Proteins > Serine/threonine-protein kinase PLK2
Page last updated: 2024-08-08 00:19:13
Serine/threonine-protein kinase PLK2
A serine/threonine-protein kinase PLK2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYY3]
Synonyms
EC 2.7.11.21;
Polo-like kinase 2;
PLK-2;
hPlk2;
Serine/threonine-protein kinase SNK;
hSNK;
Serum-inducible kinase
Research
Bioassay Publications (18)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (22.22) | 29.6817 |
| 2010's | 13 (72.22) | 24.3611 |
| 2020's | 1 (5.56) | 2.80 |
Compounds (84)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.Journal of medicinal chemistry, , Aug-08, Volume: 56, Issue:15, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
Polo-like Kinase 1 Inhibitors in Human Cancer Therapy: Development and Therapeutic Potential.Journal of medicinal chemistry, , 08-11, Volume: 65, Issue:15, 2022
Discovery of Novel Polo-Like Kinase 1 Polo-Box Domain Inhibitors to Induce Mitotic Arrest in Tumor Cells.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Polo-like Kinase 1 Inhibitors in Human Cancer Therapy: Development and Therapeutic Potential.Journal of medicinal chemistry, , 08-11, Volume: 65, Issue:15, 2022
Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
Selectivity-determining residues in Plk1.Chemical biology & drug design, , Volume: 70, Issue:6, 2007
[no title available],
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| 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] |
| ATP-dependent protein binding | molecular function | Binding to a protein or protein complex using energy from ATP hydrolysis. [GOC:jl] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
| centriole | cellular component | A cellular organelle, found close to the nucleus in many eukaryotic cells, consisting of a small cylinder with microtubular walls, 300-500 nm long and 150-250 nm in diameter. It contains nine short, parallel, peripheral microtubular fibrils, each fibril consisting of one complete microtubule fused to two incomplete microtubules. Cells usually have two centrioles, lying at right angles to each other. At division, each pair of centrioles generates another pair and the twin pairs form the pole of the mitotic spindle. [ISBN:0198547684] |
| 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] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
Active In
This protein is active in 6 target(s):
| Target | Category | Definition |
|---|
| spindle pole | cellular component | Either of the ends of a spindle, where spindle microtubules are organized; usually contains a microtubule organizing center and accessory molecules, spindle microtubules and astral microtubules. [GOC:clt] |
| centriole | cellular component | A cellular organelle, found close to the nucleus in many eukaryotic cells, consisting of a small cylinder with microtubular walls, 300-500 nm long and 150-250 nm in diameter. It contains nine short, parallel, peripheral microtubular fibrils, each fibril consisting of one complete microtubule fused to two incomplete microtubules. Cells usually have two centrioles, lying at right angles to each other. At division, each pair of centrioles generates another pair and the twin pairs form the pole of the mitotic spindle. [ISBN:0198547684] |
| centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| kinetochore | cellular component | A multisubunit complex that is located at the centromeric region of DNA and provides an attachment point for the spindle microtubules. [GOC:elh] |
| 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] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
Involved In
This protein is involved in 21 target(s):
| Target | Category | Definition |
|---|
| G1/S transition of mitotic cell cycle | biological process | The mitotic cell cycle transition by which a cell in G1 commits to S phase. The process begins with the build up of G1 cyclin-dependent kinase (G1 CDK), resulting in the activation of transcription of G1 cyclins. The process ends with the positive feedback of the G1 cyclins on the G1 CDK which commits the cell to S phase, in which DNA replication is initiated. [GOC:mtg_cell_cycle] |
| negative regulation of inflammatory response to antigenic stimulus | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of an inflammatory response to an antigenic stimulus. [GOC:add] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrest | biological process | A cascade of processes induced by the cell cycle regulator phosphoprotein p53, or an equivalent protein, in response to the detection of DNA damage and resulting in the stopping or reduction in rate of the cell cycle. [GOC:go_curators] |
| mitotic spindle organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of the microtubule spindle during a mitotic cell cycle. [GOC:go_curators, GOC:mah] |
| Ras protein signal transduction | biological process | An intracellular signaling cassette in which a small monomeric GTPase of the Ras subfamily relays a signal. [GOC:bf] |
| memory | biological process | The activities involved in the mental information processing system that receives (registers), modifies, stores, and retrieves informational stimuli. The main stages involved in the formation and retrieval of memory are encoding (processing of received information by acquisition), storage (building a permanent record of received information as a result of consolidation) and retrieval (calling back the stored information and use it in a suitable way to execute a given task). [GOC:curators, ISBN:0582227089] |
| positive regulation of autophagy | biological process | Any process that activates, maintains or increases the rate of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| negative regulation of angiogenesis | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of angiogenesis. [GOC:go_curators] |
| peptidyl-serine phosphorylation | biological process | The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037] |
| Rap protein signal transduction | biological process | An intracellular signaling cassette in which a small monomeric GTPase of the Rap subfamily relays a signal. [GOC:mah] |
| 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 canonical NF-kappaB signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl] |
| positive regulation of protein catabolic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the breakdown of a protein by the destruction of the native, active configuration, with or without the hydrolysis of peptide bonds. [GOC:go_curators] |
| regulation of centriole replication | biological process | Any process that modulates the frequency, rate or extent of the formation of a daughter centriole of an existing centriole. [GOC:ai] |
| regulation of synaptic plasticity | biological process | A process that modulates synaptic plasticity, the ability of synapses to change as circumstances require. They may alter function, such as increasing or decreasing their sensitivity, or they may increase or decrease in actual numbers. [GOC:dph, GOC:jid, GOC:tb, PMID:11891290] |
| long-term synaptic potentiation | biological process | A process that modulates synaptic plasticity such that synapses are changed resulting in the increase in the rate, or frequency of synaptic transmission at the synapse. [GOC:dgh, GOC:dph] |
| long-term synaptic depression | biological process | A process that modulates synaptic plasticity such that synapses are changed resulting in the decrease in the rate, or frequency of synaptic transmission at the synapse. [GOC:dgh, GOC:dph] |
| negative regulation of apoptotic process in bone marrow cell | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the occurrence or rate of cell death by apoptotic process in the bone marrow. [GOC:mah, GOC:mtg_apoptosis, GOC:yaf, PMID:17063141] |
| positive regulation of cell migration involved in sprouting angiogenesis | biological process | Any process that increases the frequency, rate or extent of cell migration involved in sprouting angiogenesis. Cell migration involved in sprouting angiogenesis is the orderly movement of endothelial cells into the extracellular matrix in order to form new blood vessels contributing to the process of sprouting angiogenesis. [GOC:BHF, GOC:dph, GOC:rl, GOC:tb] |
| negative regulation of cellular senescence | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of cellular senescence. [GOC:BHF] |