ArticleACS infectious diseases2016
Design of Selective Substrates and Activity-Based Probes for Hydrolase Important for Pathogenesis 1 (HIP1) from Mycobacterium tuberculosis.
Article in ACS infectious diseases, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed.
- Covalent Inhibitors Targeting Mycobacterial Enzymes: Current Status, Challenges and Future Perspectives.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Discovery of highly potent α-keto ester-based peptidomimetic inhibitors of the Hip1 protease for the treatment ofEuropean journal of medicinal chemistry reports · 2025Article
- Review
- Chemical Probes Review: Choosing the Right Path Towards Pharmacological Targets in Drug Discovery, Challenges and Future Perspectives.Combinatorial chemistry & high throughput screening · 2024Review
- Activity-based protein profiling of serine hydrolases and penicillin-binding proteins inFEMS microbes · 2024Article
- Development of Oxadiazolone Activity-Based Probes Targeting FphE for Specific Detection ofbioRxiv : the preprint server for biology · 2023Article
- Target Identification in Anti-Tuberculosis Drug Discovery.International journal of molecular sciences · 2023Review
- Chemical approaches to unraveling the biology of mycobacteria.Cell chemical biology · 2023Review
- Chemoproteomic Approaches for Unraveling Prokaryotic Biology.Israel journal of chemistry · 2023Article
- Multiplex substrate profiling by mass spectrometry for proteases.Methods in enzymology · 2023Article
- Identification of cell wall synthesis inhibitors active against Mycobacterium tuberculosis by competitive activity-based protein profiling.Cell chemical biology · 2022Article
- Universal Access to Protease Chemiluminescent Probes through Solid-Phase Synthesis.Bioconjugate chemistry · 2021Article
- Chemiluminescent Protease Probe for Rapid, Sensitive, and Inexpensive Detection of LiveACS central science · 2021Article
- Identification of highly selective covalent inhibitors by phage display.Nature biotechnology · 2021Article
- Visualizing the dynamics of tuberculosis pathology using molecular imaging.The Journal of clinical investigation · 2021Review
- From Differential Stains to Next Generation Physiology: Chemical Probes to Visualize Bacterial Cell Structure and Physiology.Molecules (Basel, Switzerland) · 2020Review
- Strategies for Tuning the Selectivity of Chemical Probes that Target Serine Hydrolases.Cell chemical biology · 2020Review
- The Antimalarial Natural Product Salinipostin A Identifies Essential α/β Serine Hydrolases Involved in Lipid Metabolism in P. falciparum Parasites.Cell chemical biology · 2020Article
- Rapid Tuberculosis Diagnosis Using Reporter Enzyme Fluorescence.Journal of clinical microbiology · 2019Article
- Leveraging Peptide Substrate Libraries to Design Inhibitors of Bacterial Lon Protease.ACS chemical biology · 2019Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
Although serine proteases are important mediators of Mycobacterium tuberculosis (Mtb) virulence, there are currently no tools to selectively block or visualize members of this family of enzymes. Selective reporter substrates or activity-based probes (ABPs) could provide a means to monitor infection and response to therapy using imaging methods. Here, we use a combination of substrate selectivity profiling and focused screening to identify optimized reporter substrates and ABPs for the Mtb "Hydrolase important for pathogenesis 1" (Hip1) serine protease. Hip1 is a cell-envelope-associated enzyme with minimal homology to host proteases, making it an ideal target for probe development. We identified substituted 7-amino-4-chloro-3-(2-bromoethoxy)isocoumarins as irreversible inhibitor scaffolds. Furthermore, we used specificity data to generate selective reporter substrates and to further optimize a selective chloroisocoumarin inhibitor. These new reagents are potentially useful in delineating the roles of Hip1 during pathogenesis or as diagnostic imaging tools for specifically monitoring Mtb infections.
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