4.7 Article

Dopamine-induced arrestin recruitment and desensitization of the dopamine D4 receptor is regulated by G protein-coupled receptor kinase-2

Related references

Note: Only part of the references are listed.
Article Chemistry, Medicinal

Highly Potent and Selective Dopamine D4 Receptor Antagonists Potentially Useful for the Treatment of Glioblastoma

Pegi Pavletic et al.

Summary: In this paper, new ligands with high affinity and selectivity for D4R were discovered to better understand its role in GBM. The D4R antagonist 24 and biased ligand 29 showed the most potential and induced a decreased viability of GBM cells. Interestingly, these compounds had a greater effect in reducing cell viability compared to temozolomide, the first-choice chemotherapeutic drug in GBM.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Biochemistry & Molecular Biology

G protein-coupled receptor kinase-2 confers isoform-specific calcium sensitivity to dopamine D2 receptor desensitization

Richard Agren et al.

Summary: The study revealed that there is a difference in Ca2+ sensitivity between the two isoforms of dopamine D-2 receptor (D2LR and D2SR), with the desensitization rate of D2SR being influenced by co-expression of GRK2 and beta-arrestin2. The Ca2+ sensitive desensitization of D2SR appears to be mediated via a GRK2 phosphorylation-dependent mechanism.

FASEB JOURNAL (2021)

Article Multidisciplinary Sciences

New phosphosite-specific antibodies to unravel the role of GRK phosphorylation in dopamine D2 receptor regulation and signaling

Anika Mann et al.

Summary: The study aimed to generate antibodies specific for intracellular D2R phosphorylation sites to investigate the regulation of D2R. By comparing measurements of D2R phosphorylation with other measurements of D2R signaling, the utility of novel phosphosite-specific antibodies in studying D2R regulation and signaling was demonstrated.

SCIENTIFIC REPORTS (2021)

Article Multidisciplinary Sciences

Structural insight into small molecule action on Frizzleds

Pawel Kozielewicz et al.

NATURE COMMUNICATIONS (2020)

Article Biochemistry & Molecular Biology

Cytoplasmic recruitment of Mdm2 as a common characteristic of G protein-coupled receptors that undergo desensitization

Mei Zheng et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2020)

Review Cell Biology

Conformational Basis of G Protein-Coupled Receptor Signaling Versatility

Laura M. Wingler et al.

TRENDS IN CELL BIOLOGY (2020)

Article Biochemistry & Molecular Biology

A Split Luciferase Complementation Assay for the Quantification of β-Arrestin2 Recruitment to Dopamine D2-Like Receptors

Lisa Forster et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

Article Physiology

Dopamine D4receptor subtype activation reduces the rat cardiac parasympathetic discharge

Jose Angel Garcia-Pedraza et al.

PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY (2020)

Article Chemistry, Medicinal

Dopamine D4 Receptor-Selective Compounds Reveal Structure-Activity Relationships that Engender Agonist Efficacy

Thomas M. Keck et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Multidisciplinary Sciences

Ultra-large library docking for discovering new chemotypes

Jiankun Lyu et al.

NATURE (2019)

Article Biochemistry & Molecular Biology

The dopamine D2 receptor can directly recruit and activate GRK2 without G protein activation

Thomas F. Pack et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2018)

Article Chemistry, Medicinal

Return of D4 Dopamine Receptor Antagonists in Drug Discovery

Craig W. Lindsley et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Multidisciplinary Sciences

Key role of the dopamine D4 receptor in the modulation of corticostriatal glutamatergic neurotransmission

Jordi Bonaventura et al.

SCIENCE ADVANCES (2017)

Article Biochemistry & Molecular Biology

NanoLuc Complementation Reporter Optimized for Accurate Measurement of Protein Interactions in Cells

Andrew S. Dixon et al.

ACS CHEMICAL BIOLOGY (2016)

Review Biochemical Research Methods

NanoLuc: A Small Luciferase Is Brightening Up the Field of Bioluminescence

Christopher G. England et al.

BIOCONJUGATE CHEMISTRY (2016)

Article Multidisciplinary Sciences

Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties

Nikhil M. Urs et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2016)

Article Biochemistry & Molecular Biology

Arrestin-dependent but G-protein coupled receptor kinase-independent uncoupling of D2-dopamine receptors

Jeremy Celver et al.

JOURNAL OF NEUROCHEMISTRY (2013)

Review Pharmacology & Pharmacy

The Physiology, Signaling, and Pharmacology of Dopamine Receptors

Jean-Martin Beaulieu et al.

PHARMACOLOGICAL REVIEWS (2011)

Article Cell Biology

Resistance of the dopamine D4 receptor to agonist-induced internalization and degradation

Anneleen Spooren et al.

CELLULAR SIGNALLING (2010)

Article Neurosciences

Arrestin3 Mediates D2 Dopamine Receptor Internalization

Mette Skinbjerg et al.

SYNAPSE (2009)

Article Biochemistry & Molecular Biology

Differential voltage-sensitivity of D2-like dopamine receptors

Kristoffer Sahlholm et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2008)

Article Biochemistry & Molecular Biology

Differential regulation of the dopamine D2 and D3 receptors by G protein-coupled receptor kinases and β-arrestins

KM Kim et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2001)

Article Biochemistry & Molecular Biology

Selective reconstitution of human D4 dopamine receptor variants with Giα subtypes

MA Kazmi et al.

BIOCHEMISTRY (2000)