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Cyclin-K
A cyclin-K that is encoded in the genome of human. [PRO:DNx, UniProtKB:O75909]
Synonyms
Research
Bioassay Publications (11)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 6 (54.55) | 24.3611 |
2020's | 5 (45.45) | 2.80 |
Compounds (7)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
staurosporine | Homo sapiens (human) | IC50 | 0.0948 | 5 | 5 |
alvocidib | Homo sapiens (human) | IC50 | 1.3700 | 1 | 1 |
palbociclib | Homo sapiens (human) | IC50 | 1.2070 | 1 | 1 |
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
abemaciclib | Homo sapiens (human) | IC50 | 0.0650 | 1 | 1 |
dinaciclib | Homo sapiens (human) | IC50 | 0.0227 | 3 | 3 |
THZ531 | Homo sapiens (human) | IC50 | 0.2656 | 6 | 6 |
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
Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 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
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
[no title available]Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Synthetic Lethality through the Lens of Medicinal Chemistry.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Synthetic Lethality through the Lens of Medicinal Chemistry.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 29, Issue:20, 2019
Enables
This protein enables 5 target(s):
Target | Category | Definition |
cyclin-dependent protein serine/threonine kinase activity | molecular function | Cyclin-dependent catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:pr, GOC:rn, PMID:7877684, PMID:9841670] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
RNA polymerase II CTD heptapeptide repeat kinase activity | molecular function | Catalysis of the reaction: ATP + RNA polymerase II large subunit CTD heptapeptide repeat (consensus YSPTSPS) = ADP + H+ + phosphorylated RNA polymerase II. [EC:2.7.11.23, GOC:mah, PMID:28248323] |
protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
cyclin-dependent protein serine/threonine kinase activator activity | molecular function | Binds to and increases the activity of a cyclin-dependent protein serine/threonine kinase. [GOC:dph, PMID:2569363, PMID:3322810] |
Located In
This protein is located in 1 target(s):
Target | Category | Definition |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
Active In
This protein is active in 1 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] |
Part Of
This protein is part of 3 target(s):
Target | Category | Definition |
cyclin K-CDK12 complex | cellular component | A protein complex consisting of cyclin Kand cyclin-dependent kinase 12 (CDK12). Cyclins are characterized by periodicity in protein abundance throughout the cell cycle. Cyclin-dependent kinases represent a family of serine/threonine protein kinases that become active upon binding to a cyclin regulatory partner. [PMID:22012619] |
cyclin K-CDK13 complex | cellular component | A protein complex consisting of cyclin Kand cyclin-dependent kinase 13 (CDK13). Cyclins are characterized by periodicity in protein abundance throughout the cell cycle. Cyclin-dependent kinases represent a family of serine/threonine protein kinases that become active upon binding to a cyclin regulatory partner. [PMID:22012619] |
cyclin/CDK positive transcription elongation factor complex | cellular component | A transcription elongation factor complex that facilitates the transition from abortive to productive elongation by phosphorylating the CTD domain of the large subunit of DNA-directed RNA polymerase II, holoenzyme. Contains a cyclin and a cyclin-dependent protein kinase catalytic subunit. [GOC:bhm, GOC:vw, PMID:10766736, PMID:16721054, PMID:17079683, PMID:19328067, PMID:7759473] |
Involved In
This protein is involved in 8 target(s):
Target | Category | Definition |
regulation of cyclin-dependent protein serine/threonine kinase activity | biological process | Any process that modulates the frequency, rate or extent of cyclin-dependent protein serine/threonine kinase activity. [GOC:go_curators, GOC:pr] |
transcription by RNA polymerase II | biological process | The synthesis of RNA from a DNA template by RNA polymerase II (RNAP II), originating at an RNA polymerase II promoter. Includes transcription of messenger RNA (mRNA) and certain small nuclear RNAs (snRNAs). [GOC:jl, GOC:txnOH, ISBN:0321000382] |
regulation of signal transduction | biological process | Any process that modulates the frequency, rate or extent of signal transduction. [GOC:sm] |
positive regulation of transcription elongation by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription elongation, the extension of an RNA molecule after transcription initiation and promoter clearance by the addition of ribonucleotides, catalyzed by RNA polymerase II. [GOC:mah, GOC:txnOH] |
negative regulation by host of viral genome replication | biological process | A process in which a host organism stops, prevents or reduces the frequency, rate or extent of viral genome replication. [GOC:jl] |
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] |
regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
positive regulation of DNA-templated transcription, elongation | biological process | Any process that activates or increases the frequency, rate or extent of transcription elongation, the extension of an RNA molecule after transcription initiation and promoter clearance by the addition of ribonucleotides catalyzed by a DNA-dependent RNA polymerase. [GOC:mah, GOC:txnOH] |