Structure-Guided Design of G-Protein-Coupled Receptor Polypharmacology.


Journal

Angewandte Chemie (International ed. in English)
ISSN: 1521-3773
Titre abrégé: Angew Chem Int Ed Engl
Pays: Germany
ID NLM: 0370543

Informations de publication

Date de publication:
09 08 2021
Historique:
received: 30 01 2021
pubmed: 28 4 2021
medline: 3 11 2021
entrez: 27 4 2021
Statut: ppublish

Résumé

Many diseases are polygenic and can only be treated efficiently with drugs that modulate multiple targets. However, rational design of compounds with multi-target profiles is rarely pursued because it is considered too difficult, in particular if the drug must enter the central nervous system. Here, a structure-based strategy to identify dual-target ligands of G-protein-coupled receptors is presented. We use this approach to design compounds that both antagonize the A

Identifiants

pubmed: 33904641
doi: 10.1002/anie.202101478
pmc: PMC8456950
doi:

Substances chimiques

Antiparkinson Agents 0
DRD2 protein, human 0
Ligands 0
Receptor, Adenosine A2A 0
Receptors, Dopamine D2 0
Small Molecule Libraries 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

18022-18030

Informations de copyright

© 2021 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH.

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Auteurs

Stefanie Kampen (S)

Science for Life Laboratory, Department of Cell and Molecular Biology, Uppsala University, 75124, Uppsala, Sweden.

Duc Duy Vo (D)

Science for Life Laboratory, Department of Cell and Molecular Biology, Uppsala University, 75124, Uppsala, Sweden.

Xiaoqun Zhang (X)

Department of Clinical Neuroscience, Karolinska Institute, 17177, Stockholm, Sweden.

Nicolas Panel (N)

Science for Life Laboratory, Department of Cell and Molecular Biology, Uppsala University, 75124, Uppsala, Sweden.

Yunting Yang (Y)

Department of Clinical Neuroscience, Karolinska Institute, 17177, Stockholm, Sweden.

Mariama Jaiteh (M)

Science for Life Laboratory, Department of Cell and Molecular Biology, Uppsala University, 75124, Uppsala, Sweden.

Pierre Matricon (P)

Science for Life Laboratory, Department of Cell and Molecular Biology, Uppsala University, 75124, Uppsala, Sweden.

Per Svenningsson (P)

Department of Clinical Neuroscience, Karolinska Institute, 17177, Stockholm, Sweden.

Jose Brea (J)

USEF Screening Platform-BioFarma Research Group, Centre for Research in Molecular Medicine and Chronic Diseases, University of Santiago de Compostela, 15706, Santiago, de Compostela, Spain.

Maria Isabel Loza (MI)

USEF Screening Platform-BioFarma Research Group, Centre for Research in Molecular Medicine and Chronic Diseases, University of Santiago de Compostela, 15706, Santiago, de Compostela, Spain.

Jan Kihlberg (J)

Department of Chemistry-BMC, Uppsala University, 75123, Uppsala, Sweden.

Jens Carlsson (J)

Science for Life Laboratory, Department of Cell and Molecular Biology, Uppsala University, 75124, Uppsala, Sweden.

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Classifications MeSH