Search results for: Harald Hübner

Items from 1 to 20 out of 78 results

article

“Photo‐Adrenalines”: Photoswitchable β₂‐Adrenergic Receptor Agonists as Molecular Probes for the Study of Spatiotemporal Adrenergic Signaling

Alexandra Sink, Hubert Gerwe, Harald Hübner, Valerie Boivin‐Jahns, more

Chemistry – A European Journal > 30 > 11 > n/a - n/a

β₂‐adrenergic receptor (β₂‐AR) agonists are used for the treatment of asthma and chronic obstructive pulmonary disease, but also play a role in other complex disorders including cancer, diabetes and heart diseases. As the cellular and molecular mechanisms in various cells and tissues of the β₂‐AR remain vastly elusive, we developed tools for this investigation with high temporal and spatial resolution...

article

The beer component hordenine inhibits alcohol addiction‐associated behaviours in mice

Yan Li, Christina Vogel, Liubov S. Kalinichenko, Harald Hübner, more

Addiction Biology > 28 > 8 > n/a - n/a

Alcohol consumption is a widespread behaviour that may eventually result in the development of alcohol use disorder (AUD). Alcohol, however, is rarely consumed in pure form but in fruit‐ or corn‐derived preparations, like beer. These preparations add other compounds to the consumption, which may critically modify alcohol intake and AUD risk. We investigated the effects of hordenine, a barley‐derived...

article

Design of Drug Efficacy Guided by Free Energy Simulations of the β₂‐Adrenoceptor

Nicolas Panel, Duc Duy Vo, Nour Aldin Kahlous, Harald Hübner, more

Angewandte Chemie > 135 > 22 > n/a - n/a

G‐protein‐coupled receptors (GPCRs) play important roles in physiological processes and are modulated by drugs that either activate or block signaling. Rational design of the pharmacological efficacy profiles of GPCR ligands could enable the development of more efficient drugs, but is challenging even if high‐resolution receptor structures are available. We performed molecular dynamics simulations...

article

Design of Drug Efficacy Guided by Free Energy Simulations of the β₂‐Adrenoceptor

Nicolas Panel, Duc Duy Vo, Nour Aldin Kahlous, Harald Hübner, more

Angewandte Chemie International Edition > 62 > 22 > n/a - n/a

article

Photochromic Fentanyl Derivatives for Controlled μ‐Opioid Receptor Activation

Ranit Lahmy, Harald Hübner, Maximilian F. Schmidt, Daniel Lachmann, more

Chemistry – A European Journal > 28 > 63 > n/a - n/a

Photoswitchable ligands as biological tools provide an opportunity to explore the kinetics and dynamics of the clinically relevant μ‐opioid receptor. These ligands can potentially activate or deactivate the receptor when desired by using light. Spatial and temporal control of biological activity allows for application in a diverse range of biological investigations. Photoswitchable ligands have been...

article

Structure‐Based Evolution of G Protein‐Biased μ‐Opioid Receptor Agonists

Haoqing Wang, Florian Hetzer, Weijiao Huang, Qianhui Qu, more

Angewandte Chemie International Edition > 61 > 26 > n/a - n/a

The μ‐opioid receptor (μOR) is the major target for opioid analgesics. Activation of μOR initiates signaling through G protein pathways as well as through β‐arrestin recruitment. μOR agonists that are biased towards G protein signaling pathways demonstrate diminished side effects. PZM21, discovered by computational docking, is a G protein biased μOR agonist. Here we report the cryoEM structure of...

article

Strukturbasierte Entwicklung von G‐Protein bevorzugenden μ‐Opioidrezeptor Agonisten

Haoqing Wang, Florian Hetzer, Weijiao Huang, Qianhui Qu, more

Angewandte Chemie > 134 > 26 > n/a - n/a

Der μ‐Opioidrezeptor (μOR) ist das Haupt‐Angriffsziel für opioide Analgetika. Die Aktivierung des μORs initiiert die Signaltransduktion über G‐Protein‐vermittelte Wege und durch β‐Arrestin‐Rekrutierung. μOR‐Agonisten, die bevorzugt die G‐Protein‐vermittelte Signalübertragung aktivieren, weisen deutlich geringere Nebenwirkungen auf. Der Wirkstoff PZM21, welcher durch computergestütztes Docking entdeckt...

article

Inside Back Cover: Selective and Wash‐Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single‐Molecule Imaging of μ‐Opioid Receptor Dimerization (Angew. Chem. Int. Ed. 15/2020)

Christian Gentzsch, Kerstin Seier, Antonios Drakopoulos, Marie‐Lise Jobin, more

Angewandte Chemie International Edition > 59 > 15 > 6289 - 6289

Highly selective fluorescent ligands derived from the opium poppy were developed by D. Calebiro, M. Decker et al. in their Research Article on page 5958 to investigate whether μ‐opioid receptors (μ‐ORs) can form dimers on the plasma membrane. These compounds exhibit long residence time and high affinity. Applying these chemical tools, single‐molecule microscopy allowed detection of a small fraction...

article

Selective and Wash‐Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single‐Molecule Imaging of μ‐Opioid Receptor Dimerization

