Page last updated: 2024-08-07 13:48:48
Aurora kinase C
An aurora kinase C that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UQB9]
Synonyms
EC 2.7.11.1;
Aurora 3;
Aurora/IPL1-related kinase 3;
ARK-3;
Aurora-related kinase 3;
Aurora/IPL1/Eg2 protein 2;
Serine/threonine-protein kinase 13;
Serine/threonine-protein kinase aurora-C
Research
Bioassay Publications (36)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 16 (44.44) | 29.6817 |
| 2010's | 15 (41.67) | 24.3611 |
| 2020's | 5 (13.89) | 2.80 |
Compounds (97)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.The Journal of biological chemistry, , Jun-05, Volume: 284, Issue:23, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
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
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
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Novel Aurora A and Protein Kinase C (α, β1, β2, and θ) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
Discovery of novel 2,4-disubstituted pyrimidines as Aurora kinase inhibitors.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 30, Issue:3, 2020
Synthesis and identification of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential Aurora A inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 27, Issue:1, 2019
A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
SAR156497, an exquisitely selective inhibitor of aurora kinases.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 23, Issue:12, 2013
Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.ACS chemical biology, , Jan-20, Volume: 7, Issue:1, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 21, Issue:18, 2011
3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Discovery and development of aurora kinase inhibitors as anticancer agents.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.The Journal of biological chemistry, , Jun-05, Volume: 284, Issue:23, 2009
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
The selectivity of protein kinase inhibitors: a further update.The Biochemical journal, , Dec-15, Volume: 408, Issue:3, 2007
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.Nature medicine, , Volume: 10, Issue:3, 2004
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
Novel Aurora A and Protein Kinase C (α, β1, β2, and θ) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
SAR156497, an exquisitely selective inhibitor of aurora kinases.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.ACS chemical biology, , Jan-20, Volume: 7, Issue:1, 2012
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.ACS chemical biology, , Jan-20, Volume: 7, Issue:1, 2012
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 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
Novel Aurora A and Protein Kinase C (α, β1, β2, and θ) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
[no title available],
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
| 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 serine/threonine/tyrosine kinase activity | molecular function | Catalysis of the reactions: ATP + a protein serine = ADP + protein serine phosphate; ATP + a protein threonine = ADP + protein threonine phosphate; and ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [GOC:mah] |
| 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 6 target(s):
| Target | Category | Definition |
|---|
| condensed chromosome | cellular component | A highly compacted molecule of DNA and associated proteins resulting in a cytologically distinct structure. [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] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| spindle | cellular component | The array of microtubules and associated molecules that forms between opposite poles of a eukaryotic cell during mitosis or meiosis and serves to move the duplicated chromosomes apart. [ISBN:0198547684] |
| midbody | cellular component | A thin cytoplasmic bridge formed between daughter cells at the end of cytokinesis. The midbody forms where the contractile ring constricts, and may persist for some time before finally breaking to complete cytokinesis. [ISBN:0815316194] |
| spindle midzone | cellular component | The area in the center of the spindle where the spindle microtubules from opposite poles overlap. [GOC:ai, PMID:15296749] |
Active In
This protein is active in 4 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] |
| spindle midzone | cellular component | The area in the center of the spindle where the spindle microtubules from opposite poles overlap. [GOC:ai, PMID:15296749] |
| spindle pole centrosome | cellular component | A centrosome from which one pole of a mitotic or meiotic spindle is organized. [GOC:mah] |
| spindle microtubule | cellular component | Any microtubule that is part of a mitotic or meiotic spindle; anchored at one spindle pole. [ISBN:0815316194] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| chromosome passenger complex | cellular component | A eukaryotically conserved protein complex that localizes to kinetochores in early mitosis, the spindle mid-zone in anaphase B and to the telophase midbody. It has been proposed that the passenger complex coordinates various events based on its location to different structures during the course of mitosis. Complex members include the BIR-domain-containing protein Survivin, Aurora kinase, INCENP and Borealin. [GOC:vw, PMID:16824200, PMID:19570910] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| attachment of spindle microtubules to kinetochore | biological process | The process in which spindle microtubules become physically associated with the proteins making up the kinetochore complex. [GOC:vw, PMID:10322137] |
| positive regulation of cytokinesis | biological process | Any process that activates or increases the frequency, rate or extent of the division of the cytoplasm of a cell, and its separation into two daughter cells. [GOC:mah] |
| mitotic spindle midzone assembly | biological process | The cell cycle process in which the aggregation, arrangement and bonding together of a set of components forms the spindle midzone. [GOC:mtg_cell_cycle, GOC:vw, PMID:24239120] |
| cell division | biological process | The process resulting in division and partitioning of components of a cell to form more cells; may or may not be accompanied by the physical separation of a cell into distinct, individually membrane-bounded daughter cells. [GOC:di, GOC:go_curators, GOC:pr] |
| meiotic cell cycle | biological process | Progression through the phases of the meiotic cell cycle, in which canonically a cell replicates to produce four offspring with half the chromosomal content of the progenitor cell via two nuclear divisions. [GOC:ai] |
| 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] |
| 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] |