ArticleNature structural & molecular biology2015
Structural basis for bifunctional peptide recognition at human δ-opioid receptor.
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Article in Nature structural & molecular biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 99 papers.
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99citing papers in PubMed
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Who cites it
99 citing papers in PubMed.
- Atomic, structural and molecular insights into GPCR ligand binding and signalling.Nature reviews. Molecular cell biology · 2026Review
- Structure-guided allosteric modulation of the delta opioid receptor.Nature communications · 2026Article
- Structural and dynamic studies uncover a distinct allosteric modulatory site at the µ-opioid receptor.Nature communications · 2026Article
- Structure-Guided Repurposing of Approved Drugs Identifies Aprepitant and Mavorixafor as Putative δ-Opioid Receptor Agonist Candidates.International journal of molecular sciences · 2026Article
- Trifluoromethylthio and Trifluoromethyl Functionalization of Endomorphin-1 Enhances its Hydrophobicity and Plasma Stability while Preserving its Affinity for the μ-Opioid Receptor.The Journal of organic chemistry · 2026Article
- Structure-based design of an opioid receptor modulator for enhanced morphine analgesia.Science advances · 2026Article
- Advances in Crystallography and Cryo-Electron Microscopy for the Study of Membrane Proteins.Advances in experimental medicine and biology · 2026Review
- Article
- Structural and dynamic studies uncover a distinct allosteric modulatory site at the μ-opioid receptor.bioRxiv : the preprint server for biology · 2025Article
- Supramolecular assembly of novel achatin structurally similar peptide as potential G protein-coupled receptors anticancer ligands: focus on its pseudo-macrocycle nature.Royal Society open science · 2025Article
- Structural insights into full-length human fascin1: a target for cancer treatment.Acta crystallographica. Section F, Structural biology communications · 2025Article
- Structural Determinants of Buprenorphine Partial Agonism at the μ-Opioid Receptor.Journal of chemical information and modeling · 2025Article
- Isolation, Structure Elucidation, and Bioactivity Evaluation of Two Alkaloids FromFood science & nutrition · 2024Article
- Cryo-EM structure of small-molecule agonist bound delta opioid receptor-GNature communications · 2024Article
- Discovery of Novel, Selective, and Nonbasic Agonists for the Kappa-Opioid Receptor Determined by Salvinorin A-Based Virtual Screening.Journal of medicinal chemistry · 2024Article
- G Protein-Coupled Receptor-Ligand Pose and Functional Class Prediction.International journal of molecular sciences · 2024Article
- Identification of 1,3,8-Triazaspiro[4.5]Decane-2,4-Dione Derivatives as a NovelThe Journal of pharmacology and experimental therapeutics · 2024Article
- Indian Shot (Journal of inflammation research · 2024Article
- Chemico-pharmacological evaluations of the dwarf elephant ear (Frontiers in pharmacology · 2024Article
- Descriptive molecular pharmacology of the δ opioid receptor (DOR): A computational study with structural approach.PloS one · 2024Article
39 more citing papers are in PubMed but not listed here.
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Authors and funding
36 authors.
Gustavo FenaltiDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, California, USA.
Nadia A ZatsepinDepartment of Physics, Arizona State University, Tempe, Arizona, USA.
Cecilia Betti1] Department of Chemistry, Vrije Universiteit Brussel, Brussels, Belgium. [2] Department of Bioengineering Sciences, Vrije Universiteit Brussel, Brussels, Belgium.
Patrick Giguere1] National Institute of Mental Health Psychoactive Drug Screening Program, University of North Carolina Chapel Hill Medical School, Chapel Hill, North Carolina, USA. [2] Department of Pharmacology, University of North Carolina Chapel Hill Medical School, Chapel Hill, North Carolina, USA. [3] Division of Chemical Biology and Medicinal Chemistry, University of North Carolina Chapel Hill Medical School, Chapel Hill, North Carolina, USA.
Gye Won HanDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, California, USA.
Andrii IshchenkoDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, California, USA.
Wei LiuDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, California, USA.
Karel Guillemyn1] Department of Chemistry, Vrije Universiteit Brussel, Brussels, Belgium. [2] Department of Bioengineering Sciences, Vrije Universiteit Brussel, Brussels, Belgium.
