TY - JOUR
AU - Fenalti, Gustavo
AU - Zatsepin, Nadia A
AU - Betti, Cecilia
AU - Giguere, Patrick
AU - Han, Gye Won
AU - Ishchenko, Andrii
AU - Liu, Wei
AU - Guillemyn, Karel
AU - Zhang, Haitao
AU - James, Daniel
AU - Wang, Dingjie
AU - Weierstall, Uwe
AU - Spence, John C H
AU - Boutet, Sébastien
AU - Messerschmidt, Marc
AU - Williams, Garth J
AU - Gati, Cornelius
AU - Yefanov, Oleksandr
AU - White, Thomas
AU - Oberthuer, Dominik
AU - Metz, Markus
AU - Yoon, Chun Hong
AU - Barty, Anton
AU - Chapman, Henry N.
AU - Basu, Shibom
AU - Coe, Jesse
AU - Conrad, Chelsie E
AU - Fromme, Raimund
AU - Fromme, Petra
AU - Tourwé, Dirk
AU - Schiller, Peter W
AU - Roth, Bryan L
AU - Ballet, Steven
AU - Katritch, Vsevolod
AU - Stevens, Raymond C
AU - Cherezov, Vadim
TI - Structural basis for bifunctional peptide recognition at human δ-opioid receptor
JO - Nature structural & molecular biology
VL - 22
IS - 3
SN - 1545-9985
CY - London [u.a.]
PB - Nature Publishing Group
M1 - PUBDB-2016-00256
SP - 265 - 268
PY - 2015
N1 - (c) Nature America, Inc.
AB - 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.
LB - PUB:(DE-HGF)16
UR - <Go to ISI:>//WOS:000350531000017
C6 - pmid:25686086
DO - DOI:10.1038/nsmb.2965
UR - https://bib-pubdb1.desy.de/record/293073
ER -