Christian Gentzsch, Kerstin Seier, Antonios Drakopoulos, Marie‐Lise Jobin, more

Angewandte Chemie > 132 > 15 > 6014 - 6020

μ‐Opioid receptors (μ‐ORs) play a critical role in the modulation of pain and mediate the effects of the most powerful analgesic drugs. Despite extensive efforts, it remains insufficiently understood how μ‐ORs produce specific effects in living cells. We developed new fluorescent ligands based on the μ‐OR antagonist E‐p‐nitrocinnamoylamino‐dihydrocodeinone (CACO), that display high affinity, long...

article

Selective and Wash‐Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single‐Molecule Imaging of μ‐Opioid Receptor Dimerization

Christian Gentzsch, Kerstin Seier, Antonios Drakopoulos, Marie‐Lise Jobin, more

Angewandte Chemie International Edition > 59 > 15 > 5958 - 5964

article

Innenrücktitelbild: Selective and Wash‐Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single‐Molecule Imaging of μ‐Opioid Receptor Dimerization (Angew. Chem. 15/2020)

Christian Gentzsch, Kerstin Seier, Antonios Drakopoulos, Marie‐Lise Jobin, more

Angewandte Chemie > 132 > 15 > 6348 - 6348

Hochselektive fluoreszierende Liganden abgeleitet aus dem Schlafmohn, wurden von D. Calebiro, M. Decker et al. in ihrem Forschungsartikel auf S. 6014 entwickelt, um zu untersuchen, ob μ‐Opioidrezeptoren (μ‐ORs) Dimere auf der Plasmamembran bilden können. Die Verbindungen weisen eine lange Verweilzeit und hohe Affinität auf, und eine kleine Fraktion kurzlebiger Homodimere konnte mithilfe dieser chemischen...

article

Perquinolines A–C: Unprecedented Bacterial Tetrahydroisoquinolines Involving an Intriguing Biosynthesis

Yuriy Rebets, Suvd Nadmid, Constanze Paulus, Charlotte Dahlem, more

Angewandte Chemie International Edition > 58 > 37 > 12930 - 12934

Metabolic profiling of Streptomyces sp. IB2014/016‐6 led to the identification of three new tetrahydroisoquinoline natural products, perquinolines A–C (1–3). Labelled precursor feeding studies and the cloning of the pqr biosynthetic gene cluster revealed that 1–3 are assembled by the action of several unusual enzymes. The biosynthesis starts with the condensation of succinyl‐CoA and l‐phenylalanine...

article

Perquinoline A–C: neuartige bakterielle Tetrahydroisochinoline mit einer bemerkenswerten Biosynthese

Yuriy Rebets, Suvd Nadmid, Constanze Paulus, Charlotte Dahlem, more

Angewandte Chemie > 131 > 37 > 13063 - 13068

Die Analyse des metabolischen Profils von Streptomyces sp. IB2014/ 016‐6 führte zur Identifizierung der drei neuen Tetrahydroisochinolin‐Naturstoffe Perquinoline A–C (1–3). Durch Fütterungsexperimente mit angereicherten Vorläuferverbindungen und Klonen des pqr‐Biosynthesegenclusters wurde entdeckt, dass 1–3 unter Wirkung einiger ungewöhnlicher Enzyme synthetisiert werden. Die Biosynthese startet mit...

article

Structure-based exploration of an allosteric binding pocket in the NTS1 receptor using bitopic NT(8-13) derivatives and molecular dynamics simulations

Ralf Christian Kling, Carolin Burchardt, Jürgen Einsiedel, Harald Hübner, more

Journal of Molecular Modeling > 2019 > 25 > 7 > 1-10

Crystal structures of neurotensin receptor subtype 1 (NTS1) allowed us to visualize the binding mode of the endogenous peptide hormone neurotensin and its pharmacologically active C-terminal fragment NT(8-13) within the orthosteric binding pocket of NTS1. Beneath the orthosteric binding pocket, we detected a cavity that exhibits different sequences in the neurotensin receptor subtypes NTS1 and NTS2...

article

β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation

Barbara Männel, Harald Hübner, Dorothée Möller, Peter Gmeiner

Bioorganic & Medicinal Chemistry > 2017 > 25 > 20 > 5613-5628

β-Arrestin biased G protein-coupled receptor ligands represent important molecular probes and may increase favorable drug action and safety as novel therapeutics. Starting from recently discovered hydroxy-substituted heterocyclic piperazine scaffolds, we have developed a series of dopamine D₂ receptor ligands with a pyrazolo[1,5-a]pyridine as secondary pharmacophore that is functionalized in position...

article

Potent haloperidol derivatives covalently binding to the dopamine D2 receptor

Tobias Schwalbe, Jonas Kaindl, Harald Hübner, Peter Gmeiner

Bioorganic & Medicinal Chemistry > 2017 > 25 > 19 > 5084-5094

The dopamine D₂ receptor (D₂R) is a common drug target for the treatment of a variety of neurological disorders including schizophrenia. Structure based design of subtype selective D₂R antagonists requires high resolution crystal structures of the receptor and pharmacological tools promoting a better understanding of the protein-ligand interactions. Recently, we reported the development of a chemically...

