ArticleJournal of medicinal chemistry2013
Structure-activity relationships and molecular modeling of sphingosine kinase inhibitors.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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Who cites it
19 citing papers in PubMed.
- PET Imaging of Sphingolipid Signaling: Current Radiotracers, Translational Gaps, and Opportunities in Neurodegeneration and Oncology.ACS omega · 2026Review
- Medicinal chemistry perspectives on anticancer drug design based on clinical applications (2015-2025).RSC advances · 2025Review
- Metabolomics analysis reveals resembling metabolites between humanized γδ TCR mice and human plasma.Scientific reports · 2024Article
- Targeting sphingosine 1-phosphate and sphingosine kinases in pancreatic cancer: mechanisms and therapeutic potential.Cancer cell international · 2024Review
- Structural insights into sphingosine-1-phosphate receptor activation.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Exploiting activity cliffs for building pharmacophore models and comparison with other pharmacophore generation methods: sphingosine kinase 1 as case study.Journal of computer-aided molecular design · 2022Article
- Targeting the Sphingosine Kinase/Sphingosine-1-Phosphate Signaling Axis in Drug Discovery for Cancer Therapy.Cancers · 2021Review
- Therapeutic Potential of SphK1 Inhibitors Based on Abnormal Expression of SphK1 in Inflammatory Immune Related-Diseases.Frontiers in pharmacology · 2021Review
- Article
- Field template-based design and biological evaluation of new sphingosine kinase 1 inhibitors.Breast cancer research and treatment · 2018Article
- Synthesis of Novel FTY720 Analogs with Anticancer Activity through PP2A Activation.Molecules (Basel, Switzerland) · 2018Article
- Development of 1,2,3-Triazole-Based Sphingosine Kinase Inhibitors and Their Evaluation as Antiproliferative Agents.International journal of molecular sciences · 2017Article
- Article
- Transforming Sphingosine Kinase 1 Inhibitors into Dual and Sphingosine Kinase 2 Selective Inhibitors: Design, Synthesis, and in Vivo Activity.Journal of medicinal chemistry · 2017Article
- Phosphorylation of a constrained azacyclic FTY720 analog enhances anti-leukemic activity without inducing S1P receptor activation.Leukemia · 2017Article
- Sphingosine kinase inhibitors: a review of patent literature (2006-2015).Expert opinion on therapeutic patents · 2016Review
- Sphingosine 1-Phosphate Activation of EGFR As a Novel Target for Meningitic Escherichia coli Penetration of the Blood-Brain Barrier.PLoS pathogens · 2016Article
- Sphingosine-1-phosphate metabolism: A structural perspective.Critical reviews in biochemistry and molecular biology · 2015Review
- Crystal Structure of Sphingosine Kinase 1 with PF-543.ACS medicinal chemistry letters · 2014Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
The design, synthesis, and evaluation of the potency of new isoform-selective inhibitors of sphingosine kinases 1 and 2 (SK1 and SK2), the enzyme that catalyzes the phosphorylation of d-erythro-sphingosine to produce the key signaling lipid, sphingosine 1-phosphate, are described. Recently, we reported that 1-(4-octylphenethyl)piperidin-4-ol (RB-005) is a selective inhibitor of SK1. Here we report the synthesis of 43 new analogues of RB-005, in which the lipophilic tail, polar headgroup, and linker region were modified to extend the structure-activity relationship profile for this lead compound, which we explain using modeling studies with the recently published crystal structure of SK1. We provide a basis for the key residues targeted by our profiled series and provide further evidence for the ability to discriminate between the two isoforms using pharmacological intervention.
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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.