ArticleJournal of medicinal chemistry2011
Development of amidine-based sphingosine kinase 1 nanomolar inhibitors and reduction of sphingosine 1-phosphate in human leukemia cells.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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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
37 citing papers in PubMed, 72 citations in OpenAlex.
- The emerging roles of sphingosine 1-phosphate and SphK1 in cancer resistance: a promising therapeutic target.Cancer cell international · 2024Review
- Development and profiling of mGluBioorganic & medicinal chemistry letters · 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
- Development of SKI-349, a dual-targeted inhibitor of sphingosine kinase and microtubule polymerization.Bioorganic & medicinal chemistry letters · 2020Article
- Design and Development of Novel Urea, Sulfonyltriurea, and Sulfonamide Derivatives as Potential Inhibitors ofPharmaceuticals (Basel, Switzerland) · 2020Article
- A 6-Membrane Protein Gene score for prognostic prediction of cytogenetically normal acute myeloid leukemia in multiple cohorts.Journal of Cancer · 2020Article
- Field template-based design and biological evaluation of new sphingosine kinase 1 inhibitors.Breast cancer research and treatment · 2018Article
- "Dicing and Splicing" Sphingosine Kinase and Relevance to Cancer.International journal of molecular sciences · 2017Review
- A Phase I Study of ABC294640, a First-in-Class Sphingosine Kinase-2 Inhibitor, in Patients with Advanced Solid Tumors.Clinical cancer research : an official journal of the American Association for Cancer Research · 2017Article
- Menoctone Resistance in Malaria Parasites Is Conferred by M133I Mutations in CytochromeAntimicrobial agents and chemotherapy · 2017Article
- Mammalian sphingosine kinase (SphK) isoenzymes and isoform expression: challenges for SphK as an oncotarget.Oncotarget · 2017Review
- The Role of Sphingosine-1-Phosphate and Ceramide-1-Phosphate in Inflammation and Cancer.Mediators of inflammation · 2017Review
- Sphingosine kinase inhibitors: a review of patent literature (2006-2015).Expert opinion on therapeutic patents · 2016Review
- Sphingosine 1-phosphate signaling impacts lymphocyte migration, inflammation and infection.Pathogens and disease · 2016Review
- Structural Requirements and Docking Analysis of Amidine-Based Sphingosine Kinase 1 Inhibitors Containing Oxadiazoles.ACS medicinal chemistry letters · 2016Article
- The emerging role of FTY720 (Fingolimod) in cancer treatment.Oncotarget · 2016Review
- Sphingosine Kinase 2 Inhibition and Blood Sphingosine 1-Phosphate Levels.The Journal of pharmacology and experimental therapeutics · 2015Article
- Structure-based functional annotation of hypothetical proteins from Candida dubliniensis: a quest for potential drug targets.3 Biotech · 2015Article
- The apoptotic mechanism of action of the sphingosine kinase 1 selective inhibitor SKI-178 in human acute myeloid leukemia cell lines.The Journal of pharmacology and experimental therapeutics · 2015Article
- Structure-activity relationship studies and in vivo activity of guanidine-based sphingosine kinase inhibitors: discovery of SphK1- and SphK2-selective inhibitors.Journal of medicinal chemistry · 2015Article
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
Sphingosine 1-phosphate (S1P) is a bioactive lipid that has been identified as an accelerant of cancer progression. The sphingosine kinases (SphKs) are the sole producers of S1P, and thus, SphK inhibitors may prove effective in cancer mitigation and chemosensitization. Of the two SphKs, SphK1 overexpression has been observed in a myriad of cancer cell lines and tissues and has been recognized as the presumptive target over that of the poorly characterized SphK2. Herein, we present the design and synthesis of amidine-based nanomolar SphK1 subtype-selective inhibitors. A homology model of SphK1, trained with this library of amidine inhibitors, was then used to predict the activity of additional, more potent, inhibitors. Lastly, select amidine inhibitors were validated in human leukemia U937 cells, where they significantly reduced endogenous S1P levels at nanomolar concentrations.
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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.