ArticleACS chemical biology2013
Proteome-wide reactivity profiling identifies diverse carbamate chemotypes tuned for serine hydrolase inhibition.
Article in ACS chemical biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 papers.
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Who cites it
64 citing papers in PubMed, 130 citations in OpenAlex.
- The biological functions of monoacylglycerol lipase (MAGL) in cancer.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2026Review
- Intrinsic N-Terminal Reactivity and Improved Analysis of DSSO-Carbamate and Carbamate-Based Cross-Linkers.Analytical chemistry · 2026Article
- Article
- Chemical Probes for Investigating the Endocannabinoid System.Current topics in behavioral neurosciences · 2026Review
- Spatially Resolved Mapping of Monoacylglycerol Lipase Activity in the Brain.ACS chemical neuroscience · 2025Article
- Methods for Assessing MAGL Enzymatic Activity: An Extensive Review of Past and Emerging Approaches.International journal of molecular sciences · 2025Review
- Discovery of orally active and serine-targeting covalent inhibitors against hCES2A for ameliorating irinotecan-triggered gut toxicity.Acta pharmaceutica Sinica. B · 2025Article
- Synthesis and evaluation ofSynlett : accounts and rapid communications in synthetic organic chemistry · 2025Article
- Photochemical Functionalization of 4‑Diazoisoquinoline-1,3(2ACS organic & inorganic Au · 2025Article
- Highly Specific Miniaturized Fluorescent Monoacylglycerol Lipase Probes Enable Translational Research.Journal of the American Chemical Society · 2025Article
- A Highly Selective and Versatile Probe Platform for Visualization of Monoacylglycerol Lipase.Angewandte Chemie (International ed. in English) · 2025Article
- Promising Inhibitors of Endocannabinoid Degrading Enzymes Sharing a Carbamate Scaffold.Mini reviews in medicinal chemistry · 2025Review
- Ligand discovery by activity-based protein profiling.Cell chemical biology · 2024Review
- Development of Oxadiazolone Activity-Based Probes Targeting FphE for Specific Detection ofbioRxiv : the preprint server for biology · 2023Article
- Assessing Squarates as Amine-Reactive Probes.Journal of the American Chemical Society · 2023Article
- Spatial Chemoproteomics for Mapping the Active Proteome.Israel journal of chemistry · 2023Article
- Endocannabinoid Degradation Enzyme Inhibitors as Potential Antipsychotics: A Medicinal Chemistry Perspective.Biomedicines · 2023Review
- A protocol to visualize on-target specific drug binding in mammalian tissue with cellular resolution using tissue clearing and click chemistry.STAR protocols · 2022Article
- Chemical Probes to Control and Visualize Lipid Metabolism in the Brain.Accounts of chemical research · 2022Review
- Identification of covalent inhibitors that disrupt M. tuberculosis growth by targeting multiple serine hydrolases involved in lipid metabolism.Cell chemical biology · 2022Article
4 more citing papers are in PubMed but not listed here.
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Serine hydrolases are one of the largest and most diverse enzyme classes in Nature. Inhibitors of serine hydrolases are used to treat many diseases, including obesity, diabetes, cognitive dementia, and bacterial and viral infections. Nonetheless, the majority of the 200+ serine hydrolases in mammals still lack selective inhibitors for their functional characterization. We and others have shown that activated carbamates, through covalent reaction with the conserved serine nucleophile of serine hydrolases, can serve as useful inhibitors for members of this enzyme family. The extent to which carbamates, however, cross-react with other protein classes remains mostly unexplored. Here, we address this problem by investigating the proteome-wide reactivity of a diverse set of activated carbamates in vitro and in vivo, using a combination of competitive and click chemistry (CC)-activity-based protein profiling (ABPP). We identify multiple classes of carbamates, including O-aryl, O-hexafluoroisopropyl (HFIP), and O-N-hydroxysuccinimidyl (NHS) carbamates that react selectively with serine hydrolases across entire mouse tissue proteomes in vivo. We exploit the proteome-wide specificity of HFIP carbamates to create in situ imaging probes for the endocannabinoid hydrolases monoacylglycerol lipase (MAGL) and α-β hydrolase-6 (ABHD6). These findings, taken together, designate the carbamate as a privileged reactive group for serine hydrolases that can accommodate diverse structural modifications to produce inhibitors that display exceptional potency and selectivity across the mammalian proteome.
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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.