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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C153377
http://purl.obolibrary.org/obo/NCIT_C153377
|
|---|---|
| Preferred Name | CDK9 Inhibitor AZD4573 |
| Definitions |
A selective, short-acting inhibitor of the serine/threonine cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the RNA polymerase II (RNA Pol II) elongation factor positive transcription elongation factor b (PTEF-b; PTEFb), with potential antineoplastic activity. Upon intravenous administration, AZD4573 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II, leading to the inhibition of gene transcription of various anti-apoptotic proteins. This induces cell cycle arrest and apoptosis, and leads to a reduction in tumor cell proliferation. CDK9 regulates elongation of transcription through phosphorylation of RNA polymerase II at serine 2 (p-Ser2-RNAPII). It is upregulated in various tumor cell types and plays a key role in the regulation of Pol II-mediated transcription of anti-apoptotic proteins. Tumor cells are dependent on anti-apoptotic proteins for their survival.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| definition | A selective, short-acting inhibitor of the serine/threonine cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the RNA polymerase II (RNA Pol II) elongation factor positive transcription elongation factor b (PTEF-b; PTEFb), with potential antineoplastic activity. Upon intravenous administration, AZD4573 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II, leading to the inhibition of gene transcription of various anti-apoptotic proteins. This induces cell cycle arrest and apoptosis, and leads to a reduction in tumor cell proliferation. CDK9 regulates elongation of transcription through phosphorylation of RNA polymerase II at serine 2 (p-Ser2-RNAPII). It is upregulated in various tumor cell types and plays a key role in the regulation of Pol II-mediated transcription of anti-apoptotic proteins. Tumor cells are dependent on anti-apoptotic proteins for their survival. |
|---|---|
| prefLabel | CDK9 Inhibitor AZD4573
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| label | CDK9 Inhibitor AZD4573
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| NCI_META_CUI | CL554533
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| PDQ_Closed_Trial_Search_ID | 793903
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| code | C153377
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| Has_Target | |
| prefixIRI | NCIT:C153377
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| in_subset |
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| Display_Name | CDK9 Inhibitor AZD4573
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| Preferred_Name | CDK9 Inhibitor AZD4573
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| FDA_UNII_Code | E5XSP3X68B
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| Contributing_Source |
CTRP
FDA
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| Maps_To | CDK9 Inhibitor AZD4573
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| CAS_Registry | 2057509-72-3
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| NCI_Drug_Dictionary_ID | 793903
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| type | |
| Is_Value_For_GDC_Property | |
| subClassOf | |
| PDQ_Open_Trial_Search_ID | 793903
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| Semantic_Type | Pharmacologic Substance
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