ArticleACS chemical biology2014
Inhibiting AMPylation: a novel screen to identify the first small molecule inhibitors of protein AMPylation.
Article in ACS chemical biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Small-Molecule FICD Inhibitors Suppress Endogenous and Pathologic FICD-Mediated Protein AMPylation.ACS chemical biology · 2025Article
- Small molecule FICD inhibitors suppress endogenous and pathologic FICD-mediated protein AMPylation.bioRxiv : the preprint server for biology · 2024Article
- The AMPylase FIC-1 modulates TGF-β signaling inFrontiers in molecular neuroscience · 2022Article
- Investigation of the Detailed AMPylated Reaction Mechanism for the Huntingtin Yeast-Interacting Protein E Enzyme HYPE.International journal of molecular sciences · 2021Article
- Bacterial virulence mediated by orthogonal post-translational modification.Nature chemical biology · 2020Review
- A Fluorescence Polarization-Based High-Throughput Screen to Identify the First Small-Molecule Modulators of the Human Adenylyltransferase HYPE/FICD.International journal of molecular sciences · 2020Article
- Enzymes Involved in AMPylation and deAMPylation.Chemical reviews · 2018Review
- DNA-Catalyzed Introduction of Azide at Tyrosine for Peptide Modification.Angewandte Chemie (International ed. in English) · 2016Article
- Global Profiling of Huntingtin-associated protein E (HYPE)-Mediated AMPylation through a Chemical Proteomic Approach.Molecular & cellular proteomics : MCP · 2016Article
- High-throughput identification of proteins with AMPylation using self-assembled human protein (NAPPA) microarrays.Nature protocols · 2015Article
- HypE-specific nanobodies as tools to modulate HypE-mediated target AMPylation.The Journal of biological chemistry · 2015Article
- A novel link between Fic (filamentation induced by cAMP)-mediated adenylylation/AMPylation and the unfolded protein response.The Journal of biological chemistry · 2015Article
- Crystal structure of the human, FIC-domain containing protein HYPE and implications for its functions.Structure (London, England : 1993) · 2014Article
- Chemical reporters for exploring ADP-ribosylation and AMPylation at the host-pathogen interface.Current opinion in chemical biology · 2014Review
- HDX-MS guided drug discovery: small molecules and biopharmaceuticals.Current opinion in structural biology · 2014Review
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Authors and funding
9 authors.
Funding
Abstract
Enzymatic transfer of the AMP portion of ATP to substrate proteins has recently been described as an essential mechanism of bacterial infection for several pathogens. The first AMPylator to be discovered, VopS from Vibrio parahemolyticus, catalyzes the transfer of AMP onto the host GTPases Cdc42 and Rac1. Modification of these proteins disrupts downstream signaling events, contributing to cell rounding and apoptosis, and recent studies have suggested that blocking AMPylation may be an effective route to stop infection. To date, however, no small molecule inhibitors have been discovered for any of the AMPylators. Therefore, we developed a fluorescence-polarization-based high-throughput screening assay and used it to discover the first inhibitors of protein AMPylation. Herein we report the discovery of the first small molecule VopS inhibitors (e.g., calmidazolium, GW7647, and MK886) with Ki's ranging from 6 to 50 μM and upward of 30-fold selectivity versus HYPE, the only known human AMPylator.
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