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Article

Preferential Coupling of Dopamine D2S and D2L Receptor Isoforms with Gi1 and Gi2 Proteins—In Silico Study

1
Department of Synthesis and Chemical Technology of Pharmaceutical Substances with Computer Modeling Laboratory, Faculty of Pharmacy, Medical University of Lublin, 4A Chodzki St., PL-20093 Lublin, Poland
2
School of Pharmacy, University of Eastern Finland, Yliopistonranta 1, P.O. Box 1627, FI-70211 Kuopio, Finland
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(2), 436; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21020436
Received: 2 December 2019 / Revised: 31 December 2019 / Accepted: 6 January 2020 / Published: 9 January 2020
(This article belongs to the Special Issue Computer Simulation on Membrane Receptors)
The dopamine D2 receptor belongs to rhodopsin-like G protein-coupled receptors (GPCRs) and it is an important molecular target for the treatment of many disorders, including schizophrenia and Parkinson’s disease. Here, computational methods were used to construct the full models of the dopamine D2 receptor short (D2S) and long (D2L) isoforms (differing with 29 amino acids insertion in the third intracellular loop, ICL3) and to study their coupling with Gi1 and Gi2 proteins. It was found that the D2L isoform preferentially couples with the Gi2 protein and D2S isoform with the Gi1 protein, which is in accordance with experimental data. Our findings give mechanistic insight into the interplay between isoforms of dopamine D2 receptors and Gi proteins subtypes, which is important to understand signaling by these receptors and their mediation by pharmaceuticals, in particular psychotic and antipsychotic agents. View Full-Text
Keywords: dopamine D2 receptor; GPCRs; molecular dynamics; molecular switches; principal component analysis dopamine D2 receptor; GPCRs; molecular dynamics; molecular switches; principal component analysis
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MDPI and ACS Style

Żuk, J.; Bartuzi, D.; Matosiuk, D.; Kaczor, A.A. Preferential Coupling of Dopamine D2S and D2L Receptor Isoforms with Gi1 and Gi2 Proteins—In Silico Study. Int. J. Mol. Sci. 2020, 21, 436. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21020436

AMA Style

Żuk J, Bartuzi D, Matosiuk D, Kaczor AA. Preferential Coupling of Dopamine D2S and D2L Receptor Isoforms with Gi1 and Gi2 Proteins—In Silico Study. International Journal of Molecular Sciences. 2020; 21(2):436. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21020436

Chicago/Turabian Style

Żuk, Justyna, Damian Bartuzi, Dariusz Matosiuk, and Agnieszka A. Kaczor 2020. "Preferential Coupling of Dopamine D2S and D2L Receptor Isoforms with Gi1 and Gi2 Proteins—In Silico Study" International Journal of Molecular Sciences 21, no. 2: 436. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21020436

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