Computational design of constitutively active mutants of Dopamine D2 receptor inspired by ligand-independent activation mechanisms

This study elucidates how CAMs reshape the activation landscape of D2R and establishes a broadly applicable computational-experimental framework for discovering constitutively active GPCR variants. These CAMs provide valuable ligand-independent models for probing receptor activation mechanisms at structural, cellular, and physiological levels.

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Publication Details

Journal
BMC Biology
Published
2026-02-05
DOI
https://doi.org/10.1186/s12915-026-02542-6
Primary Topic
Receptor Mechanisms and Signaling
Type
article
Field-Weighted Citation Impact
0.00
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article

Computational design of constitutively active mutants of Dopamine D2 receptor inspired by ligand-independent activation mechanisms

Lucie Delemotte, Y. Chen, Akshay Naraine, Marcus Saarinen et al.
BMC Biology
Receptor Mechanisms and Signaling
article

Computational design of constitutively active mutants of Dopamine D2 receptor inspired by ligand-independent activation mechanisms

Lucie Delemotte, Y. Chen, Akshay Naraine, Marcus Saarinen, Jörgen Carlsson, Per Svenningsson
article en

Abstract

This study elucidates how CAMs reshape the activation landscape of D2R and establishes a broadly applicable computational-experimental framework for discovering constitutively active GPCR variants. These CAMs provide valuable ligand-independent models for probing receptor activation mechanisms at structural, cellular, and physiological levels.

BMC BiologyVol. 24(1)
Science for Life Laboratory (SE), Karolinska Institutet (SE), KTH Royal Institute of Technology (SE)
Openalex Percentile: Top 67%
Receptor Mechanisms and Signaling
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Computational design of constitutively active mutants of Dopamine D2 receptor inspired by ligand-independent activation mechanisms — Lucie Delemotte, Y. Chen, et al. · BMC Biology (2026) | TGRS Research Map | TGRS