Search Results - "Voss, Jan H."
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Cell‐permeable high‐affinity tracers for Gq proteins provide structural insights, reveal distinct binding kinetics and identify small molecule inhibitors
Published in British journal of pharmacology (01-04-2020)“…Background and Purpose G proteins are intracellular switches that transduce and amplify extracellular signals from GPCRs. The Gq protein subtypes, which are…”
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Irreversible Antagonists for the Adenosine A2B Receptor
Published in Molecules (Basel, Switzerland) (13-06-2022)“…Blockade of the adenosine A2B receptor (A2BAR) represents a potential novel strategy for the immunotherapy of cancer. In the present study, we designed,…”
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Imaging of Gα q Proteins in Mouse and Human Organs and Tissues
Published in Pharmaceutics (24-12-2022)“…G protein-coupled receptors (GPCRs) transfer extracellular signals across cell membranes by activating intracellular heterotrimeric G proteins. Several studies…”
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Structure-affinity and structure-residence time relationships of macrocyclic Gαq protein inhibitors
Published in iScience (21-04-2023)“…The macrocyclic depsipeptides YM-254890 (YM) and FR900359 (FR) are potent inhibitors of Gαq/11 proteins. They are important pharmacological tools and have…”
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Macrocyclic Gq Protein Inhibitors FR900359 and/or YM-254890–Fit for Translation?
Published in ACS pharmacology & translational science (09-04-2021)“…Guanine nucleotide-binding proteins (G proteins) transduce extracellular signals received by G protein-coupled receptors (GPCRs) to intracellular signaling…”
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Crystal structure of adenosine A2A receptor in complex with clinical candidate Etrumadenant reveals unprecedented antagonist interaction
Published in Communications chemistry (01-06-2023)“…The G s protein-coupled adenosine A 2A receptor (A 2A AR) represents an emerging drug target for cancer immunotherapy. The clinical candidate Etrumadenant was…”
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Sensitive LC-MS/MS Method for the Quantification of Macrocyclic Gαq Protein Inhibitors in Biological Samples
Published in Frontiers in chemistry (24-09-2020)“…The cyclic depsipeptide FR900359 (FR) isolated from the plant Ardisia crenata and produced by endosymbiotic bacteria acts as a selective Gq protein inhibitor…”
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Unraveling binding mechanism and kinetics of macrocyclic Gαq protein inhibitors
Published in Pharmacological research (01-11-2021)“…G proteins represent intracellular switches that transduce signals relayed from G protein-coupled receptors. The structurally related macrocyclic depsipeptides…”
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Discovery of Anthranilic Acid Derivatives as Antagonists of the Pro-Inflammatory Orphan G Protein-Coupled Receptor GPR17
Published in Journal of medicinal chemistry (14-11-2024)“…The G protein-coupled receptor 17 (GPR17) is an orphan receptor involved in inflammatory diseases. GPR17 antagonists have been proposed for the treatment of…”
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Single Stabilizing Point Mutation Enables High‐Resolution Co‐Crystal Structures of the Adenosine A2A Receptor with Preladenant Conjugates
Published in Angewandte Chemie International Edition (23-05-2022)“…The G protein‐coupled adenosine A2A receptor (A2AAR) is an important new (potential) drug target in immuno‐oncology, and for neurodegenerative diseases…”
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Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A 2A Receptor with Preladenant Conjugates
Published in Angewandte Chemie International Edition (23-05-2022)“…The G protein-coupled adenosine A receptor (A AR) is an important new (potential) drug target in immuno-oncology, and for neurodegenerative diseases…”
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Class-Wide Analysis of Frizzled-Dishevelled Interactions Using BRET Biosensors Reveals Functional Differences among Receptor Paralogs
Published in ACS sensors (27-09-2024)“…Wingless/Int-1 (WNT) signaling is mediated by WNT binding to 10 Frizzleds (FZD1–10), which propagate the signal inside the cell by interacting with different…”
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Feature-Based Molecular Networking for the Targeted Identification of Gq‑Inhibiting FR900359 Derivatives
Published in Journal of natural products (Washington, D.C.) (23-07-2021)“…Both the soil bacterium Chromobacterium vaccinii and the bacterial endosymbiont Candidatus Burkholderia crenata of the plant Ardisia crenata are producers of…”
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Cell-permeable high-affinity tracers for G q proteins provide structural insights, reveal distinct binding kinetics and identify small molecule inhibitors
Published in British journal of pharmacology (01-04-2020)“…G proteins are intracellular switches that transduce and amplify extracellular signals from GPCRs. The G protein subtypes, which are coupled to PLC activation,…”
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Innentitelbild: Eine einzige stabilisierende Punktmutation ermöglicht hochaufgelöste Co‐Kristallstrukturen des Adenosin‐A2A‐Rezeptors mit Preladenant‐Konjugaten (Angew. Chem. 22/2022)
Published in Angewandte Chemie (23-05-2022)“…Der Adenosin‐A2A‐Rezeptor (A2AAR), der durch das extrazelluläre Nukleosid Adenosin aktiviert wird, gehört zur Familie der G‐Protein‐gekoppelten Rezeptoren…”
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Inside Cover: Single Stabilizing Point Mutation Enables High‐Resolution Co‐Crystal Structures of the Adenosine A2A Receptor with Preladenant Conjugates (Angew. Chem. Int. Ed. 22/2022)
Published in Angewandte Chemie International Edition (23-05-2022)“…The adenosine A2A receptor (A2AAR), which is activated by the extracellular nucleoside adenosine, belongs to the family of G protein‐coupled receptors (GPCRs)…”
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Feature-Based Molecular Networking for the Targeted Identification of G q -Inhibiting FR900359 Derivatives
Published in Journal of natural products (Washington, D.C.) (23-07-2021)Get full text
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Irreversible Antagonists for the Adenosine A 2B Receptor
Published in Molecules (Basel, Switzerland) (13-06-2022)“…Blockade of the adenosine A2B receptor (A2BAR) represents a potential novel strategy for the immunotherapy of cancer. In the present study, we designed,…”
Get full text
Journal Article -
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Crystal structure of adenosine A 2A receptor in complex with clinical candidate Etrumadenant reveals unprecedented antagonist interaction
Published in Communications chemistry (01-06-2023)“…The G protein-coupled adenosine A receptor (A AR) represents an emerging drug target for cancer immunotherapy. The clinical candidate Etrumadenant was…”
Get full text
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