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A Transmembrane Intracellular Estrogen Receptor Mediates Rapid Cell Signaling
TLDR
It is found that of all G protein–coupled receptors characterized to date, GPR30 is uniquely localized to the endoplasmic reticulum, where it specifically binds estrogen and fluorescent estrogen derivatives.
Virtual and biomolecular screening converge on a selective agonist for GPR30
TLDR
The identification of the first G PR30-specific agonist, G-1 (1), capable of activating GPR30 in a complex environment of classical and new estrogen receptors is described.
Estrogen signaling through the transmembrane G protein-coupled receptor GPR30.
TLDR
An overview of the evidence for the cellular and physiological actions of GPR30 in estrogen-dependent processes and the relationship of G PR30 with classical estrogen receptors is provided.
In vivo Effects of a GPR30 Antagonist
TLDR
In vivo administration of G15 reveals that GPR30 contributes to both uterine and neurological responses initiated by estrogen, and the identification and characterization of a G-1 analog, G15, that binds to G PR30 with high affinity and acts as an antagonist of estrogen signaling through GPR28.
A quantitative fluorimetric assay for the determination of oxidant production by polymorphonuclear leukocytes: its use in the simultaneous fluorimetric assay of cellular activation processes.
TLDR
A fluorimetric assay for the indirect determination of superoxide production during the respiratory burst of stimulated polymorphonuclear leukocytes was described, and was sufficiently sensitive that first-derivative kinetic analysis of the respiratory Burst could be quickly analyzed.
Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity
TLDR
An isosteric G-1 derivative, G36, containing an isopropyl moiety in place of the ethanone moiety is synthesized, demonstrating that G36 shows decreased binding and activation of ERα, while maintaining its antagonist profile towards GPER.
Dysregulated FcepsilonRI signaling and altered Fyn and SHIP activities in Lyn-deficient mast cells.
TLDR
It is confirmed that Lyn(-/-) BMMCs release more beta-hexosaminidase than wild-type BMMC’s following FcepsilonRI cross-linking and shown that multiple mast cell responses to FcePSilonRICrosslinking are slow to initiate in Lyn-deficient mice, but persist far longer than in wild- type cells.
Characterization of a Cdc42 Protein Inhibitor and Its Use as a Molecular Probe*
TLDR
The characterization of a novel Cdc42-selective allosteric inhibitor and a related analog are presented, the use of which will facilitate drug development targeting CDC42-related diseases and molecular pathway studies that involve GTPases.
Hydrogen peroxide-induced injury of cells and its prevention by inhibitors of poly(ADP-ribose) polymerase.
TLDR
In the current studies, inhibition of poly(ADP-ribose) polymerase by 3-aminobenzamide, nicotinamide, or theophylline in cells exposed to lethal concentrations of H2O2 prevented the sequence of events that eventually led to cell lysis--i.e., the decrease in NAD, followed by depletion of ATP, influx of extracellular Ca2+, actin polymerization and, finally, cell death.
Distribution and characterization of estrogen receptor G protein-coupled receptor 30 in the rat central nervous system.
TLDR
A high expression of irGPR30 is shown in the hypothalamic-pituitary axis, hippocampal formation, and brainstem autonomic nuclei; and the activation of GPR30 by G-1 is associated with a mobilization of calcium in dissociated and cultured rat hypothalamic neurons.
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