article

Photochromic Dopamine Receptor Ligands Based on Dithienylethenes and Fulgides

Daniel Lachmann, Carolin Studte, Barbara Männel, Harald Hübner, more

Chemistry – A European Journal > 23 > 54 > 13423 - 13434

We describe the incorporation of the well‐investigated class of photochromic dithienylethenes (DTEs) and fulgides into known dopamine receptor ligands such as 1,4‐disubstituted aromatic and hydroxybenzoxazinone piperazines as well as aminoindanes. Subtype and functional selective photochromic ligands were obtained and characterized by NMR and UV/VIS spectroscopic measurements. The photophysical properties...

article

Development of molecular tools based on the dopamine D3 receptor ligand FAUC 329 showing inhibiting effects on drug and food maintained behavior

Anne Stößel, Regine Brox, Nirupam Purkayastha, Harald Hübner, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 13 > 3491-3499

Dopamine D₃ receptor-mediated networks have been associated with a wide range of neuropsychiatric diseases, drug addiction and food maintained behavior, which makes D₃ a highly promising biological target. The previously described dopamine D₃ receptor ligand FAUC 329 (1) showed protective effects against dopamine depletion in a MPTP mouse model of Parkinson’s disease. We used the radioligand [¹⁸F]2,...

article

NTS2-selective neurotensin mimetics with tetrahydrofuran amino acids

Nadja A. Simeth, Manuel Bause, Michael Dobmeier, Ralf C. Kling, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 1 > 350-359

Stimulation of the NTS2 neurotensin receptor causes antipsychotic effects and leads to a promotion of the μ-opioid-independent antinociception, which is important in the modulation of tonic pain sensitivity. We report the synthesis and properties of a small library of peptidic agonists based on the active neurotensin fragment NT(8–13). Two tetrahydrofuran amino acid derivatives were synthesized to...

article

Dibenzo[b,f][1,4]oxazepines and dibenzo[b,e]oxepines: Influence of the chlorine substitution pattern on the pharmacology at the H1R, H4R, 5-HT2AR and other selected GPCRs

Franziska Naporra, Susanne Gobleder, Hans-Joachim Wittmann, Julia Spindler, more

Pharmacological Research > 2016 > 113 > PA > 610-625

Inspired by VUF6884 (7-Chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine), reported as a dual H₁/H₄ receptor ligand (pK_i: 8.11 (human H₁R (hH₁R)), 7.55 (human H₄R (hH₄R))), four known and 28 new oxazepine and related oxepine derivatives were synthesised and pharmacologically characterized at histamine receptors and selected aminergic GPCRs. In contrast to the oxazepine series, within the...

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INFONA - science communication portal

Search results for: Harald Hübner

“Photo‐Adrenalines”: Photoswitchable β₂‐Adrenergic Receptor Agonists as Molecular Probes for the Study of Spatiotemporal Adrenergic Signaling

The beer component hordenine inhibits alcohol addiction‐associated behaviours in mice

Design of Drug Efficacy Guided by Free Energy Simulations of the β₂‐Adrenoceptor

Design of Drug Efficacy Guided by Free Energy Simulations of the β₂‐Adrenoceptor

Photochromic Fentanyl Derivatives for Controlled μ‐Opioid Receptor Activation

Structure‐Based Evolution of G Protein‐Biased μ‐Opioid Receptor Agonists

Strukturbasierte Entwicklung von G‐Protein bevorzugenden μ‐Opioidrezeptor Agonisten

Inside Back Cover: Selective and Wash‐Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single‐Molecule Imaging of μ‐Opioid Receptor Dimerization (Angew. Chem. Int. Ed. 15/2020)

Selective and Wash‐Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single‐Molecule Imaging of μ‐Opioid Receptor Dimerization

Selective and Wash‐Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single‐Molecule Imaging of μ‐Opioid Receptor Dimerization

Innenrücktitelbild: Selective and Wash‐Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single‐Molecule Imaging of μ‐Opioid Receptor Dimerization (Angew. Chem. 15/2020)

Perquinolines A–C: Unprecedented Bacterial Tetrahydroisoquinolines Involving an Intriguing Biosynthesis

Perquinoline A–C: neuartige bakterielle Tetrahydroisochinoline mit einer bemerkenswerten Biosynthese

Structure-based exploration of an allosteric binding pocket in the NTS1 receptor using bitopic NT(8-13) derivatives and molecular dynamics simulations

β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation

Potent haloperidol derivatives covalently binding to the dopamine D2 receptor

Photochromic Dopamine Receptor Ligands Based on Dithienylethenes and Fulgides

Development of molecular tools based on the dopamine D3 receptor ligand FAUC 329 showing inhibiting effects on drug and food maintained behavior

NTS2-selective neurotensin mimetics with tetrahydrofuran amino acids

Dibenzo[b,f][1,4]oxazepines and dibenzo[b,e]oxepines: Influence of the chlorine substitution pattern on the pharmacology at the H1R, H4R, 5-HT2AR and other selected GPCRs

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