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February 1, 2002Journal of Biological ChemistryOpen Access

Constitutive Internalization of Constitutively Active Angiotensin II AT1A Receptor Mutants Is Blocked by Inverse Agonists

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Population

Cells expressing fluorescently tagged N111A, I245T, and L305Q mutants of the angiotensin II AT1A receptor…

Comparison

Losartan (inverse agonist) incubation for 2 hours vs Absence of ligand and wild-type AT1A receptor

Design

Preclinical

Authors

SMStéphanie Miserey‐LenkeiCentre National de la Recherche ScientifiqueCPCharles ParnotCentre National de la Recherche ScientifiqueSBSabine BardinInstitut Curie

Discussion

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Implication

Losartan may alter AT1A trafficking in mutants; leaves open relevance to human cardiovascular therapy.

Structured PICO

P
Population
Cells expressing fluorescently tagged N111A, I245T, and L305Q mutants of the angiotensin II AT1A receptor, and H295 human adrenocortical cell line
I
Intervention
Losartan (inverse agonist) incubation for 2 hours
C
Comparator
Absence of ligand and wild-type AT1A receptor
O
Outcome
Cellular localization and internalization/externalization of the AT1A receptor mutantssurrogate

Constitutively active mutants of the angiotensin II AT1A receptor are permanently internalized and recycled, a process that can be blocked by inverse agonists like losartan.

Cite This Study

Miserey‐Lenkei et al. (2002) studied this question.

synapsesocial.com/papers/6a6f779a75498292b708dc05https://doi.org/10.1074/jbc.m108398200
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  1. 1A Functional Enhanced Green Fluorescent Protein (EGFP)-Tagged Angiotensin II AT<sub>1A</sub>Receptor Recruits the Endogenous Gαq/11 Protein to the Membrane and Induces Its Specific Internalization Independently of Receptor- G Protein Coupling in HEK-293 Cells2001 · 30 citations
  2. 2Phosphorylation of the Type 1A Angiotensin II Receptor by G Protein-coupled Receptor Kinases and Protein Kinase C1996 · 251 citations
  3. 3Short-term desensitization of the angiotensin II receptor of bovine adrenal glomerulosa cells corresponds to a shift from a high to a low affinity state.1994 · 48 citations
  4. 4Constitutive activation of muscarinic receptors by the G‐protein Gq1995 · 76 citations
  5. 5Constitutive arrestin-mediated desensitization of a human vasopressin receptor mutant associated with nephrogenic diabetes insipidus2000 · 242 citations