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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C62783
http://purl.obolibrary.org/obo/NCIT_C62783
|
|---|---|
| Preferred Name | Seliciclib |
| Definitions |
An orally available small molecule and cyclin-dependent kinase (CDK) inhibitor with potential apoptotic and antineoplastic activity. CDKs, serine/threonine kinases that play an important role in cell cycle regulation, are overexpressed in various malignancies. Seliciclib primarily inhibits CDK 2, 7, and 9 by competing for the ATP binding sites on these kinases, leading to a disruption of cell cycle progression. In addition, this agent seems to interfere with CDK-mediated phosphorylation of the carboxy-terminal domain of RNA polymerase II, thereby inhibiting RNA polymerase II-dependent transcription. This may lead to the down-regulation of anti-apoptotic factors, such as myeloid cell leukemia sequence 1 (Mcl-1), a protein crucial for the survival of a range of tumor cell types. The down-regulation of anti-apoptotic factors may lead to an induction of apoptosis, thereby further contributing to seliciclib's antiproliferative effects.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| definition | An orally available small molecule and cyclin-dependent kinase (CDK) inhibitor with potential apoptotic and antineoplastic activity. CDKs, serine/threonine kinases that play an important role in cell cycle regulation, are overexpressed in various malignancies. Seliciclib primarily inhibits CDK 2, 7, and 9 by competing for the ATP binding sites on these kinases, leading to a disruption of cell cycle progression. In addition, this agent seems to interfere with CDK-mediated phosphorylation of the carboxy-terminal domain of RNA polymerase II, thereby inhibiting RNA polymerase II-dependent transcription. This may lead to the down-regulation of anti-apoptotic factors, such as myeloid cell leukemia sequence 1 (Mcl-1), a protein crucial for the survival of a range of tumor cell types. The down-regulation of anti-apoptotic factors may lead to an induction of apoptosis, thereby further contributing to seliciclib's antiproliferative effects. |
|---|---|
| prefLabel | Seliciclib
|
| label | Seliciclib
|
| PDQ_Closed_Trial_Search_ID | 511023
|
| code | C62783
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| Has_Target | |
| prefixIRI | NCIT:C62783
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| in_subset |
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| Display_Name | Seliciclib
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| Preferred_Name | Seliciclib
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| FDA_UNII_Code | 0ES1C2KQ94
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| Contributing_Source |
CTRP
FDA
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| Chemical_Formula | C19H26N6O
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| Maps_To | Seliciclib
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| CAS_Registry | 186692-46-6
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| NCI_Drug_Dictionary_ID | 511023
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| Legacy Concept Name | Seliciclib
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| type | |
| Is_Value_For_GDC_Property | |
| subClassOf | |
| PDQ_Open_Trial_Search_ID | 511023
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| Semantic_Type |
Organic Chemical
Pharmacologic Substance
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| UMLS_CUI | C1436187
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