Haitao ZhangDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, California, USA.
Daniel JamesDepartment of Physics, Arizona State University, Tempe, Arizona, USA.
Dingjie WangDepartment of Physics, Arizona State University, Tempe, Arizona, USA.
Uwe WeierstallDepartment of Physics, Arizona State University, Tempe, Arizona, USA.
John C H SpenceDepartment of Physics, Arizona State University, Tempe, Arizona, USA.
Sébastien BoutetLinac Coherent Light Source, SLAC National Accelerator Laboratory, Menlo Park, California, USA.
Marc MesserschmidtLinac Coherent Light Source, SLAC National Accelerator Laboratory, Menlo Park, California, USA.
Garth J WilliamsLinac Coherent Light Source, SLAC National Accelerator Laboratory, Menlo Park, California, USA.
Cornelius GatiCenter for Free Electron Laser Science, Deutsches Elektronen-Synchrotron (DESY), Hamburg, Germany.
Oleksandr M YefanovCenter for Free Electron Laser Science, Deutsches Elektronen-Synchrotron (DESY), Hamburg, Germany.
Thomas A WhiteCenter for Free Electron Laser Science, Deutsches Elektronen-Synchrotron (DESY), Hamburg, Germany.
Dominik Oberthuer1] Center for Free Electron Laser Science, Deutsches Elektronen-Synchrotron (DESY), Hamburg, Germany. [2] Institute of Biochemistry and Molecular Biology, University of Hamburg, Hamburg, Germany.
Markus Metz1] Center for Free Electron Laser Science, Deutsches Elektronen-Synchrotron (DESY), Hamburg, Germany. [2] Department of Physics, University of Hamburg, Hamburg, Germany.
Chun Hong Yoon1] Center for Free Electron Laser Science, Deutsches Elektronen-Synchrotron (DESY), Hamburg, Germany. [2] European X-ray Free-Electron Laser Facility (XFEL GmbH), Hamburg, Germany.
Anton BartyCenter for Free Electron Laser Science, Deutsches Elektronen-Synchrotron (DESY), Hamburg, Germany.
Henry N Chapman1] Center for Free Electron Laser Science, Deutsches Elektronen-Synchrotron (DESY), Hamburg, Germany. [2] Department of Physics, University of Hamburg, Hamburg, Germany.
Shibom Basu1] Department of Chemistry and Biochemistry, Arizona State University, Tempe, Arizona, USA. [2] Center for Applied Structural Discovery at the Biodesign Institute, Arizona State University, Tempe, Arizona, USA.
Jesse Coe1] Department of Chemistry and Biochemistry, Arizona State University, Tempe, Arizona, USA. [2] Center for Applied Structural Discovery at the Biodesign Institute, Arizona State University, Tempe, Arizona, USA.ORCID 000000025544320X
Chelsie E Conrad1] Department of Chemistry and Biochemistry, Arizona State University, Tempe, Arizona, USA. [2] Center for Applied Structural Discovery at the Biodesign Institute, Arizona State University, Tempe, Arizona, USA.
Raimund Fromme1] Department of Chemistry and Biochemistry, Arizona State University, Tempe, Arizona, USA. [2] Center for Applied Structural Discovery at the Biodesign Institute, Arizona State University, Tempe, Arizona, USA.
Petra Fromme1] Department of Chemistry and Biochemistry, Arizona State University, Tempe, Arizona, USA. [2] Center for Applied Structural Discovery at the Biodesign Institute, Arizona State University, Tempe, Arizona, USA.
Dirk Tourwé1] Department of Chemistry, Vrije Universiteit Brussel, Brussels, Belgium. [2] Department of Bioengineering Sciences, Vrije Universiteit Brussel, Brussels, Belgium.
Peter W SchillerLaboratory of Chemical Biology and Peptide Research, Clinical Research Institute of Montreal, Montreal, Quebec, Canada.
Bryan L Roth1] National Institute of Mental Health Psychoactive Drug Screening Program, University of North Carolina Chapel Hill Medical School, Chapel Hill, North Carolina, USA. [2] Department of Pharmacology, University of North Carolina Chapel Hill Medical School, Chapel Hill, North Carolina, USA. [3] Division of Chemical Biology and Medicinal Chemistry, University of North Carolina Chapel Hill Medical School, Chapel Hill, North Carolina, USA.
