Preferred Label : CDK7 Inhibitor LY3405105 Besylate;
NCIt synonyms : LY3405105 Besylate; LY 3405105 Besylate; Cyclin-dependent Kinase 7 Inhibitor LY3405105 Besylate; LY-3405105 Besylate;
NCIt definition : The besylate salt form of LY3405105, 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.;
NCI Metathesaurus CUI : CL1642405;
Origin ID : C176565;
UMLS CUI : C5447310;
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
