A sphingosine kinase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYA1]
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Lipophilic tail modifications of 2-(hydroxymethyl)pyrrolidine scaffold reveal dual sphingosine kinase 1 and 2 inhibitors.Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
Topographical Mapping of Isoform-Selectivity Determinants for J-Channel-Binding Inhibitors of Sphingosine Kinases 1 and 2.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Identification of selective inhibitors of sphingosine kinases 1 and 2 through a structure-activity relationship study of 4-epi-jaspine B.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
[no title available]Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
An integrative study to identify novel scaffolds for sphingosine kinase 1 inhibitors.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Development of hydroxy-based sphingosine kinase inhibitors and anti-inflammation in dextran sodium sulfate induced colitis in mice.Bioorganic & medicinal chemistry, , 07-15, Volume: 24, Issue:14, 2016
From Sphingosine Kinase to Dihydroceramide Desaturase: A Structure-Activity Relationship (SAR) Study of the Enzyme Inhibitory and Anticancer Activity of 4-((4-(4-Chlorophenyl)thiazol-2-yl)amino)phenol (SKI-II).Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
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, , Feb-26, Volume: 58, Issue:4, 2015
Structure guided design of a series of sphingosine kinase (SphK) inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 23, Issue:16, 2013
Development of amidine-based sphingosine kinase 1 nanomolar inhibitors and reduction of sphingosine 1-phosphate in human leukemia cells.Journal of medicinal chemistry, , May-26, Volume: 54, Issue:10, 2011
[no title available]Journal of medicinal chemistry, , 06-09, Volume: 65, Issue:11, 2022
Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 34, 2021
Lipophilic tail modifications of 2-(hydroxymethyl)pyrrolidine scaffold reveal dual sphingosine kinase 1 and 2 inhibitors.Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
Probing the substitution pattern of indole-based scaffold reveals potent and selective sphingosine kinase 2 inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
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, , Nov-15, Volume: 206, 2020
Topographical Mapping of Isoform-Selectivity Determinants for J-Channel-Binding Inhibitors of Sphingosine Kinases 1 and 2.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
[no title available]Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
An integrative study to identify novel scaffolds for sphingosine kinase 1 inhibitors.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype-Distinct Screening Hits.Journal of medicinal chemistry, , 03-23, Volume: 60, Issue:6, 2017
Identification of selective inhibitors of sphingosine kinases 1 and 2 through a structure-activity relationship study of 4-epi-jaspine B.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
From Sphingosine Kinase to Dihydroceramide Desaturase: A Structure-Activity Relationship (SAR) Study of the Enzyme Inhibitory and Anticancer Activity of 4-((4-(4-Chlorophenyl)thiazol-2-yl)amino)phenol (SKI-II).Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
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, , Feb-26, Volume: 58, Issue:4, 2015
Crystal Structure of Sphingosine Kinase 1 with PF-543.ACS medicinal chemistry letters, , Dec-11, Volume: 5, Issue:12, 2014
Novel sphingosine-containing analogues selectively inhibit sphingosine kinase (SK) isozymes, induce SK1 proteasomal degradation and reduce DNA synthesis in human pulmonary arterial smooth muscle cells.MedChemComm, , Volume: 4, Issue:10, 2013
Target | Category | Definition |
blood vessel development | biological process | The process whose specific outcome is the progression of a blood vessel over time, from its formation to the mature structure. The blood vessel is the vasculature carrying blood. [GOC:hjd, UBERON:0001981] |
sphingosine-1-phosphate receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by sphingosine-1-phosphate binding to its receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ascb_2009, GOC:signaling, PMID:14592418, PMID:22001186, Reactome:R-HSA-419428] |
protein acetylation | biological process | The addition of an acetyl group to a protein amino acid. An acetyl group is CH3CO-, derived from acetic [ethanoic] acid. [GOC:ai] |
sphingosine metabolic process | biological process | The chemical reactions and pathways involving sphingosine (sphing-4-enine), trans-D-erytho-2-amino-octadec-4-ene-1,3-diol, a long chain amino diol sphingoid base that occurs in most sphingolipids in animal tissues. [GOC:ma, ISBN:0198506732] |
inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
brain development | biological process | The process whose specific outcome is the progression of the brain over time, from its formation to the mature structure. Brain development begins with patterning events in the neural tube and ends with the mature structure that is the center of thought and emotion. The brain is responsible for the coordination and control of bodily activities and the interpretation of information from the senses (sight, hearing, smell, etc.). [GOC:dph, GOC:jid, GOC:tb, UBERON:0000955] |
cell population proliferation | biological process | The multiplication or reproduction of cells, resulting in the expansion of a cell population. [GOC:mah, GOC:mb] |
