General Information of the Protein
| Protein ID |
PT01975
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| Protein Name |
Cyclin-dependent kinase 8
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| Secondarily Protein Name |
Cell division protein kinase 8
Mediator complex subunit CDK8
Mediator of RNA polymerase II transcription subunit CDK8
Protein kinase K35
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| Gene Name |
CDK8
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| Sequence |
MDYDFKVKLSSERERVEDLFEYEGCKVGRGTYGHVYKAKRKDGKDDKDYALKQIEGTGISMSACREIALLRELKHPNVISLQKVFLSHADRKVWLLFDYAEHDLWHIIKFHRASKANKKPVQLPRGMVKSLLYQILDGIHYLHANWVLHRDLKPANILVMGEGPERGRVKIADMGFARLFNSPLKPLADLDPVVVTFWYRAPELLLGARHYTKAIDIWAIGCIFAELLTSEPIFHCRQEDIKTSNPYHHDQLDRIFNVMGFPADKDWEDIKKMPEHSTLMKDFRRNTYTNCSLIKYMEKHKVKPDSKAFHLLQKLLTMDPIKRITSEQAMQDPYFLEDPLPTSDVFAGCQIPYPKREFLTEEEPDDKGDKKNQQQQQGNNHTNGTGHPGNQDSSHTQGPPLKKVRVVPPTTTSGGLIMTSDYQRSNPHAAYPNPGPSTSQPQSSMGYSATSQQPPQYSHQTHRY
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| Organism |
Homo sapiens, Human
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| Protein Classification |
Enzyme
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Kinase
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Protein Kinase
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CMGC protein kinase group
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CMGC protein kinase CDK family
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CMGC protein kinase CDK8 subfamily
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| Function |
Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional pre-initiation complex with RNA polymerase II and the general transcription factors. Phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex. Phosphorylates CCNH leading to down-regulation of the TFIIH complex and transcriptional repression. Recruited through interaction with MAML1 to hyperphosphorylate the intracellular domain of NOTCH, leading to its degradation.
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| Uniprot ID |
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| HGNC ID | |||||
| Subcellular Location |
Nucleus
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Map of Molecular Bioactivity Related to the Protein
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Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity |
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Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000068 , A-549
Cell Line ID: CL000067 , HCT 116
Cell Line ID: CL000006 , HEK293
Cell Line ID: CL000103 , LS174T
Cell Line ID: CL000015 , SW480
Cell Line ID: CL000104 , SW620
Biochemical Assays
Clinical Information about the Protein
Target 1 ( Cyclin-dependent kinase 8 (CDK8) )
| Target Type | Clinical trial Target | ||||
|---|---|---|---|---|---|
| Disease | 3 Target-related Diseases | 3 | |||
| 1 | Acute myeloid leukaemia [ICD-11: 2A60] | ||||
| 2 | Colorectal cancer [ICD-11: 2B91.Z] | ||||
| 3 | Pain [ICD-11: MG30-MG3Z] | ||||
| Clinical Trial Drug(s) | 1 Clinical Trial Drug | 1 | |||
| 1 | SEL120 | Phase 1 | |||
| Investigative Drug(s) | 1 Investigative Drug | 1 | |||
| 1 | Oxindole 94 | Investigative | |||
| Preclinical Drug(s) | 1 Preclinical Drug | 1 | |||
| 1 | CCT251545 | Preclinical | |||