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- NCIT_C176565 IAO_0000115 "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." @default.
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- NCIT_C176565 NCIT_P106 "Organic Chemical" @default.
- NCIT_C176565 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C176565 NCIT_P107 "CDK7 Inhibitor LY3405105 Besylate" @default.
- NCIT_C176565 NCIT_P108 "CDK7 Inhibitor LY3405105 Besylate" @default.
- NCIT_C176565 NCIT_P208 "CL1642405" @default.
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- NCIT_C176565 hasExactSynonym "CDK7 Inhibitor LY3405105 Besylate" @default.
- NCIT_C176565 hasExactSynonym "Cyclin-dependent Kinase 7 Inhibitor LY3405105 Besylate" @default.
- NCIT_C176565 hasExactSynonym "LY 3405105 Besylate" @default.
- NCIT_C176565 hasExactSynonym "LY-3405105 Besylate" @default.
- NCIT_C176565 hasExactSynonym "LY3405105 Besylate" @default.
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- NCIT_C176565 type Class @default.
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- NCIT_C176565 label "CDK7 Inhibitor LY3405105 Besylate" @default.
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