The membrane glucocorticoid receptor on the pituitary is G protein coupled and interacts with the cytoskeleton

Maier, Christina; Rünzler, Dominik; Kerschner, H.; Schindelar, J.; Grabner, Gottfried; Köhler, Gabriele; Luger, Anton

doi:10.1055/s-2005-862932

Cited by 3 publications

(3 citation statements)

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“…In fact, we previously used portions of trajectories where the steroid was continuously bonded to the ar/R arginine to calculate K D while in the present work, all the trajectory was taken into account to better discriminate the tested molecules. Finally, if we compare the median K D for the two drugs with the best affinity for ACBS to the literature, similar values are found: Dexamethasone has a median K D of 193 nM, and experimental K D for glucocorticoid membrane receptors ligands was estimated at 180 nM (46); vitamin D3 has a K D for its receptor equal to 32 nM (47) which is close to our estimated median K D of 101 nM or 114 nM.…”

Section: Additional Evidence In Favor Of Physiological Relevance For ...supporting

confidence: 84%

In silico pharmacological study of AQP2 inhibition by steroids contextualized to Ménière’s disease treatments

Mom,

Réty,

Mocquet

et al. 2023

Front. Neurol.

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Ménière’s disease (MD) is characterized by an abnormal dilatation of the endolymphatic compartment called endolymphatic hydrops and is associated with fluctuating hearing losses and vertigo. Corticosteroid treatment is typically administered for its anti-inflammatory effects to MD patients. However, we recently described for the first time a direct interaction of two corticosteroids (dexamethasone and cortisol) with human AQP2 which strongly inhibited water fluxes. From these initial studies, we proposed an AQPs Corticosteroids Binding Site (ACBS). In the present work, we tested the interaction of 10 molecules associated to the steroid family for this putative ACBS. We observed a wide diversity of affinity and inhibitory potential of these molecules toward AQP2 and discussed the implications for inner ear physiology. Among the tested compounds, cholecalciferol, calcitriol and oestradiol were the most efficient AQP2 water permeability inhibitors.

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Section: Additional Evidence In Favor Of Physiological Relevance For ...supporting

confidence: 84%

In silico pharmacological study of AQP2 inhibition by steroids contextualized to Ménière’s disease treatments

Mom,

Réty,

Mocquet

et al. 2023

Front. Neurol.

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“…Therefore, FCS can directly measure the mobilities of biomolecules, and it can monitor the average association and dissociation of target labeled with fluorescence probe—which vary with interaction kinetics, complex composition and complex size—in vivo without photobleaching. For example, FCS can be used to detect the clustering of somatostatin receptors [ 59 ] and the binding affinities of glucocorticoids (GC) in different subcellular compartments [ 60 ].…”

Section: Fluorescent Molecular Imaging Approachesmentioning

confidence: 99%

Optical molecular imaging for systems biology: from molecule to organism

Wang

Luo

et al. 2006

Anal Bioanal Chem

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The development of highly efficient analytical methods capable of probing biological systems at system level is an important task that is required in order to meet the requirements of the emerging field of systems biology. Optical molecular imaging (OMI) is a very powerful tool for studying the temporal and spatial dynamics of specific biomolecules and their interactions in real time in vivo. In this article, recent advances in OMI are reviewed extensively, such as the development of molecular probes that make imaging brighter, more stable and more informative (e.g., FPs and semiconductor nanocrystals, also referred to as quantum dots), the development of imaging approaches that provide higher resolution and greater tissue penetration, and applications for measuring biological events from molecule to organism level, including gene expression, protein and subcellular compartment localization, protein activation and interaction, and low-mass molecule dynamics. These advances are of great significance in the field of biological science and could also be applied to disease diagnosis and pharmaceutical screening. Further developments in OMI for systems biology are also proposed.

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“…For example, it is thought that they emanate from a membrane localized GR that may share some structural similarities but is nevertheless distinct from the intracellular receptor . Alternatively, a novel receptor structurally different from the intracellular GR is thought to be responsible for these rapid effects . Furthermore, there are theories that the rapid effects are caused by glucocorticoid‐mediated changes in membrane fluidity that result in alterations in membrane surface topography and viscoelasticity …”

Section: Introductionmentioning

confidence: 99%

Localization and Dynamics of Glucocorticoid Receptor at the Plasma Membrane of Activated Mast Cells

Oppong

Hedde

Sekula-Neuner

et al. 2014

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In addition to their actions in the cell nucleus, glucocorticoids exhibit rapid non-nuclear responses that are mechanistically not well understood. To explain these effects, the localization of a glucocorticoid receptor (GR) expressed in mast cells as a GFP fusion was analyzed after activation of the cells on allergenic lipid arrays. These arrays were produced on glass slides by dip-pen nanolithography (DPN) and total internal reflection (TIRF) microscopy was used to visualize the GR. A rapid glucocorticoid-independent and -dependent recruitment of the GR-GFP to the plasma cell membrane was observed following contact of the cells with the allergenic array. In addition, the mobility of the GR at the membrane was monitored by fluorescence recovery after photobleaching (FRAP) and shown to follow binding kinetics demonstrating interactions of the receptor with membrane-bound factors. Furthermore the recruitment of the GR to the cell membrane was shown to result in a glucocorticoid-mediated increase in Erk phosphorylation. This is evidenced by findings that destruction of the membrane composition of the mast cells by cholesterol depletion impairs the membrane localization of the GR and subsequent glucocorticoid-mediated enhancement of Erk phosphorylation. These results demonstrate a membrane localization and function of the GR in mast cell signaling.

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The membrane glucocorticoid receptor on the pituitary is G protein coupled and interacts with the cytoskeleton

Cited by 3 publications

References 0 publications

In silico pharmacological study of AQP2 inhibition by steroids contextualized to Ménière’s disease treatments

In silico pharmacological study of AQP2 inhibition by steroids contextualized to Ménière’s disease treatments

Optical molecular imaging for systems biology: from molecule to organism

Localization and Dynamics of Glucocorticoid Receptor at the Plasma Membrane of Activated Mast Cells

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