ArticleACS chemical neuroscience2010
Engineering a GPCR-ligand pair that simulates the activation of D(2L) by Dopamine.
Article in ACS chemical neuroscience, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 28 citations in OpenAlex.
- Structure-Based Discovery of Mouse Trace Amine-Associated Receptor 5 Antagonists.Journal of chemical information and modeling · 2023Article
- Optical Control of Dopamine D2-like Receptors with Cell-Specific Fast-Relaxing Photoswitches.Journal of the American Chemical Society · 2023Article
- Identification of Novel Dopamine DMolecules (Basel, Switzerland) · 2022Article
- Allosteric modulation of dopamine DPharmacological reports : PR · 2022Article
- Fluorescent ligands for dopamine DScientific reports · 2020Article
- Preferential Coupling of Dopamine DInternational journal of molecular sciences · 2020Article
- A Complete Assessment of Dopamine Receptor- Ligand Interactions through Computational Methods.Molecules (Basel, Switzerland) · 2019Article
- Active-state model of a dopamine D2 receptor-Gαi complex stabilized by aripiprazole-type partial agonists.PloS one · 2014Article
- Development of 7TM receptor-ligand complex models using ligand-biased, semi-empirical helix-bundle repacking in torsion space: application to the agonist interaction of the human dopamine D2 receptor.Journal of computer-aided molecular design · 2013Article
- Investigation of D₂ receptor-agonist interactions using a combination of pharmacophore and receptor homology modeling.ChemMedChem · 2012Article
- Cross-receptor interactions between dopamine D2L and neurotensin NTS1 receptors modulate binding affinities of dopaminergics.ACS chemical neuroscience · 2011Article
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In the past decade, engineered G-protein-coupled receptors activated solely by synthetic ligands (RASSLs) have been implemented as a new means to study neurotransmission, which is controlled by G-protein-coupled receptors in vitro and in vivo. In this study, we report an engineered dopamine receptor D(2L) F390(6.52)W, which is the first identified RASSL for the dopamine receptor family. The mutant receptor is characterized by a disrupted ligand binding and complete loss of efficacy for the endogenous ligand, dopamine, which is putatively due to a sterically induced perturbation of H-bonding with conserved serine residues in TM5. Based on this model, we rationally developed an aminoindane-derived set of agonists. Because these agonists forgo analogous H-bonding functionalities, their binding energy does not depend on the respective interactions. Binding affinity and potency were optimized by ligand modifications bearing molecular appendages that obviously interact with a secondary recognition site provided by four hydrophobic residues in TM2 and TM3. Thus, the ferrocenyl carboxamide 5b (FAUC 185) was identified as a synthetic agonist that is able to stimulate the mutant receptor in a manner similar to that by which endogenous dopamine activates the D(2L) wild-type receptor. The engineered dopamine receptor D(2L) F390(6.52)W in combination with FAUC 185 (5b) provides a new tool to probe GPCR functions selectively in specific cell populations in vitro and in vivo.
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