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Cyclin-T1
A cyclin-T1 that is encoded in the genome of human. [PRO:CNA]
Synonyms
CycT1;
Cyclin-T
Research
Bioassay Publications (69)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 8 (11.59) | 29.6817 |
2010's | 48 (69.57) | 24.3611 |
2020's | 13 (18.84) | 2.80 |
Compounds (58)
Drugs with Inhibition Measurements
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.Journal of medicinal chemistry, , 03-09, Volume: 60, Issue:5, 2017
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
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
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
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
A β-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases.European journal of medicinal chemistry, , Volume: 61, 2013
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.European journal of medicinal chemistry, , Volume: 56, 2012
Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 18, Issue:21, 2008
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Current progress and novel strategies that target CDK12 for drug discovery.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency.European journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
[no title available]Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.Journal of medicinal chemistry, , 12-14, Volume: 60, Issue:23, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
[no title available]MedChemComm, , Mar-01, Volume: 6, Issue:3, 2015
Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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]European journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 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
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
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 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
[no title available]Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
[no title available]Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.Journal of medicinal chemistry, , 12-14, Volume: 60, Issue:23, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
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
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 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
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
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
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
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
[no title available]Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Discovery of Journal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 2021
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.MedChemComm, , Aug-01, Volume: 7, Issue:8, 2016
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
Discovery of novel CDK inhibitors via scaffold hopping from CAN508.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 28, Issue:8, 2018
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.European journal of medicinal chemistry, , Volume: 62, 2013
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Enables
This protein enables 10 target(s):
Target | Category | Definition |
transcription cis-regulatory region binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls transcription of that section of the DNA. The transcribed region might be described as a gene, cistron, or operon. [GOC:txnOH] |
DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
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] |
RNA polymerase binding | molecular function | Binding to an RNA polymerase molecule or complex. [GOC:BHF, GOC:mah, GOC:txnOH] |
7SK snRNA binding | molecular function | Binding to a 7SK small nuclear RNA (7SK snRNA). [GOC:nhn, PMID:21853533] |
DNA-binding transcription factor binding | molecular function | Binding to a DNA-binding transcription factor, a protein that interacts with a specific DNA sequence (sometimes referred to as a motif) within the regulatory region of a gene to modulate transcription. [GOC:txnOH-2018] |
molecular condensate scaffold activity | molecular function | Binding and bringing together two or more macromolecules in contact, permitting those molecules to organize as a molecular condensate. [PMID:28225081] |
Located In
This protein is located in 3 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] |
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 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 2 target(s):
Target | Category | Definition |
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] |
P-TEFb complex | cellular component | A dimeric positive transcription elongation factor complex b that comprises a cyclin-dependent kinase containing the catalytic subunit, Cdk9, and a regulatory subunit, cyclin T. [GOC:mah, GOC:vw, PMID:16721054, PMID:19328067, Wikipedia:P-TEFb] |
Involved In
This protein is involved in 9 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] |
response to xenobiotic stimulus | 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 from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
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] |
positive regulation by host of viral transcription | biological process | Any process in which a host organism activates or increases the frequency, rate or extent of viral transcription, the synthesis of either RNA on a template of DNA or DNA on a template of RNA. [GOC:jl] |
positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
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] |