ArticleACS chemical biology2015
Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival.
Article in ACS chemical biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
29 citing papers in PubMed, 52 citations in OpenAlex.
- ThermoTargetMiner as a proteome integral solubility alteration target database for prospective drugs against lung cancer.Communications chemistry · 2026Article
- Lipid Metabolism-Driven CNS Repair via Targeted EV Delivery of PAF to Neurons.Journal of extracellular vesicles · 2026Article
- Regioselective and site-divergent synthesis of tetrahydropyridines by controlled reductive-oxidative dearomative hydroarylation of pyridinium salts.Nature communications · 2025Article
- Fenugreek inhibits cathepsin G activity and suppresses the progression of malignant phenotypes in MCF-7 cells.Biochemistry and biophysics reports · 2025Article
- Unlocking Platelet Mechanisms through Multi-omics Integration: A Brief Review.Current cardiology reviews · 2025Review
- Unveiling the role of Pafah1b3 in liver fibrosis: A novel mechanism revealed.Journal of pharmaceutical analysis · 2025Article
- Activity-based protein profiling of human andiScience · 2022Article
- Article
- Prognostic significance of esterase gene expression in multiple myeloma.British journal of cancer · 2021Article
- Identification of PAFAH1B3 as Candidate Prognosis Marker and Potential Therapeutic Target for Hepatocellular Carcinoma.Frontiers in oncology · 2021Article
- Aberrant Expression of PAFAH1B3 Affects Proliferation and Apoptosis in Osteosarcoma.Frontiers in oncology · 2021Article
- MicroRNA-212-5p and its target PAFAH1B2 suppress vascular proliferation and contraction via the downregulation of RhoA.PloS one · 2021Article
- PAFAH1B3 Expression Is Correlated With Gastric Cancer Cell Proliferation and Immune Infiltration.Frontiers in oncology · 2021Article
- High-Resolution Confocal Fluorescence Imaging of Serine Hydrolase Activity in Cryosections - Application to Glioma Brain Unveils Activity Hotspots Originating from Tumor-Associated Neutrophils.Biological procedures online · 2020Article
- Aberrant expression of PAFAH1B3 associates with poor prognosis and affects proliferation and aggressiveness in hypopharyngeal squamous cell carcinoma.OncoTargets and therapy · 2019Article
- Chemoproteomic Discovery of a Ritanserin-Targeted Kinase Network Mediating Apoptotic Cell Death of Lung Tumor Cells.Molecular pharmacology · 2018Article
- In vivo RNAi screening identifiesBlood advances · 2018Article
- Isoform-selective activity-based profiling of ERK signaling.Chemical science · 2018Article
- Deconstructing Lipid Kinase Inhibitors by Chemical Proteomics.Biochemistry · 2018Article
- The Ligand Binding Landscape of Diacylglycerol Kinases.Cell chemical biology · 2017Article
Corrections and comments
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Authors and funding
19 authors at 2 institutions in 1 country.
Funding
Abstract
Platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3 are poorly characterized serine hydrolases that form a complex with a noncatalytic protein (1b1) to regulate brain development, spermatogenesis, and cancer pathogenesis. Determining physiological substrates and biochemical functions for the PAFAH1b complex would benefit from selective chemical probes that can perturb its activity in living systems. Here, we report a class of tetrahydropyridine reversible inhibitors of PAFAH1b2/3 discovered using a fluorescence polarization-activity-based protein profiling (fluopol-ABPP) screen of the NIH 300,000+ compound library. The most potent of these agents, P11, exhibited IC50 values of ∼40 and 900 nM for PAFAH1b2 and 1b3, respectively. We confirm selective inhibition of PAFAH1b2/3 in cancer cells by P11 using an ABPP protocol adapted for in situ analysis of reversible inhibitors and show that this compound impairs tumor cell survival, supporting a role for PAFAH1b2/3 in cancer.
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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.