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G1/S-specific cyclin-D3
A G1/S-specific cyclin-D3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P30281]
Synonyms
Research
Bioassay Publications (32)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 9 (28.13) | 29.6817 |
2010's | 15 (46.88) | 24.3611 |
2020's | 8 (25.00) | 2.80 |
Compounds (13)
Drugs with Inhibition Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
alvocidib | Homo sapiens (human) | ID50 | 0.4000 | 1 | 1 |
Ring closure strategy leads to potent RIPK3 inhibitors.European journal of medicinal chemistry, , May-05, Volume: 217, 2021
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
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
[no title available]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
[no title available]European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation.Journal of medicinal chemistry, , 03-09, Volume: 60, Issue:5, 2017
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant CancerJournal of medicinal chemistry, , 04-12, Volume: 61, Issue:7, 2018
[no title available]European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 2017
[no title available]Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
[no title available]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity Bioorganic & medicinal chemistry letters, , 03-01, Volume: 28, Issue:5, 2018
[no title available]European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.European journal of medicinal chemistry, , Mar-25, Volume: 148, 2018
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
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] |
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] |
cyclin-dependent protein serine/threonine kinase regulator activity | molecular function | Modulates the activity of a cyclin-dependent protein serine/threonine kinase, enzymes of the protein kinase family that are regulated through association with cyclins and other proteins. [GOC:pr, GOC:rn, PMID:7877684, PMID:9442875] |
Located In
This protein is located in 2 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] |
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] |
Active In
This protein is active in 3 target(s):
Target | Category | Definition |
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] |
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 3 target(s):
Target | Category | Definition |
cyclin D3-CDK4 complex | cellular component | A protein complex consisting of cyclin D3 and cyclin-dependent kinase 4 (CDK4). 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. [GOC:so, PMID:15935619] |
cyclin D3-CDK6 complex | cellular component | A protein complex consisting of cyclin D3 and cyclin-dependent kinase 6 (CDK6). 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. [GOC:so, PMID:15935619] |
cyclin-dependent protein kinase holoenzyme complex | cellular component | Cyclin-dependent protein kinases (CDKs) are enzyme complexes that contain a kinase catalytic subunit associated with a regulatory cyclin partner. [GOC:krc, PMID:11602261] |
Involved In
This protein is involved in 10 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 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] |
positive regulation of protein phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of addition of phosphate groups to amino acids within a protein. [GOC:hjd] |
signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
T cell proliferation | biological process | The expansion of a T cell population by cell division. Follows T cell activation. [GOC:jl] |
regulation of cell population proliferation | biological process | Any process that modulates the frequency, rate or extent of cell proliferation. [GOC:jl] |
positive regulation of cyclin-dependent protein serine/threonine kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of CDK activity. [GOC:go_curators, GOC:pr] |
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] |
positive regulation of G1/S transition of mitotic cell cycle | biological process | Any signaling pathway that increases or activates a cell cycle cyclin-dependent protein kinase to modulate the switch from G1 phase to S phase of the mitotic cell cycle. [GOC:mtg_cell_cycle] |
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] |