ArticleAnalytical biochemistry2015
Förster resonance energy transfer-based cholesterolysis assay identifies a novel hedgehog inhibitor.
Article in Analytical biochemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed.
- In vitro reconstitution of vertebrate Sonic Hedgehog protein cholesterolysis.bioRxiv : the preprint server for biology · 2026Article
- Conserved C143 forms a branched intermediate in Hedgehog autoprocessing: A cancer drug discovery target against Hedgehog signaling.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Enzyme fragment complementation driven by nucleic acid hybridization sans self-labeling protein.Bioorganic chemistry · 2025Article
- Enzyme Fragment Complementation Driven by Nucleic Acid Hybridization.bioRxiv : the preprint server for biology · 2023Article
- There's more to enzyme antagonism than inhibition.Bioorganic & medicinal chemistry · 2023Review
- Paracatalytic induction: Subverting specificity in hedgehog protein autoprocessing with small molecules.Methods in enzymology · 2023Article
- Calcimycin InhibitsACS infectious diseases · 2022Article
- Nanomolar, Noncovalent Antagonism of Hedgehog Cholesterolysis: Exception to the "Irreversibility Rule" for Protein Autoprocessing Inhibition.Biochemistry · 2022Article
- Inteins as Drug Targets and Therapeutic Tools.Frontiers in molecular biosciences · 2022Review
- Hedgehog Autoprocessing: From Structural Mechanisms to Drug Discovery.Frontiers in molecular biosciences · 2022Review
- Small-molecule inhibitors for the Prp8 intein as antifungal agents.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Intein Inhibitors as Novel Antimicrobials: Protein Splicing in Human Pathogens, Screening Methods, and Off-Target Considerations.Frontiers in molecular biosciences · 2021Review
- Subverting Hedgehog Protein Autoprocessing by Chemical Induction of Paracatalysis.Biochemistry · 2020Article
- General Base Swap Preserves Activity and Expands Substrate Tolerance in Hedgehog Autoprocessing.Journal of the American Chemical Society · 2019Article
- Protein-Nucleic Acid Conjugation with Sterol Linkers Using Hedgehog Autoprocessing.Bioconjugate chemistry · 2019Article
- Sterol A-ring plasticity in hedgehog protein cholesterolysis supports a primitive substrate selectivity mechanism.Chemical communications (Cambridge, England) · 2019Article
- Chemical Bypass of General Base Catalysis in Hedgehog Protein Cholesterolysis Using a Hyper-Nucleophilic Substrate.Journal of the American Chemical Society · 2018Article
- Hedgehog Proteins Consume Steroidal CYP17A1 Antagonists: Potential Therapeutic Significance in Advanced Prostate Cancer.ChemMedChem · 2016Article
- A Single Aspartate Coordinates Two Catalytic Steps in Hedgehog Autoprocessing.Journal of the American Chemical Society · 2016Article
- Review
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Authors and funding
6 authors.
Funding
Abstract
Hedgehog (Hh) proteins function in cell/cell signaling processes linked to human embryo development and the progression of several types of cancer. Here, we describe an optical assay of hedgehog cholesterolysis, a unique autoprocessing event critical for Hh function. The assay uses a recombinant Förster resonance energy transfer (FRET)-active Hh precursor whose cholesterolysis can be monitored continuously in multi-well plates (dynamic range=4, Z'=0.7), offering advantages in throughput over conventional sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) assays. Application of the optical assay in a pilot small molecule screen produced a novel cholesterolysis inhibitor (apparent IC50=5×10(-6)M) that appears to inactivate hedgehog covalently by a substitution nucleophilic aromatic (SNAr) mechanism.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.