Proteins > Bromodomain testis-specific protein
Page last updated: 2024-08-07 23:55:36
Bromodomain testis-specific protein
A bromodomain testis-specific protein that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q58F21]
Synonyms
Cancer/testis antigen 9;
CT9;
RING3-like protein
Research
Bioassay Publications (17)
| 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 | 8 (47.06) | 24.3611 |
| 2020's | 9 (52.94) | 2.80 |
Compounds (16)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| sb 202190 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| nu 7441 | Homo sapiens (human) | IC50 | 3.5000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | IC50 | 0.8300 | 2 | 2 |
| tg101209 | Homo sapiens (human) | IC50 | 0.2300 | 1 | 1 |
| fedratinib | Homo sapiens (human) | IC50 | 0.3400 | 1 | 1 |
| jq1 compound | Homo sapiens (human) | IC50 | 0.1902 | 13 | 11 |
| dinaciclib | Homo sapiens (human) | IC50 | 37.0000 | 1 | 1 |
| LSM-6732 | Homo sapiens (human) | IC50 | 0.1395 | 2 | 2 |
| gsk1210151a | Homo sapiens (human) | IC50 | 0.5801 | 3 | 3 |
| i-bet726 | Homo sapiens (human) | IC50 | 21.0986 | 3 | 3 |
| rvx 208 | Homo sapiens (human) | IC50 | 2.8168 | 4 | 4 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| volasertib | Homo sapiens (human) | Kd | 0.9477 | 3 | 3 |
| bi 2536 | Homo sapiens (human) | Kd | 0.3837 | 3 | 3 |
| ro3280 | Homo sapiens (human) | Kd | 1.3633 | 3 | 3 |
| xmd 8-92 | Homo sapiens (human) | Kd | 2.7917 | 3 | 3 |
| lrrk2-in1 | Homo sapiens (human) | Kd | 0.9300 | 3 | 3 |
| jq1 compound | Homo sapiens (human) | Kd | 0.1786 | 7 | 6 |
| gsk525762a | Homo sapiens (human) | Kd | 0.0860 | 2 | 2 |
| rvx 208 | Homo sapiens (human) | Kd | 2.7720 | 2 | 2 |
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy.Journal of medicinal chemistry, , 12-23, Volume: 64, Issue:24, 2021
[no title available]Journal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of Thieno[2,3-Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Development of live-cell imaging probes for monitoring histone modifications.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
[no title available],
Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| transcription coactivator activity | molecular function | A transcription coregulator activity that activates or increases the transcription of specific gene sets via binding to a DNA-bound DNA-binding transcription factor, either on its own or as part of a complex. Coactivators often act by altering chromatin structure and modifications. For example, one class of transcription coactivators modifies chromatin structure through covalent modification of histones. A second class remodels the conformation of chromatin in an ATP-dependent fashion. A third class modulates interactions of DNA-bound DNA-binding transcription factors with other transcription coregulators. A fourth class of coactivator activity is the bridging of a DNA-binding transcription factor to the general (basal) transcription machinery. The Mediator complex, which bridges sequence-specific DNA binding transcription factors and RNA polymerase, is also a transcription coactivator. [GOC:txnOH-2018, PMID:10213677, PMID:16858867] |
| histone binding | molecular function | Binding to a histone, any of a group of water-soluble proteins found in association with the DNA of eukaryotic or archaeal chromosomes. They are involved in the condensation and coiling of chromosomes during cell division and have also been implicated in gene regulation and DNA replication. They may be chemically modified (methylated, acetlyated and others) to regulate gene transcription. [GOC:jl, PMID:16209651, PMID:30212449, PMID:9305837] |
| lysine-acetylated histone binding | molecular function | Binding to a histone in which a lysine residue has been modified by acetylation. [GOC:BHF, GOC:mah, GOC:rl, PMID:17582821] |
| histone reader activity | molecular function | A chromatin adaptor that recognizes specific forms of histones, either modified by a post-translational modification, or the unmodified form. Histone readers have roles in many processes, including in centromere function or in modulating the accessibility of cis-regulatory regions to the transcription machinery. [PMID:11498575, PMID:25688442, PMID:31082667, PMID:32260176, PMID:34726351] |
Located In
This protein is located 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] |
Involved In
This protein is involved in 9 target(s):
| Target | Category | Definition |
|---|
| chromatin remodeling | biological process | A dynamic process of chromatin reorganization resulting in changes to chromatin structure. These changes allow DNA metabolic processes such as transcriptional regulation, DNA recombination, DNA repair, and DNA replication. [GOC:jid, GOC:vw, PMID:12042764, PMID:12697820] |
| regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| mRNA processing | biological process | Any process involved in the conversion of a primary mRNA transcript into one or more mature mRNA(s) prior to translation into polypeptide. [GOC:mah] |
| male meiotic nuclear division | biological process | A cell cycle process by which the cell nucleus divides as part of a meiotic cell cycle in the male germline. [GOC:dph, GOC:mah, GOC:vw] |
| male meiosis I | biological process | A cell cycle process comprising the steps by which a cell progresses through male meiosis I, the first meiotic division in the male germline. [GOC:dph, GOC:mah] |
| RNA splicing | biological process | The process of removing sections of the primary RNA transcript to remove sequences not present in the mature form of the RNA and joining the remaining sections to form the mature form of the RNA. [GOC:krc, GOC:mah] |
| sperm DNA condensation | biological process | The progressive compaction of the spermatid chromatin so that it reaches a level of condensation that is not compatible with nuclear activities such as transcription or DNA replication. [GOC:bf, PMID:11735001] |
| regulation of RNA splicing | biological process | Any process that modulates the frequency, rate or extent of RNA splicing, the process of removing sections of the primary RNA transcript to remove sequences not present in the mature form of the RNA and joining the remaining sections to form the mature form of the RNA. [GOC:jl] |
| positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |