ArticleJournal of lipids2011
Potent inhibition of Acid ceramidase by novel B-13 analogues.
Article in Journal of lipids, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
11 citing papers in PubMed, 27 citations in OpenAlex.
- Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors.Journal of medicinal chemistry · 2020Article
- Sphingolipid Metabolism in Glioblastoma and Metastatic Brain Tumors: A Review of Sphingomyelinases and Sphingosine-1-Phosphate.Biomolecules · 2020Review
- Antineoplastic Agents Targeting Sphingolipid Pathways.Frontiers in oncology · 2020Review
- Ceramide-induced BOK promotes mitochondrial fission in preeclampsia.Cell death & disease · 2018Article
- Comparison of a ceramidase inhibitor (ceranib-2) with C2 ceramide and cisplatin on cytotoxicity and apoptosis of glioma cells.Turkish journal of biology = Turk biyoloji dergisi · 2018Article
- Fragment-Based Hologram QSAR Studies on a Series of 2,4-Dioxopyrimidine-1-Carboxamides As Highly Potent Inhibitors of Acid Ceramidase.Iranian journal of pharmaceutical research : IJPR · 2016Article
- Induction of apoptosis in prostate cancer cells by the novel ceramidase inhibitor ceranib-2.In vitro cellular & developmental biology. Animal · 2015Article
- Alterations in Spinal Cord Metabolism during Treatment of Neuropathic Pain.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2015Article
- Disruption of sphingolipid metabolism augments ceramide-induced autophagy in preeclampsia.Autophagy · 2015Article
- Benzoxazolone carboxamides: potent and systemically active inhibitors of intracellular acid ceramidase.Angewandte Chemie (International ed. in English) · 2015Article
- Regulation of metabolism and transport of sphingosine-1-phosphate in mammalian cells.Molecular and cellular biochemistry · 2012Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The lipid-signalling molecule ceramide is known to induce apoptosis in a variety of cell types. Inhibition of the lysosomal acid ceramidase can increase cellular ceramide levels and thus induce apoptosis. Indeed, inhibitors of acid ceramidase have been reported to induce cell death and to display potentiating effects to classical radio- or chemo therapy in a number of in vitro and in vivo cancer models. The most potent in vitro inhibitor of acid ceramidase, B-13, recently revealed to be virtually inactive towards lysosomal acid ceramidase in living cells. In contrast, a number of weakly basic B-13 analogues have been shown to accumulate in the acidic compartments of living cells and to efficiently inhibit lysosomal acid ceramidase. However, introduction of weakly basic groups at the ω-position of the fatty acid moiety of B-13 led to a significant reduction of potency towards acid ceramidase from cellular extracts. Herein, we report a novel B-13-derived scaffold for more effective inhibitors of acid ceramidase. Furthermore, we provide hints for an introduction of basic functional groups at an alternative site of the B-13 scaffold that do not interfere with acid ceramidase inhibition in vitro.
Identifiers
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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.