ArticleNature chemical biology2009
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
Article in Nature chemical biology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 160 papers.
What it found
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Who cites it
160 citing papers in PubMed, 271 citations in OpenAlex.
- PLD1 and PLD2 promote an immunosuppressive tumor microenvironment via CCL19-dependent macrophage polarization and PD-L1 induction.Experimental & molecular medicine · 2026Article
- Arabidopsis phospholipid modifications mediate cellulase-induced resistance to a fungal peptide antibiotic by imposing cell polarity.The New phytologist · 2026Article
- Development and Evaluation of Indole-Based Phospholipase D Inhibitors for Lung Cancer Immunotherapy.Journal of medicinal chemistry · 2025Article
- PLD1 is a key player in cancer stemness and chemoresistance: Therapeutic targeting of cross-talk between the PI3K/Akt and Wnt/β-catenin pathways.Experimental & molecular medicine · 2024Review
- Research progress of the engagement of inorganic nanomaterials in cancer immunotherapy.Drug delivery · 2022Article
- Inhibition of phospholipase D1 induces immunogenic cell death and potentiates cancer immunotherapy in colorectal cancer.Experimental & molecular medicine · 2022Article
- Upregulated phospholipase D2 expression and activity is related to the metastatic properties of melanoma.Oncology letters · 2022Article
- Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance.ACS medicinal chemistry letters · 2022Article
- PLD1 promotes reactive oxygen species production in vascular smooth muscle cells and injury-induced neointima formation.Biochimica et biophysica acta. Molecular and cell biology of lipids · 2022Article
- Choline-Sigma-1R as an Additional Mechanism for Potentiation of Orexin by Cocaine.International journal of molecular sciences · 2021Article
- Diacylglycerol kinase and phospholipase D inhibitors alter the cellular lipidome and endosomal sorting towards the Golgi apparatus.Cellular and molecular life sciences : CMLS · 2021Article
- Ral GTPases promote breast cancer metastasis by controlling biogenesis and organ targeting of exosomes.eLife · 2021Article
- Phospholipase Signaling in Breast Cancer.Advances in experimental medicine and biology · 2021Review
- Structure and regulation of human phospholipase D.Advances in biological regulation · 2021Review
- Aldolase A and Phospholipase D1 Synergistically Resist Alkylating Agents and Radiation in Lung Cancer.Frontiers in oncology · 2021Article
- Enhancement in Phospholipase D Activity as a New Proposed Molecular Mechanism of Haloperidol-Induced Neurotoxicity.International journal of molecular sciences · 2020Article
- Dopamine receptors in emesis: Molecular mechanisms and potential therapeutic function.Pharmacological research · 2020Review
- Phospholipase D1 inhibition sensitizes glioblastoma to temozolomide and suppresses its tumorigenicity.The Journal of pathology · 2020Article
- Inhibition of phospholipase D2 augments histone deacetylase inhibitor-induced cell death in breast cancer cells.Biological research · 2020Article
- Increased phospholipase D activity contributes to tumorigenesis in prostate cancer cell models.Molecular and cellular biochemistry · 2020Article
100 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
Phospholipase D (PLD) is an essential enzyme responsible for the production of the lipid second messenger phosphatidic acid. Phosphatidic acid participates in both G protein-coupled receptor and receptor tyrosine kinase signal transduction networks. The lack of potent and isoform-selective inhibitors has limited progress in defining the cellular roles of PLD. We used a diversity-oriented synthetic approach and developed a library of PLD inhibitors with considerable pharmacological characterization. Here we report the rigorous evaluation of that library, which contains highly potent inhibitors, including the first isoform-selective PLD inhibitors. Specific members of this series inhibit isoforms with >100-fold selectivity both in vitro and in cells. A subset of inhibitors was shown to block invasiveness in metastatic breast cancer models. These findings demonstrate the power of diversity-oriented synthesis combined with biochemical assays and mass spectrometric lipid profiling of cellular responses to develop the first isoform-selective PLD inhibitors--a new class of antimetastatic agents.
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What OpenQuestion holds
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.