ArticleBioorganic & medicinal chemistry2012
Design, synthesis and biological activity of sphingosine kinase 2 selective inhibitors.
Article in Bioorganic & medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 41 citations in OpenAlex.
- Natural Products and Small Molecules Targeting Cellular Ceramide Metabolism to Enhance Apoptosis in Cancer Cells.Cancers · 2023Review
- Discovery of In Vivo Active Sphingosine-1-phosphate Transporter (Spns2) Inhibitors.Journal of medicinal chemistry · 2022Article
- Structure-activity relationship studies and bioactivity evaluation of 1,2,3-triazole containing analogues as a selective sphingosine kinase-2 inhibitors.European journal of medicinal chemistry · 2020Article
- Targeting the SphK-S1P-SIPR Pathway as a Potential Therapeutic Approach for COVID-19.International journal of molecular sciences · 2020Review
- Analysis of selective target engagement by small-molecule sphingosine kinase inhibitors using the Cellular Thermal Shift Assay (CETSA).Cancer biology & therapy · 2020Article
- SphK2 over-expression promotes osteosarcoma cell growth.Oncotarget · 2017Article
- Mammalian sphingosine kinase (SphK) isoenzymes and isoform expression: challenges for SphK as an oncotarget.Oncotarget · 2017Review
- Structure-Activity Relationship Studies and Molecular Modeling of Naphthalene-Based Sphingosine Kinase 2 Inhibitors.ACS medicinal chemistry letters · 2016Article
- The impact of sphingosine kinase inhibitor-loaded nanoparticles on bioelectrical and biomechanical properties of cancer cells.Lab on a chip · 2016Article
- Structure-activity relationship studies of the lipophilic tail region of sphingosine kinase 2 inhibitors.Bioorganic & medicinal chemistry letters · 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
- Diversity-oriented synthetic strategies applied to cancer chemical biology and drug discovery.Molecules (Basel, Switzerland) · 2014Review
- Inhibition of dihydroceramide desaturase activity by the sphingosine kinase inhibitor SKI II.Journal of lipid research · 2014Article
- Structure-activity relationships and molecular modeling of sphingosine kinase inhibitors.Journal of medicinal chemistry · 2013Article
- Sphingosine kinase A is a pleiotropic and essential enzyme for Leishmania survival and virulence.Molecular microbiology · 2013Article
- Synthesis of selective inhibitors of sphingosine kinase 1.Chemical communications (Cambridge, England) · 2013Article
- The sphingosine kinase inhibitor 2-(p-hyroxyanilino)-4-(p-chlorophenyl)thiazole reduces androgen receptor expression via an oxidative stress-dependent mechanism.British journal of pharmacology · 2013Article
- Targeting the sphingosine kinase/sphingosine 1-phosphate pathway in disease: review of sphingosine kinase inhibitors.Biochimica et biophysica acta · 2013Review
- Article
- Effect of alkyl chain length on sphingosine kinase 2 selectivity.Bioorganic & medicinal chemistry letters · 2012Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Sphingosine kinase (SphK) has emerged as an attractive target for cancer therapeutics due to its role in cell survival. SphK phosphorylates sphingosine to form sphingosine 1-phosphate (S1P), which has been implicated in cancer growth and survival. SphK exists as two different isotypes, namely SphK1 and SphK2, which play different roles inside the cell. In this report, we describe SphK inhibitors based on the immunomodulatory drug, FTY720, which is phosphorylated by SphK2 to generate a S1P mimic. Structural modification of FTY720 provided a template for synthesizing new inhibitors. A diversity-oriented synthesis generated a library of SphK inhibitors with a novel scaffold and headgroup. We have discovered subtype selective inhibitors with K(i)'s in the low micromolar range. This is the first report describing quaternary ammonium salts as SphK inhibitors.
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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.