Publications de Rudolf Hovius | EPFL Graph Search

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Background Impaired 5-HT3 receptor function is likely involved in the pathogenesis of functional gastrointestinal disorders (FGID) and 5-HT3 receptor antagonists are effective treatments for chemotherapy-induced nausea and vomiting (CINV) and irritable bow ...

With the reversible sequential (ReSeq) binding assay, we present a novel approach for the ultrasensitive profiling of receptor function in single living cells. This assay is based on the repetitive application of fluorescent ligands that have fast assocn.- ...

Two types of ligand-gated ion channels were expressed with the Semliki Forest virus (SFV) expression system. The cDNAs for mouse serotonin 5-HT3 receptor and rat and human purinoreceptor P2x subtypes were introduced into the pSFV1 vector. In vitro transcribed RNAs were coelectroporated with pSFV-Helper2 RNA into BHK cells, where in vivo packaging resulted in high titer SFV-5-HT3 and SFV-P2x virus stocks. Infection of BHK, CHO, and RIN cells resulted in high-level expression of recombinant receptors. Satn. b

Understanding cellular signaling mediated by cell surface receptors is key to modern biomedical research and drug development. The discovery of a growing no. of potential mol. targets and therapeutic compds. requires downscaling and accelerated functional ...

A serotonin 5-HT3 receptor was functionally expressed to high levels and on a large scale in mammalian cells with the Semliki Forest virus system. Conditions were optimized to maximize detergent solubilization of the receptor, while preserving ligand binding activity. An efficient one-step purifn. yielding .apprx.50% of the histidine-tagged 5-HT3 receptor was achieved with immobilized metal ion chromatog. The expressed receptor, in both membranes and purified prepns., exhibited wild-type ligand binding prop

High signal-to-noise Fourier transform IR (FTIR) spectra of the 5-hydroxytryptamine (serotonin) receptor (5-HT3R) and the nicotinic acetylcholine receptor (nAChR) were obtained by microscope FTIR spectroscopy using micrometer-sized, fully hydrated protein films. Because this novel procedure requires only nanogram quantities of membrane proteins, which is 4-5 orders of magnitude less than the amt. of protein typically used for conventional FTIR spectroscopy, it opens the possibility to access the structure a

The binding of the fluorescein-labeled antagonist GR-flu ([1,2,3,9-tetrahydro-3-[(5-methyl-1H-imidazol-4-yl)methyl]-9-(3-amino- (N-fluoresceinthiocarbamoyl)propyl)-4H-carbazol-4-one]) to a purified, detergent-solubilized ligand-gated ion channel, the type-3 serotonin (5-hydroxytryptamine, 5HT) receptor (5HT3R), was characterized by frequency-domain time-resolved fluorescence spectroscopy (TRFS). Detailed understanding of how ligands interact with the homopentameric receptor was obtained. While a 1:1 stoichi

Human genetic studies have revealed an association between GTP cyclohydrolase 1 polymorphisms, which decrease tetrahydrobiopterin (BH4) levels, and reduced pain in patients. We now show that excessive BH4 is produced in mice by both axotom- ized sensory neurons and macrophages infiltrating damaged nerves and inflamed tissue. Constitutive BH4 overproduction in sensory neurons increases pain sensitivity, whereas blocking BH4 production only in these cells reduces nerve injury-induced hy- persensitivity withou

Chem. and biol. labeling is fundamental for the elucidation of the function of proteins within biochem. cellular networks. In particular, fluorescent probes allow detection of mol. interactions, mobility and conformational changes of proteins in live cells with high temporal and spatial resoln. We present a generic method to label proteins in vivo selectively, rapidly (seconds) and reversibly, with small mol. probes that can have a wide variety of properties. These probes comprise a chromophore and a metal-

A fluorescently labeled ligand for the 5-HT3 serotonin receptor was synthesized and its sub-nanomolar affinity for the purified, detergent solubilized receptor was measured. The change in the ligand's fluorescence upon receptor binding was used to directly measure its dissocn. const. for receptor binding, to det. the pharmacol. of the receptor, and finally to characterize the binding site of the receptor. A total internal reflection fluorescence (TIRF) assay for the 5-HT3 receptor was developed, which is su

The screening of ligands for membrane receptor proteins is central to the discovery of new pharmaceutical drugs. We present a general method to reversibly attach receptor proteins via an affinity tag to a quartz surface and subsequently detect with high sensitivity the real-time binding of ligands by total internal reflection fluorescence. A serotonin-gated ion channel protein was immobilized, and the binding of a fluorescent ligand was investigated. The affinity and the kinetic parameters of binding were m

High-aspect-ratio, monocryst. Cd chloride nanowires doped with fluorescent CdS nanoparticles were synthesized using planar lipid membranes as templates. Cd2+ ions bound to the lipid bilayers (a) are released at low pH to the nanometer-sized, interlamellar ...

