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CDK7 (cyclin-dependent kinase 7) is a serine/threonine kinase
that functions as part of the CDK-activating kinase complex with cyclin H and
MAT1 and also forms a kinase subunit of the general transcription factor TFIIH.
CDK7 activates several cell-cycle CDKs by phosphorylating their activation loops
and promotes transcription by phosphorylating the C-terminal domain of RNA
polymerase II. Many cancers depend on elevated or sustained CDK7 activity to
maintain rapid proliferation and transcription of oncogenic programs, including
MYC-, estrogen-receptor- and androgen-receptor-regulated genes. CDK7 inhibition
can reduce RNA polymerase II phosphorylation, suppress oncogene transcription,
cause cell-cycle arrest and induce apoptosis. The typical cancer-associated
direction is up or hyperactive, while the desired anticancer
modulation is generally down or kinase inhibition.
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