Aug 3, 2024 · To determine if Cdk7 S164 phosphorylation influences the formation of ternary complexes with Mat1, we established a surface plasmon resonance (SPR) spectroscopy assay.

Cdk7, associated with the transcription initiation factor TFIIH, is both an effector CDK that phosphorylates Pol II and other targets within the transcriptional machinery, and a CDK-activating kinase (CAK) for at least one other essential CDK involved in transcription.

Feb 14, 2024 · Cdk7 forms an active complex upon association with Cyclin H and Mat1, and its catalytic activity is regulated by two phosphorylations in the activation segment (T loop): the canonical activating modification at T170 and another at S164. Here we report .

Nov 2, 2021 · To accurately characterize the affinity of these molecules, a surface plasmon resonance (SPR) assay using immobilized CDK7/CyclinH dimer was developed, enabling measurement of compound binding kinetics, including off-rates (koff) reported here and determining subnanomolar Kd values for this series.

Cyclin-dependent kinase 7, or cell division protein kinase 7, is an enzyme that in humans is encoded by the CDK7 gene. [5] The protein encoded by this gene is a member of the cyclin-dependent protein kinase (CDK) family.

Nov 2, 2021 · This report describes the discovery of SY-5609, a highly potent (sub-nM CDK7 Kd) and selective, orally available inhibitor of CDK7 that entered the clinic in 2020 (ClinicalTrials.gov Identifier: NCT04247126).

Sep 13, 2021 · Recent efforts to develop small molecule inhibitors that target cyclin-dependent kinase 7 (CDK7) have suggested that CDK7 may play a critical role in mediating the transcription of key cancer dependence genes.

Feb 14, 2024 · Cyclin-dependent kinase (CDK) 7 is aberrantly overexpressed in many types of cancer and is an attractive target for cancer therapy due to its dual role in transcription and cell cycle...

Feb 14, 2024 · To determine if Cdk7 S164 phosphorylation influences formation of ternary complexes with Mat1, we established a surface plasmon resonance (SPR) assay. We covalently coupled an anti-maltose binding protein (MBP) antibody to a CM5 chip, which allowed us to immobilize MBP-Mat1 230-309.

We show that cdk7 activity is required for the activation of both Cdc2/Cyclin A and Cdc2/Cyclin B complexes, and for cell division. These results suggest that there may be a fundamental difference in the way metazoans and budding yeast effect a key modification of Cdks. Keywords: Drosophila, Cdk, CAK, mitosis, cell cycle.