Page last updated: 2024-08-07 16:49:09
Cyclin-H
A cyclin-H that is encoded in the genome of human. [PRO:DNx]
Synonyms
MO15-associated protein;
p34;
p37
Research
Bioassay Publications (41)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 7 (17.07) | 29.6817 |
| 2010's | 24 (58.54) | 24.3611 |
| 2020's | 10 (24.39) | 2.80 |
Compounds (47)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gw8510 | Homo sapiens (human) | IC50 | 0.3170 | 1 | 1 |
| nu6102 | Homo sapiens (human) | IC50 | 3.4500 | 2 | 2 |
| staurosporine | Homo sapiens (human) | IC50 | 0.2793 | 5 | 5 |
| cyc 202 | Homo sapiens (human) | IC50 | 0.5614 | 13 | 17 |
| 2H-pyrazolo[4,3-b]quinoxalin-3-amine | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| 6-bromoindirubin-3'-oxime | Homo sapiens (human) | IC50 | 3.5000 | 1 | 1 |
| purvalanol a | Homo sapiens (human) | IC50 | 0.0497 | 1 | 3 |
| 2-methyl-5-(4-methylanilino)-1,3-benzothiazole-4,7-dione | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| cgp 60474 | Homo sapiens (human) | IC50 | 0.2000 | 1 | 1 |
| cgp 74514a | Homo sapiens (human) | IC50 | 0.2790 | 1 | 1 |
| 1,4-dimethoxy-10H-acridine-9-thione | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | IC50 | 0.0823 | 6 | 6 |
| harmine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| wogonin | Homo sapiens (human) | IC50 | 12.3000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 0.3413 | 3 | 3 |
| su 9516 | Homo sapiens (human) | IC50 | 0.9050 | 1 | 1 |
| arcyriaflavin a | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| palbociclib | Homo sapiens (human) | IC50 | 6.6665 | 2 | 2 |
| palbociclib | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| cyc 116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| cvt 313 | Homo sapiens (human) | IC50 | 9.2000 | 1 | 1 |
| leucettamine b | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nu 6140 | Homo sapiens (human) | IC50 | 2.3000 | 1 | 1 |
| rgb 286638 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| at 7519 | Homo sapiens (human) | IC50 | 2.4000 | 2 | 2 |
| at 7519 | Homo sapiens (human) | Ki | 2.8000 | 1 | 1 |
| pf 573228 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | IC50 | 0.1900 | 3 | 3 |
| 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 | 0.0200 | 2 | 2 |
| p276-00 | Homo sapiens (human) | IC50 | 2.8700 | 1 | 1 |
| cink4 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ldc067 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| bs 194 | Homo sapiens (human) | IC50 | 0.2500 | 1 | 1 |
| (R)-DRF053 | Homo sapiens (human) | IC50 | 0.8220 | 1 | 1 |
| pf 3758309 | Homo sapiens (human) | IC50 | 0.0070 | 1 | 1 |
| ribociclib | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| bay 1000394 | Homo sapiens (human) | IC50 | 0.0250 | 3 | 3 |
| pha 793887 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | IC50 | 2.6027 | 3 | 3 |
| abemaciclib | Homo sapiens (human) | Ki | 3.9100 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | IC50 | 0.1700 | 2 | 2 |
| gilteritinib | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| longdaysin | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
| bs-181 | Homo sapiens (human) | IC50 | 0.0775 | 2 | 2 |
| on123300 | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| ly2857785 | Homo sapiens (human) | IC50 | 0.2460 | 1 | 1 |
| THZ531 | Homo sapiens (human) | IC50 | 5.8173 | 3 | 3 |
| can 508 | Homo sapiens (human) | IC50 | 28.1062 | 3 | 8 |
| ((5z)5-(1,3-benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4h-imidazol-4-one) | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ro 3306 | Homo sapiens (human) | IC50 | 17.4000 | 1 | 1 |
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
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
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 (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 29, Issue:20, 2019
Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
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
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
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
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 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
Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1.Cancer research, , Jun-15, Volume: 65, Issue:12, 2005
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
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
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 18, Issue:21, 2008
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
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
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
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 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
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
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
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
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
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
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, 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
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
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
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 29, Issue:20, 2019
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
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
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| 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 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 5 target(s):
| Target | Category | Definition |
|---|
| 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] |
| transcription factor TFIIH core complex | cellular component | The 7 subunit core of TFIIH that is a part of either the general transcription factor holo-TFIIH or the nucleotide-excision repair factor 3 complex. In S. cerevisiae/humans the complex is composed of: Ssl2/XPB, Tfb1/p62, Tfb2/p52, Ssl1/p44, Tfb4/p34, Tfb5/p8 and Rad3/XPD. [GOC:ew, GOC:krc, PMID:14500720, PMID:17215295, PMID:22308316, PMID:22572993, PMID:23028141, PMID:7813015] |
| transcription factor TFIIH holo complex | cellular component | A complex that is capable of kinase activity directed towards the C-terminal Domain (CTD) of the largest subunit of RNA polymerase II and is essential for initiation at RNA polymerase II promoters in vitro. It is composed of the core TFIIH complex and the TFIIK complex. [GOC:ew, GOC:krc, PMID:14500720, PMID:22308316, PMID:22572993, PMID:7813015] |
| CAK-ERCC2 complex | cellular component | A protein complex formed by the association of the cyclin-dependent protein kinase activating kinase (CAK) holoenzyme complex with ERCC2. [PMID:8692841, PMID:8692842] |
| transcription factor TFIIK complex | cellular component | A transcription factor complex that forms part of the holo TFIIH complex. In Saccharomyces/human, TFIIK contains Ccl1p/Cyclin H, Tfb3p/MAT1 and Kin28p/CDK7. [GOC:mah, PMID:19818408, PMID:22572993] |
Involved In
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|
| 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] |
| transcription initiation at RNA polymerase II promoter | biological process | A transcription initiation process that takes place at a RNA polymerase II gene promoter. Messenger RNAs (mRNA) genes, as well as some non-coding RNAs, are transcribed by RNA polymerase II. [GOC:mah, GOC:txnOH] |
| protein stabilization | biological process | Any process involved in maintaining the structure and integrity of a protein and preventing it from degradation or aggregation. [GOC:ai] |
| regulation of G1/S transition of mitotic cell cycle | biological process | Any signaling pathway that modulates the activity of 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] |