positive regulation of peptidyl-threonine phosphorylation | biological process | Any process that increases the frequency, rate or extent of peptidyl-threonine phosphorylation. Peptidyl-threonine phosphorylation is the phosphorylation of peptidyl-threonine to form peptidyl-O-phospho-L-threonine. [GOC:dph, GOC:tb] |
regulation of tumor necrosis factor-mediated signaling pathway | biological process | Any process that modulates the rate or extent of the tumor necrosis factor-mediated signaling pathway. The tumor necrosis factor-mediated signaling pathway is the series of molecular signals generated as a consequence of tumor necrosis factor binding to a cell surface receptor. [GOC:dph, GOC:tb] |
phosphorylation | biological process | The process of introducing a phosphate group into a molecule, usually with the formation of a phosphoric ester, a phosphoric anhydride or a phosphoric amide. [ISBN:0198506732] |
calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |
regulation of endocytosis | biological process | Any process that modulates the frequency, rate or extent of endocytosis. [GOC:go_curators] |
sphingolipid biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of sphingolipids, any of a class of lipids containing the long-chain amine diol sphingosine or a closely related base (a sphingoid). [GOC:mah, ISBN:0198506732] |
positive regulation of cell growth | biological process | Any process that activates or increases the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
positive regulation of cell migration | biological process | Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators] |
positive regulation of protein ubiquitination | biological process | Any process that activates or increases the frequency, rate or extent of the addition of ubiquitin groups to a protein. [GOC:mah] |
regulation of interleukin-1 beta production | biological process | Any process that modulates the frequency, rate, or extent of interleukin-1 beta production. [GOC:mah] |
positive regulation of interleukin-17 production | biological process | Any process that activates or increases the frequency, rate, or extent of production of any member of the interleukin-17 family of cytokines. [GOC:add, GOC:mah, PMID:16482511] |
response to tumor necrosis factor | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a tumor necrosis factor stimulus. [GOC:mah] |
intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
cellular response to vascular endothelial growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a vascular endothelial growth factor stimulus. [GOC:BHF, GOC:rl, PMID:18440775] |
negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
positive regulation of angiogenesis | biological process | Any process that activates or increases angiogenesis. [GOC:go_curators] |
positive regulation of mitotic nuclear division | biological process | Any process that activates or increases the frequency, rate or extent of mitosis. [GOC:go_curators] |
positive regulation of mitotic cell cycle | biological process | Any process that activates or increases the rate or extent of progression through the mitotic cell cycle. [GOC:dph, GOC:go_curators, GOC:tb] |
positive regulation of smooth muscle contraction | biological process | Any process that activates or increases the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
sphingosine biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of sphingosine (sphing-4-enine), trans-D-erytho-2-amino-octadec-4-ene-1,3-diol, a long chain amino diol sphingoid base that occurs in most sphingolipids in animal tissues. [GOC:ma, ISBN:0198506732] |
sphingoid catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of sphingoids, any of a class of compounds comprising sphinganine and its homologues and stereoisomers, and derivatives of these compounds. [ISBN:0198506732] |
regulation of phagocytosis | biological process | Any process that modulates the frequency, rate or extent of phagocytosis, the process in which phagocytes engulf external particulate material. [GOC:ai] |
positive regulation of NF-kappaB transcription factor activity | biological process | Any process that activates or increases the frequency, rate or extent of activity of the transcription factor NF-kappaB. [GOC:dph, GOC:tb, PMID:15087454, PMID:15170030] |
cellular response to hydrogen peroxide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hydrogen peroxide (H2O2) stimulus. [CHEBI:16240, GOC:mah] |
DNA biosynthetic process | biological process | The biosynthetic process resulting in the formation of DNA. [GOC:mah] |
regulation of neuroinflammatory response | biological process | Any process that modulates the frequency, rate or extent of neuroinflammatory response. [GOC:aruk, GOC:bc, PMID:10981966, PMID:11099416, PMID:18164423] |
negative regulation of ceramide biosynthetic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of a ceramide biosynthetic process. [GOC:TermGenie, PMID:15302821] |
positive regulation of p38MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of p38MAPK cascade. [GOC:TermGenie] |
positive regulation of non-canonical NF-kappaB signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of the non-canonical NF-kappaB cascade. [GOC:TermGenie] |
regulation of microglial cell activation | biological process | Any process that modulates the frequency, rate or extent of microglial cell activation. [GO_REF:0000058, GOC:BHF, GOC:nc, GOC:TermGenie, PMID:19100238] |
regulation of endosomal vesicle fusion | biological process | Any process that modulates the frequency, rate or extent of endosomal vesicle fusion. [GO_REF:0000058, GOC:bc, GOC:PARL, GOC:TermGenie, PMID:26911690] |
cellular response to growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a growth factor stimulus. [GOC:mah] |