ArticleACS chemical biology2015
Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.
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 19 papers.
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Who cites it
19 citing papers in PubMed, 47 citations in OpenAlex.
- Antibacterial activity of tamoxifen derivatives against methicillin-resistantFrontiers in pharmacology · 2025Article
- Sustainable Synthesis of Medicinally Important Heterocycles.Mini reviews in medicinal chemistry · 2025Review
- Discovery of new antimicrobial thiophene derivatives with activity against drug-resistant Gram negative-bacteria.Frontiers in pharmacology · 2024Article
- Phospholipase D, a Novel Therapeutic Target Contributes to the Pathogenesis of Neurodegenerative and Neuroimmune Diseases.Analytical cellular pathology (Amsterdam) · 2024Review
- The Link Between the Microbiota and HER2+ Breast Cancer: The New Challenge of Precision Medicine.Frontiers in oncology · 2022Review
- Repurposing of the Tamoxifen Metabolites to Treat Methicillin-Resistant Staphylococcus epidermidis and Vancomycin-Resistant Enterococcus faecalis Infections.Microbiology spectrum · 2021Article
- Repurposing of the Tamoxifen Metabolites to Combat Infections by Multidrug-Resistant Gram-Negative Bacilli.Antibiotics (Basel, Switzerland) · 2021Article
- Structure-Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors ofJournal of medicinal chemistry · 2021Article
- Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice.Nature chemical biology · 2020Article
- Human PLD structures enable drug design and characterization of isoenzyme selectivity.Nature chemical biology · 2020Article
- Crystal structure of plant PLDα1 reveals catalytic and regulatory mechanisms of eukaryotic phospholipase D.Cell research · 2020Article
- Druggable Targets in Endocannabinoid Signaling.Advances in experimental medicine and biology · 2020Review
- Phospholipase D and Choline Metabolism.Handbook of experimental pharmacology · 2020Review
- Microbiome-Microbial Metabolome-Cancer Cell Interactions in Breast Cancer-Familiar, but Unexplored.Cells · 2019Review
- Gut bacterial phospholipase Ds support disease-associated metabolism by generating choline.Nature microbiology · 2019Article
- A unique mid-sequence linker used to multimerize the lipid-phosphatidylserine (PS) binding peptide-peptoid hybrid PPS1.European journal of medicinal chemistry · 2017Article
- Targeting phospholipase D in cancer, infection and neurodegenerative disorders.Nature reviews. Drug discovery · 2017Review
- The Chemical Biology of Human Metallo-β-Lactamase Fold Proteins.Trends in biochemical sciences · 2016Review
- Human phospholipase D activity transiently regulates pyrimidine biosynthesis in malignant gliomas.ACS chemical biology · 2015Article
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
Phospholipase D (PLD) hydrolyses cellular lipids to produce the important lipid second messenger phosphatidic acid. A PLD enzyme expressed by Pseudomonas aeruginosa (PldA) has been shown to be important in bacterial infection, and NAPE-PLD has emerged as being key in the synthesis of endocannabinoids. In order to better understand the biology and therapeutic potential of these less explored PLD enzymes, small molecule tools are required. Selective estrogen receptor modulators (SERMs) have been previously shown to inhibit mammalian PLD (PLD1 and PLD2). By targeted screening of a library of SERM analogues, additional parallel synthesis, and evaluation in multiple PLD assays, we discovered a novel desketoraloxifene-based scaffold that inhibited not only the two mammalian PLDs but also structurally divergent PldA and NAPE-PLD. This finding represents an important first step toward the development of small molecules possessing universal inhibition of divergent PLD enzymes to advance the field.
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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.