Preferred Label : CDK7 Inhibitor LY3405105;
NCIt synonyms : Cyclin-dependent Kinase 7 Inhibitor LY3405105;
NCIt definition : An orally bioavailable, selective inhibitor of cyclin-dependent kinase 7 (CDK7), with
potential antineoplastic activity. Upon oral administration, LY3405105 selectively
targets, binds to and inhibits the activity of CDK7, thereby inhibiting CDK7-mediated
signaling. Specifically, inhibition of CDK7 prevents phosphorylation of the carboxy-terminal
domain (CTD) of RNA Polymerase II, thereby preventing transcription of important cancer-promoting
genes. In addition, it prevents phosphorylation of the cell cycle kinases CDK1, 2,
4, and 6, thereby disrupting uncontrolled cell cycle progression. Altogether, this
may induce apoptosis, cause cell cycle arrest, inhibit DNA damage repair and inhibit
tumor cell proliferation in certain cancers that are dependent on CDK7-mediated transcriptional
regulation and signaling. CDK7, a serine/threonine kinase, plays a role in controlling
cell cycle progression, transcriptional regulation, and promotes the expression of
key oncogenes such as c-Myc and beta-catenin, through the phosphorylation of RNA polymerase
II.;
Molecule name : LY-3405105; LY 3405105;
NCI Metathesaurus CUI : CL1642442;
Origin ID : C176563;
UMLS CUI : C5447308;
Semantic type(s)
- 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
