Page last updated: 2024-08-08 00:18:09
Sphingosine kinase 2
A sphingosine kinase 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NRA0]
Synonyms
SK 2;
SPK 2;
EC 2.7.1.91
Research
Bioassay Publications (25)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 2 (8.00) | 29.6817 |
2010's | 14 (56.00) | 24.3611 |
2020's | 9 (36.00) | 2.80 |
Compounds (9)
Drugs with Inhibition Measurements
Drugs with Other Measurements
Lipophilic tail modifications of 2-(hydroxymethyl)pyrrolidine scaffold reveal dual sphingosine kinase 1 and 2 inhibitors.Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents.European journal of medicinal chemistry, , Jan-15, Volume: 210, 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
[no title available]Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 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
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
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
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
Importance of sphingosine kinase (SphK) as a target in developing cancer therapeutics and recent developments in the synthesis of novel SphK inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 2014
Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases.Journal of medicinal chemistry, , Jun-25, Volume: 52, Issue:12, 2009
Iodophenyl tagged sphingosine derivatives: synthesis and preliminary biological evaluation.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
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
[no title available]Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 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
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
Structure-activity relationship studies of the lipophilic tail region of sphingosine kinase 2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 25, Issue:21, 2015
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
Importance of sphingosine kinase (SphK) as a target in developing cancer therapeutics and recent developments in the synthesis of novel SphK inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 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
Structure guided design of a series of sphingosine kinase (SphK) inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 23, Issue:16, 2013
Effect of alkyl chain length on sphingosine kinase 2 selectivity.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
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
Importance of sphingosine kinase (SphK) as a target in developing cancer therapeutics and recent developments in the synthesis of novel SphK inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 2014
[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
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
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
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
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 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
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
Structure-Activity Relationship Studies and Molecular Modeling of Naphthalene-Based Sphingosine Kinase 2 Inhibitors.ACS medicinal chemistry letters, , Mar-10, Volume: 7, Issue:3, 2016
Importance of sphingosine kinase (SphK) as a target in developing cancer therapeutics and recent developments in the synthesis of novel SphK inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 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
Effect of alkyl chain length on sphingosine kinase 2 selectivity.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
Enables
This protein enables 8 target(s):
Target | Category | Definition |
lipid kinase activity | molecular function | Catalysis of the phosphorylation of a simple or complex lipid. [GOC:hjd] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
sphinganine kinase activity | molecular function | Catalysis of the reaction: ATP + sphinganine = ADP + sphinganine 1-phosphate. [EC:2.7.1.91] |
D-erythro-sphingosine kinase activity | molecular function | Catalysis of the reaction: sphingosine + ATP = sphingosine 1-phosphate + ADP. [MetaCyc:RXN3DJ-11417] |
small GTPase binding | molecular function | Binding to a small monomeric GTPase. [GOC:mah, PMID:27218782] |
sphingosine-1-phosphate receptor activity | molecular function | Combining with the sphingolipid sphingosine-1-phosphate (S1P), and transmitting the signal across the membrane by activating an associated G-protein. [GOC:bf, PMID:12728273, Wikipedia:S1PR1] |
histone binding | molecular function | Binding to a histone, any of a group of water-soluble proteins found in association with the DNA of eukaryotic or archaeal chromosomes. They are involved in the condensation and coiling of chromosomes during cell division and have also been implicated in gene regulation and DNA replication. They may be chemically modified (methylated, acetlyated and others) to regulate gene transcription. [GOC:jl, PMID:16209651, PMID:30212449, PMID:9305837] |
Located In
This protein is located in 9 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
mitochondrial inner membrane | cellular component | The inner, i.e. lumen-facing, lipid bilayer of the mitochondrial envelope. It is highly folded to form cristae. [GOC:ai] |
lysosomal membrane | cellular component | The lipid bilayer surrounding the lysosome and separating its contents from the cell cytoplasm. [GOC:ai] |
endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 3 target(s):
Target | Category | Definition |
intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
nucleosome | cellular component | A complex comprised of DNA wound around a multisubunit core and associated proteins, which forms the primary packing unit of DNA into higher order structures. [GOC:elh] |
Involved In
This protein is involved in 27 target(s):
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] |
positive regulation of cytokine production involved in immune response | biological process | Any process that activates or increases the frequency, rate, or extent of cytokine production that contributes to an immune response. [GOC:add] |
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] |
sphinganine-1-phosphate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of sphinganine-1-phosphate, the phosphorylated derivative of D-erythro-2-amino-1,3-octadecanediol. [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] |
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 cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [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] |
negative regulation of cell growth | biological process | Any process that stops, prevents, or reduces the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
positive regulation of interleukin-13 production | biological process | Any process that activates or increases the frequency, rate, or extent of interleukin-13 production. [GOC:mah] |
positive regulation of interleukin-6 production | biological process | Any process that activates or increases the frequency, rate, or extent of interleukin-6 production. [GOC:mah] |
positive regulation of tumor necrosis factor production | biological process | Any process that activates or increases the frequency, rate or extent of tumor necrosis factor production. [GO_REF:0000058, GOC:TermGenie, PMID:10891884, PMID:15560120] |
positive regulation of mast cell activation involved in immune response | biological process | Any process that activates or increases the frequency, rate, or extent of mast cell activation as part of an immune response. [GOC:mah] |
positive regulation of apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
regulation of canonical NF-kappaB signal transduction | biological process | Any process that modulates the canonical NF-kappaB signaling cascade. [GOC:jl, PMID:12773372] |
positive regulation of mast cell degranulation | biological process | Any process that activates or increases the frequency, rate or extent of mast cell degranulation. [ISBN:0781735149] |
transcription initiation-coupled chromatin remodeling | biological process | An epigenetic mechanism of regulation of gene expression that involves chromatin remodeling to capacitate gene expression by either modifying the chromatin fiber, the nucleosomal histones, or the DNA. [PMID:34414474] |
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] |
positive regulation of protein kinase C signaling | biological process | Any process that increases the frequency, rate, or extent of a series of reactions, mediated by the intracellular serine/threonine kinase protein kinase C, which occurs as a result of a single trigger reaction or compound. [GOC:dph, GOC:tb] |
positive regulation of calcium ion import | biological process | Any process that increases the rate, frequency, or extent of the directed movement of calcium ions into a cell or organelle. [GOC:BHF] |
regulation of reactive oxygen species biosynthetic process | biological process | Any process that modulates the frequency, rate or extent of reactive oxygen species biosynthetic process. [GO_REF:0000058, GOC:bf, GOC:PARL, GOC:TermGenie, PMID:24252804] |
cellular response to phorbol 13-acetate 12-myristate | 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 phorbol 13-acetate 12-myristate stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:2200903] |
regulation of cytochrome-c oxidase activity | biological process | Any process that modulates the frequency, rate or extent of cytochrome-c oxidase activity. [GO_REF:0000059, GOC:TermGenie, PMID:26734017] |
positive regulation of ceramide biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of ceramide biosynthetic process. [GOC:dph] |
regulation of ATP biosynthetic process | biological process | Any process that modulates the frequency, rate or extent of ATP biosynthetic process. [GOC:obol] |
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] |