Proteins > Serine/threonine-protein kinase PLK3
Page last updated: 2024-08-07 18:49:56
Serine/threonine-protein kinase PLK3
A serine/threonine-protein kinase PLK3 that is encoded in the genome of human. [PMID:15190214, PRO:KER]
Synonyms
EC 2.7.11.21;
Cytokine-inducible serine/threonine-protein kinase;
FGF-inducible kinase;
Polo-like kinase 3;
PLK-3;
Proliferation-related kinase
Research
Bioassay Publications (21)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 9 (42.86) | 29.6817 |
| 2010's | 11 (52.38) | 24.3611 |
| 2020's | 1 (4.76) | 2.80 |
Compounds (91)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
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 kinases inhibited by wortmannin. Labeling site and downstream effects.The Journal of biological chemistry, , Jan-26, Volume: 282, Issue:4, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
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
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
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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.Biochemistry, , Aug-21, Volume: 46, Issue:33, 2007
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 kinases inhibited by wortmannin. Labeling site and downstream effects.The Journal of biological chemistry, , Jan-26, Volume: 282, Issue:4, 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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Discovery of thiophene inhibitors of polo-like kinase.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 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
[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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.Proceedings of the National Academy of Sciences of the United States of America, , Dec-18, Volume: 104, Issue:51, 2007
Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).Bioorganic & medicinal chemistry, , Jan-15, Volume: 15, Issue:2, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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 |
|---|
| p53 binding | molecular function | Binding to one of the p53 family of proteins. [GOC:hjd] |
| 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] |
| 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 8 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] |
| nucleolus | cellular component | A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| Golgi stack | cellular component | The set of thin, flattened membrane-bounded compartments, called cisternae, that form the central portion of the Golgi complex. The stack usually comprises cis, medial, and trans cisternae; the cis- and trans-Golgi networks are not considered part of the stack. [GOC:mah, ISBN:0815316194] |
| 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] |
| 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] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
Active In
This protein is active in 5 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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] |
| 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] |
| 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] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 23 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] |
| G2/M transition of mitotic cell cycle | biological process | The mitotic cell cycle transition by which a cell in G2 commits to M phase. The process begins when the kinase activity of M cyclin/CDK complex reaches a threshold high enough for the cell cycle to proceed. This is accomplished by activating a positive feedback loop that results in the accumulation of unphosphorylated and active M cyclin/CDK complex. [GOC:mtg_cell_cycle] |
| negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
| response to reactive oxygen species | 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 reactive oxygen species stimulus. Reactive oxygen species include singlet oxygen, superoxide, and oxygen free radicals. [GOC:krc] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
| response to osmotic stress | 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 stimulus indicating an increase or decrease in the concentration of solutes outside the organism or cell. [GOC:jl] |
| DNA damage response | 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 stimulus indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators] |
| 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] |
| endomitotic cell cycle | biological process | A mitotic cell cycle in which chromosomes are replicated and sister chromatids separate, but spindle formation, nuclear membrane breakdown and nuclear division do not occur, resulting in an increased number of chromosomes in the cell. [GOC:curators, GOC:dos, GOC:expert_vm] |
| response to radiation | 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 an electromagnetic radiation stimulus. Electromagnetic radiation is a propagating wave in space with electric and magnetic components. These components oscillate at right angles to each other and to the direction of propagation. [GOC:jl, Wikipedia:Electromagnetic_radiation] |
| cytoplasmic microtubule 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 structures formed of microtubules and associated proteins in the cytoplasm of a cell. [GOC:mah] |
| regulation of cytokinesis | biological process | Any process that modulates the frequency, rate or extent of the division of the cytoplasm of a cell and its separation into two daughter cells. [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] |
| mitotic G1/S transition checkpoint signaling | biological process | A cell cycle checkpoint that detects and negatively regulates progression from G1 to S phase as part of a mitotic cell cycle. [GOC:mtg_cell_cycle] |
| regulation of cell division | biological process | Any process that modulates the frequency, rate or extent of the physical partitioning and separation of a cell into daughter cells. [GOC:go_curators] |
| negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| Golgi disassembly | biological process | A cellular process that results in the breakdown of a Golgi apparatus that contributes to Golgi inheritance. [GOC:ascb_2009, GOC:dph, GOC:tb] |
| positive regulation of intracellular protein transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of proteins within cells. [GOC:tb] |
| regulation of signal transduction by p53 class mediator | biological process | Any process that modulates the frequency, rate or extent of signal transduction by p53 class mediator. [GOC:TermGenie] |
| positive regulation of chaperone-mediated autophagy | biological process | Any process that activates or increases the frequency, rate or extent of chaperone-mediated autophagy. [GO_REF:0000058, GOC:pad, GOC:PARL, GOC:TermGenie, PMID:20176123] |
| positive regulation of proteasomal ubiquitin-dependent protein catabolic process involved in cellular response to hypoxia | biological process | Any positive regulation of proteasomal ubiquitin-dependent protein catabolic process that is involved in a cellular response to hypoxia. [GOC:mah] |
| 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] |