Steven Ballet1] Department of Chemistry, Vrije Universiteit Brussel, Brussels, Belgium. [2] Department of Bioengineering Sciences, Vrije Universiteit Brussel, Brussels, Belgium.
Vsevolod KatritchDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, California, USA.
Raymond C StevensDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, California, USA.
Vadim CherezovDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, California, USA.ORCID 0000000252653914
Funding
X-ray Absorption Spectroscopy (XAS) pp.711-759P41GM103393 · NIGMS · STANFORD UNIVERSITY · PI HODGSON, KEITH O · 2012 to 2019
$30.6MProject 3U54GM094618 · NIGMS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI STEVENS, RAYMOND C · 2010 to 2014
$17.1MScreening CoreU19MH082441 · NIMH · UNIV OF NORTH CAROLINA CHAPEL HILL · PI CARON, MARC G., ROTH, BRYAN L. · 2007 to 2016
$15.2MStructure-Function of Opioid ReceptorsP01DA035764 · NIDA · UNIVERSITY OF SOUTHERN CALIFORNIA · PI CHEREZOV, VADIM, ROTH, BRYAN L. · 2014 to 2018
$7.1MCenter for the Rational Design of Membrane Protein CrystallographyU54GM094599 · NIGMS · ARIZONA STATE UNIVERSITY-TEMPE CAMPUS · PI FROMME, PETRA · 2010 to 2014
$6.8MFemtosecond nano-crystallography of membrane proteinsR01GM095583 · NIGMS · ARIZONA STATE UNIVERSITY-TEMPE CAMPUS · PI FROMME, PETRA · 2010 to 2023
$4.3MDiterpines as Selective Kappa Opioid Receptor AgonistsR01DA017204 · NIDA · UNIV OF NORTH CAROLINA CHAPEL HILL · PI ROTH, BRYAN L. · 2003 to 2014
$3.2MDEVELOPMENT OF RECEPTOR-SPECIFIC OPIOID PEPTIDE ANALOGSR01DA004443 · NIDA · CLINICAL RESEARCH INSTITUTE OF MONTREAL · PI SCHILLER, PETER W · 1987 to 2016
$2.0MHT structure determination of GPCRs by LCP serial femtosecond nanocrystallographyR01GM108635 · NIGMS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI CHEREZOV, VADIM · 2014 to 2017
$1.5MRational discovery of new DOR chemotypes to prevent addiction and overdoseR33DA038858 · NIDA · UNIVERSITY OF SOUTHERN CALIFORNIA · PI KATRITCH, VSEVOLOD · 2017 to 2018
$719kDEVELOPMENT OF RECEPTOR SPECIFIC OPIOID PEPTIDE ANALOGSR37DA004443 · NIDA · CLINICAL RESEARCH INSTITUTE OF MONTREAL · PI SCHILLER, PETER W · 1997 to 2003
$621kRational discovery of new DOR chemotypes to prevent addiction and overdoseR21DA038858 · NIDA · UNIVERSITY OF SOUTHERN CALIFORNIA · PI KATRITCH, VSEVOLOD · 2015 to 2016
$410kCIHR MOP-89716NCI NIH HHS Y1-CO-1020NIDA NIH HHS DA-004443NIDA NIH HHS P01 DA035764NIDA NIH HHS R01 DA004443NIDA NIH HHS R01 DA017204NIDA NIH HHS R21 DA038858NIDA NIH HHS R33 DA038858NIDA NIH HHS R37 DA004443NIGMS NIH HHS P41 GM103393NIGMS NIH HHS R01 GM095583NIGMS NIH HHS R01 GM108635NIGMS NIH HHS U54 GM094599NIGMS NIH HHS U54 GM094618NIGMS NIH HHS Y1-GM-1104NIMH NIH HHS U19 MH082441
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.
Indexed as
Binding SitesCrystallography, X-RayHEK293 CellsHumansModels, MolecularOligopeptidesProtein Structure, TertiaryReceptors, Opioid, deltaTetrahydroisoquinolines2',6'-dimethyltyrosyl-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-phenylalanyl-phenylalaninamideOligopeptidesReceptors, Opioid, deltaTetrahydroisoquinolines
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