Title |
Structural basis for bifunctional peptide recognition at human δ-opioid receptor
|
---|---|
Published in |
Nature Structural & Molecular Biology, February 2015
|
DOI | 10.1038/nsmb.2965 |
Pubmed ID | |
Authors |
Gustavo Fenalti, Nadia A Zatsepin, Cecilia Betti, Patrick Giguere, Gye Won Han, Andrii Ishchenko, Wei Liu, Karel Guillemyn, Haitao Zhang, Daniel James, Dingjie Wang, Uwe Weierstall, John C H Spence, Sébastien Boutet, Marc Messerschmidt, Garth J Williams, Cornelius Gati, Oleksandr M Yefanov, Thomas A White, Dominik Oberthuer, Markus Metz, Chun Hong Yoon, Anton Barty, Henry N Chapman, Shibom Basu, Jesse Coe, Chelsie E Conrad, Raimund Fromme, Petra Fromme, Dirk Tourwé, Peter W Schiller, Bryan L Roth, Steven Ballet, Vsevolod Katritch, Raymond C Stevens, Vadim Cherezov |
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. |
X Demographics
Geographical breakdown
Country | Count | As % |
---|---|---|
United Kingdom | 2 | 22% |
United States | 1 | 11% |
Russia | 1 | 11% |
Switzerland | 1 | 11% |
Unknown | 4 | 44% |
Demographic breakdown
Type | Count | As % |
---|---|---|
Members of the public | 8 | 89% |
Scientists | 1 | 11% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Spain | 1 | <1% |
United States | 1 | <1% |
Denmark | 1 | <1% |
Canada | 1 | <1% |
Unknown | 184 | 98% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 49 | 26% |
Researcher | 46 | 24% |
Student > Bachelor | 17 | 9% |
Student > Master | 15 | 8% |
Professor > Associate Professor | 11 | 6% |
Other | 27 | 14% |
Unknown | 23 | 12% |
Readers by discipline | Count | As % |
---|---|---|
Biochemistry, Genetics and Molecular Biology | 47 | 25% |
Agricultural and Biological Sciences | 34 | 18% |
Chemistry | 32 | 17% |
Pharmacology, Toxicology and Pharmaceutical Science | 14 | 7% |
Physics and Astronomy | 8 | 4% |
Other | 22 | 12% |
Unknown | 31 | 16% |