Preferred Label : Seliciclib;
NCIt synonyms : R-roscovitine;
NCIt 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.;
UNII : 0ES1C2KQ94;
InChIKey : BTIHMVBBUGXLCJ-OAHLLOKOSA-N;
CAS number : 186692-46-6;
Molecule name : CYC202;
Chemical formula : C19H26N6O;
Origin ID : C62783;
UMLS CUI : C1609861;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- Validated automatic mappings to NTBT
- chemical_or_drug_affects_gene_product
- chemical_or_drug_has_mechanism_of_action
- chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
- has_target
