Search Results - "Claff, Tobias"
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Inhibition of cellular RNA methyltransferase abrogates influenza virus capping and replication
Published in Science (American Association for the Advancement of Science) (10-02-2023)“…Orthomyxo- and bunyaviruses steal the 5' cap portion of host RNAs to prime their own transcription in a process called "cap snatching." We report that RNA…”
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Activated microglia nibbling glycosaminoglycans from spinal cord perineural nets: a new mechanism for neuropathic pain
Published in Signal transduction and targeted therapy (22-09-2022)Get full text
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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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Development of an active-site titrant for SARS-CoV-2 main protease as an indispensable tool for evaluating enzyme kinetics
Published in Acta pharmaceutica Sinica. B (01-05-2024)“…A titrant for the SARS-CoV-2 main protease (M ) was developed that enables, for the first time, the exact determination of the concentration of the…”
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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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Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV‑2 Main Protease Inhibitors with High Target Specificity and Low Toxicity
Published in Journal of medicinal chemistry (13-10-2022)“…The continuous spread of SARS-CoV-2 calls for more direct-acting antiviral agents to combat the highly infectious variants. The main protease (Mpro) is an…”
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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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Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV‑2 Main Protease Inhibitors
Published in Journal of medicinal chemistry (22-12-2022)“…The spread of SARS-CoV-2 keeps threatening human life and health, and small-molecule antivirals are in demand. The main protease (Mpro) is an effective and…”
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Nonpeptidic Irreversible Inhibitors of SARS-CoV-2 Main Protease with Potent Antiviral Activity
Published in Journal of medicinal chemistry (12-09-2024)“…SARS-CoV-2 infections pose a high risk for vulnerable patients. In this study, we designed benzoic acid halopyridyl esters bearing a variety of substituents as…”
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Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV‑2 Main Protease Inhibitors as Antiviral Drugs
Published in Journal of medicinal chemistry (13-06-2024)“…Given the crucial role of the main protease (Mpro) in the replication cycle of SARS-CoV-2, this viral cysteine protease constitutes a high-profile drug target…”
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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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Elucidating the active δ-opioid receptor crystal structure with peptide and small-molecule agonists
Published in Science advances (01-11-2019)“…Selective activation of the δ-opioid receptor (DOP) has great potential for the treatment of chronic pain, benefitting from ancillary anxiolytic and…”
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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
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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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Structural Insights into Partial Activation of the Prototypic G Protein-Coupled Adenosine A 2A Receptor
Published in ACS pharmacology & translational science (10-05-2024)“…The adenosine A receptor (A AR) belongs to the rhodopsin-like G protein-coupled receptor (GPCR) family, which constitutes the largest class of GPCRs. Partial…”
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Eine einzige stabilisierende Punktmutation ermöglicht hochaufgelöste Co‐Kristallstrukturen des Adenosin‐A2A‐Rezeptors mit Preladenant‐Konjugaten
Published in Angewandte Chemie (23-05-2022)“…Der G‐Protein‐gekoppelte Adenosin‐A2A‐Rezeptor (A2AAR) stellt eine wichtige neue (potentielle) Arzneistoff‐Zielstruktur für die Immunonkologie und für…”
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Structural Insights into Partial Activation of the Prototypic G Protein-Coupled Adenosine A2A Receptor
Published in ACS pharmacology & translational science (10-05-2024)“…The adenosine A2A receptor (A2AAR) belongs to the rhodopsin-like G protein-coupled receptor (GPCR) family, which constitutes the largest class of GPCRs…”
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