ArticleBioorganic & medicinal chemistry2014
Targeting (cellular) lysosomal acid ceramidase by B13: design, synthesis and evaluation of novel DMG-B13 ester prodrugs.
Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 33 citations in OpenAlex.
- A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid Pathways.Biomolecules · 2025Review
- Therapeutic Potential for Sphingolipids in Inflammatory Bowel Disease and Colorectal Cancer.Cancers · 2024Review
- A Near-Infrared Fluorogenic Probe for Rapid, Specific, and Ultrasensitive Detection of Sphingosine in Living Cells and In Vivo.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Acid Ceramidase Inhibitor LCL-805 Antagonizes Akt Signaling and Promotes Iron-Dependent Cell Death in Acute Myeloid Leukemia.Cancers · 2023Article
- Tumors evade immune cytotoxicity by altering the surface topology of NK cells.Nature immunology · 2023Article
- Targeting Acid Ceramidase Inhibits Glioblastoma Cell Migration through Decreased AKT Signaling.Cells · 2022Article
- Polyploid giant cancer cells are dependent on cholesterol for progeny formation through amitotic division.Scientific reports · 2022Article
- Targeting acid ceramidase ameliorates fibrosis in mouse models of non-alcoholic steatohepatitis.Frontiers in medicine · 2022Article
- Controlling Immunoregulatory Cell Activity for Effective Photodynamic Therapy of Cancer.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Synthesis of erythro- B13 enantiomers and stereospecific action of full set of B13-isomers in MCF7 breast carcinoma cells: Cellular metabolism and effects on sphingolipids.Bioorganic & medicinal chemistry · 2021Article
- Article
- Targeting acid ceramidase inhibits YAP/TAZ signaling to reduce fibrosis in mice.Science translational medicine · 2020Article
- Tamoxifen is a candidate first-in-class inhibitor of acid ceramidase that reduces amitotic division in polyploid giant cancer cells-Unrecognized players in tumorigenesis.Cancer medicine · 2020Article
- Antineoplastic Agents Targeting Sphingolipid Pathways.Frontiers in oncology · 2020Review
- Genetic and pharmacological inhibition of acid ceramidase prevents asymmetric cell division by neosis.Journal of lipid research · 2019Article
- Dose dependent actions of LCL521 on acid ceramidase and key sphingolipid metabolites.Bioorganic & medicinal chemistry · 2018Article
- Molecular Targeting of Acid Ceramidase in Glioblastoma: A Review of Its Role, Potential Treatment, and Challenges.Pharmaceutics · 2018Review
- Interdiction of Sphingolipid Metabolism Revisited: Focus on Prostate Cancer.Advances in cancer research · 2018Review
- Therapeutic implications of bioactive sphingolipids: A focus on colorectal cancer.Cancer biology & therapy · 2017Review
- The emergence of acid ceramidase as a therapeutic target for acute myeloid leukemia.Expert opinion on therapeutic targets · 2017Review
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 1 country.
Funding
Abstract
Acid ceramidase (ACDase) is being recognized as a therapeutic target for cancer. B13 represents a moderate inhibitor of ACDase. The present study concentrates on the lysosomal targeting of B13 via its N,N-dimethylglycine (DMG) esters (DMG-B13 prodrugs). Novel analogs, the isomeric mono-DMG-B13, LCL522 (3-O-DMG-B13·HCl) and LCL596 (1-O-DMG-B13·HCl) and di-DMG-B13, LCL521 (1,3-O, O-DMG-B13·2HCl) conjugates, were designed and synthesized through N,N-dimethyl glycine (DMG) esterification of the hydroxyl groups of B13. In MCF7 cells, DMG-B13 prodrugs were efficiently metabolized to B13. The early inhibitory effect of DMG-B13 prodrugs on cellular ceramidases was ACDase specific by their lysosomal targeting. The corresponding dramatic decrease of cellular Sph (80-97% Control/1h) by DMG-B13 prodrugs was mainly from the inhibition of the lysosomal ACDase.
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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.