weierstall, U.>Extern* ; Spence, J. C. H. ; Boutet, S.>Extern* ; Messerschmidt, M.Extern* ; Williams, G. J. ; Gati, C.CFEL* ; Yefanov, O.CFEL*DESY* ; White, T.CFEL*DESY* ; Oberthuer, D.CFEL*>Extern* ; Metz, M.CFEL*>Extern* ; Yoon, C. H.CFEL*DESY* ; Barty, A.CFEL*DESY* ; Chapman, H. N.CFEL*DESY* ; Basu, S. ; Coe, J. ; Conrad, C. E. ; Fromme, R. ; Fromme, P.>Extern* ; Tourwé, D. ; Schiller, P. W. ; Roth, B. L. ; Ballet, S. ; Katritch, V. ; Stevens, R. C. ; Cherezov, V. (Corresponding author)

2015
Nature Publishing Group London [u.a.]

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Please use a persistent id in citations: doi:10.1038/nsmb.2965  doi:10.3204/PUBDB-2016-00256

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.

Note: (c) Nature America, Inc.

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Contributing Institute(s):

1. CFEL-Coherent X-Ray Imaging (FS-CFEL-1)

Research Program(s):

1. 6215 - Soft Matter, Health and Life Sciences (POF3-621) (POF3-621)
2. NANOMEM - Membrane Protein Nanocrystallography (317079) (317079)
3. CUI - Hamburger Zentrum für ultraschnelle Beobachtung (194651731) (194651731)
4. VH-GS-500 - PIER Helmholtz Graduate School (2015_IFV-VH-GS-500) (2015_IFV-VH-GS-500)

Experiment(s):

1. Experiments at CFEL

Appears in the scientific report 2015

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Database coverage:
; ; BIOSIS Previews ; Current Contents - Life Sciences ; IF >= 10 ; JCR ; NCBI Molecular Biology Database ; Nationallizenz ; SCOPUS ; Science Citation Index ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection

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