Hannes Schihada

Subcellular pharmacology of a novel cell-permeable fluorescent phosphodiesterase inhibitor using advanced fluorescence microscopy

Soumyabrata Banik, Mchele Anselmi, Jagannath Satpathy, Pier Giorgio Cozzi et autres

Abstract Direct visualisation of drug–target engagement within living cells remains a major challenge. Here we develop a cell-permeable fluorogenic analogue of the phosphodiesterase 4 (PDE4) inhibitor rolipram (MAN193), generated by conjugation to fluorescein diacetate. Following intracellular activation, the probe functions as a …

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Competitive antagonists of the Parathyroid Hormone Receptor 1 identified through docking calculations to an inactive receptor conformation

Jonas Kammertöns, Stefania Monteleone, Andreas M. Kany, Hannes Schihada et autres

Making use of the first published X-ray structure of the Parathyroid Hormone 1 Receptor, we employed small-molecule docking calculations in order to identify novel ligands. Besides directly using the experimental structure, we also generated several models through homology modeling or by reverting …

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GPR3 Ligands Discovered through Combined Virtual and Conformational Biosensor-Based Screening

Hannes Schihada, Aida Shahraki, Ainoleena Turku, Maximilian Rath et autres

GPR3 belongs to the protein superfamily of G protein-coupled receptors (GPCRs) and plays a central role in both benign and malignant physiological processes, such as energy expenditure in adipocytes and Alzheimer’s disease pathology, respectively. Despite the therapeutic potential of both receptor agonists …

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Erratum: BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells.

Adeline Cœugnet, Hannes Schihada, Estelle Rascol, Isabel Alves et autres

This corrects the article 10.3791/68463.

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Functional diversity of GPCR-Gustducin complexes controls signaling output and suppresses alternative pathways

Victoria Jaime Arce, Mona Stefanie Toegl, Santiago Javier Bonn Garcia, Isabell Kaczmarek et autres

Abstract Gustducin (G gust ), the G protein mediating taste receptor signaling, is expressed not only in sensory taste cells but throughout the human body alongside numerous non-taste G protein-coupled receptors (GPCRs). Whether and how these receptors engage G gust , and …

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BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells

Adeline Cœugnet, Hannes Schihada, Estelle Rascol, Isabel D. Alves et autres

G protein-coupled receptors (GPCRs) constitute the largest family of transmembrane receptors, playing a crucial role in cellular signaling by transducing extracellular stimuli into intracellular responses. GPCR activation leads to conformational changes that enable interactions with heterotrimeric G proteins. Upon activation, the Gα …

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Author Correction: In vivo measurement of an Apelin gradient with a genetically encoded APLNR conformation biosensor

Lukas Herdt, Hannes Schihada, Michael E. Kurz, Sebastian Ernst et autres

Author notes These authors contributed equally: Lukas Herdt, Hannes Schihada. Authors and Affiliations Department of Biology, Animal Cell Biology, Marburg University, Marburg, Germany Lukas Herdt, Jean Eberlein & Christian S. M. Helker Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, Marburg University, Marburg, …

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In vivo measurement of an Apelin gradient with a genetically encoded APLNR conformation biosensor

Lukas Herdt, Hannes Schihada, Michael E. Kurz, Sebastian Ernst et autres

The Apelin receptor (APLNR), a class A G-protein coupled receptor, plays a crucial role during cardiovascular development and tumor angiogenesis. To understand its spatiotemporal activity in health and disease is fundamental for the development of drugs to manipulate its activation state. To …

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Cyclic peptide inhibitors function as molecular glues to stabilize Gq/11 heterotrimers

Jonas Mühle, Judith Alenfelder, Matthew J. Rodrigues, Lars Jürgenliemke et autres

Heterotrimeric Gα:Gβγ G proteins function as molecular switches downstream of G protein–coupled receptors (GPCRs). They alternate between a heterotrimeric GDP-bound OFF-state and a GTP-bound ON-state in which Gα GTP is separated from the Gβγ dimer. Consequently, pharmacological tools to securely prevent the …

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Complex G-protein signaling of the adhesion GPCR, ADGRA3

Hannes Schihada, Anna L. Walser, Anna Katarzyna Drzazga, Lukas Grätz et autres

ADGRA3 (GPR125) is an orphan adhesion G protein-coupled receptor (aGPCR) involved in planar cell polarity, primarily through recruitment of the signaling components disheveled (DVL) during vertebrate gastrulation and discs large homolog 1, implicated in cancer. Limited knowledge exists of the canonical G …

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Glue-Tiful Inhibitors: Cyclic Depsipeptides Enhance Protein-Protein Interaction within the Subunits of Heterotrimeric Gq/11 Proteins (Abstract ID: 164994)

Lars Juergenliemke, Judith Alenfelder, Hannes Schihada, Jonas Mühle et autres

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ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system

Necla Birgül İyison, Clauda Abboud, Dayana Abboud, Abdulrasheed O. Abdulrahman et autres

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