ArticleACS medicinal chemistry letters2014
Crystal Structure of Sphingosine Kinase 1 with PF-543.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 papers.
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Who cites it
47 citing papers in PubMed, 100 citations in OpenAlex.
- DDI-4 induces a temperature-sensitive exocytotic remodeling during C. elegans spermiogenesis via nsun-2-dependent sphingosine signaling.PLoS genetics · 2026Article
- Targeting Leishmania donovani Sphingosine Kinase 1 using PF-543 enhances immune response and limits parasite load.PLoS neglected tropical diseases · 2026Article
- Structural dynamics of sphingosine kinase 1 regulation and inhibition.bioRxiv : the preprint server for biology · 2025Article
- Machine learning models to identify lead compound and substitution optimization to have derived energetics and conformational stability through docking and MD simulations for sphingosine kinase 1.Molecular diversity · 2025Article
- A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid Pathways.Biomolecules · 2025Review
- Structural dynamics of sphingosine kinase 1 regulation and inhibition.Research square · 2025Article
- Discovery of Sphingosine Kinase Inhibition by Modified Quinoline-5,8-Diones.Pharmaceuticals (Basel, Switzerland) · 2025Article
- The emerging roles of sphingosine 1-phosphate and SphK1 in cancer resistance: a promising therapeutic target.Cancer cell international · 2024Review
- Molecular docking analysis of sphingosine kinase 1 inhibitors for cancer management.Bioinformation · 2023Article
- Tumor Derived Extracellular Vesicles Drive T Cell Exhaustion in Tumor Microenvironment through Sphingosine Mediated Signaling and Impacting Immunotherapy Outcomes in Ovarian Cancer.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022Article
- New Druggable Targets for Rheumatoid Arthritis Based on Insights From Synovial Biology.Frontiers in immunology · 2022Review
- Vitamin D3 Prevents the Deleterious Effects of Testicular Torsion on Testis by Targeting miRNA-145 and ADAM17: In Silico and In Vivo Study.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Design, synthesis and analysis of novel sphingosine kinase-1 inhibitors to improve oral bioavailability.Bioorganic & medicinal chemistry letters · 2021Article
- A Dansyl-Modified Sphingosine Kinase Inhibitor DPF-543 Enhanced De Novo Ceramide Generation.International journal of molecular sciences · 2021Article
- A chemical screen for modulators of mRNA translation identifies a distinct mechanism of toxicity for sphingosine kinase inhibitors.PLoS biology · 2021Article
- Activation of SphK1 by adipocytes mediates epithelial ovarian cancer cell proliferation.Journal of ovarian research · 2021Article
- Probing the substitution pattern of indole-based scaffold reveals potent and selective sphingosine kinase 2 inhibitors.European journal of medicinal chemistry · 2021Article
- Lipophilic tail modifications of 2-(hydroxymethyl)pyrrolidine scaffold reveal dual sphingosine kinase 1 and 2 inhibitors.Bioorganic & medicinal chemistry · 2021Article
- Therapeutic Potential of SphK1 Inhibitors Based on Abnormal Expression of SphK1 in Inflammatory Immune Related-Diseases.Frontiers in pharmacology · 2021Review
- Identifying novel sphingosine kinase 1 inhibitors as therapeutics against breast cancer.Journal of enzyme inhibition and medicinal chemistry · 2020Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
The most potent inhibitor of Sphingosine Kinase 1 (SPHK1) so far identified is PF-543. The crystal structure of SPHK1 in complex with inhibitor PF-543 to 1.8 Å resolution reveals the inhibitor bound in a bent conformation analogous to that expected of a bound sphingosine substrate but with a rotated head group. The structural data presented will aid in the design of SPHK1 and SPHK2 inhibitors with improved properties.
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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.