We have measured fluorescence resonance energy transfer (FRET) between a fluorescent antagonist, bound to the purified detergent-solubilized serotonin type 3 receptor, and a lipophilic acceptor probe partitioned into the micelle surrounding the detergent-solubilized receptor. The exptl. obsd. FRET efficiency was evaluated on the basis of the characteristic dimensions of the receptor-micelle complex and the av. no. of acceptor mols. in such micelles. The binding site was detd. to be 5.4 +- 0.9 nm above the c

5 HT receptors expressed throughout the human body are targets for established therapeutics and various drugs in development. Their diversity of structure and function reflects the important role 5-HT receptors play in physiologic and pathophysiological pr ...

Neurotransmitter-gated ion channels of the Cys-loop receptor family mediate fast neurotransmission throughout the nervous system. The molecular processes of neurotransmitter binding, subsequent opening of the ion channel and ion permeation remain poorly un ...

The ability of organisms, or individual cells, to react to external chemical signals, which are detected and transduced by cell-surface receptors, is crucial for their survival. These receptors are the targets of the majority of clinically used medicines. Combinatorial genetics can provide almost unlimited numbers of mutant receptor proteins and combinatorial chemistry can produce large libraries of potential therapeutic compounds that act on these membrane receptors. What is missing for the fundamental und

The inner nuclear membrane is functionalized by diverse transmembrane proteins that associate with nuclear lamins and/or chromatin. When cells enter mitosis, membrane-chromatin contacts must be broken to allow for proper chromosome segregation; yet how thi ...

Tryptophan metabolites in the kynurenine pathway are up-regulated by pro-inflammatory cytokines or glucocorticoids, and are linked to anti-inflammatory and immunosuppressive activities. In addition, they are up-regulated in pathologies such as cancer, auto ...

Fluorescence Correlation Spectroscopy (FCS) is a suitable technique to investigate biomol. interactions. The advantage of FCS lies in its wide dynamic range in the time and concn. domain, its sensitivity, and thus in the small amt. of material needed. The characteristic time of the processes that can be measured spans more than eleven orders of magnitude, between several nanoseconds up to hours; the measurable concn. range extends from 0.1 nM to several mM. Here we report on FCS expts. to investigate the pr

A highly-sensitive surface fluorescence technique was combined with a powerful method for the oriented reversible immobilization of membrane proteins on oxide surfaces. Affinity and kinetic parameters of the interaction of the receptor and a fluorescent ligand were evaluated. The approach is particularly suited for the study of rapid ligand-receptor interactions where optimized cell volume, flow and injection conditions are required.

Rudolf Hovius

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Natural compounds boldine and menthol are antagonists of human 5-HT

Reversible sequential-binding probe receptor-ligand interactions in single cells

Expression of ligand-gated ion channels with the Semliki Forest virus expression system

Investigating cellular signaling reactions in single attoliter vesicles

Characterization of a mouse serotonin 5-HT3 receptor purified from mammalian cells

Downscaling Fourier Transform Infrared Spectroscopy to the Micrometer and Nanogram Scale: Secondary Structure of Serotonin and Acetylcholine Receptors

In vitro and in vivo ligand binding to the 5HT3 serotonin receptor characterised by time-resolved fluorescence spectroscopy

Reduction of Neuropathic and Inflammatory Pain through Inhibition of the Tetrahydrobiopterin Pathway

Reversible site-selective labeling of membrane proteins in live cells

Fluorescence techniques for fundamental and applied studies of membrane protein receptors: the 5-HT3 serotonin receptor

Screening Ligands for Membrane Protein Receptors by Total Internal Reflectance Fluorescence: The 5-HT3 Serotonin Receptor

Synthesis of nanoscopic optical fibers using lipid membranes as templates

Mapping the Antagonist Binding Site of the Serotonin Type 3 Receptor by Fluorescence Resonance Energy Transfer

International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function

X-ray structure of the mouse serotonin 5-HT3 receptor

Fluorescence techniques: shedding light on ligand-receptor interactions

Torsin ATPases influence chromatin interaction of the Torsin regulator LAP1

Tetrahydrobiopterin Biosynthesis as a Potential Target of the Kynurenine Pathway Metabolite Xanthurenic Acid

Characterization of a transmembrane receptor protein by fluorescence correlation spectroscopy

Waveguide fluorosensor for the detection of ligand-receptor interactions - The 5-HT3 serotonin receptor