Structure and inhibition of novel cyclin-dependent kinases

Thesis

Protein phosphorylation by members of the cyclin-dependent kinase (CDK) family determines the cell cycle and regulates gene transcription. CDK12 and CDK16 are relatively poorly characterised family members containing atypical domain extensions and represent novel targets for structural studies, as well as cancer drug discovery. In this thesis, I developed protocols to express and purify the human CDK12 kinase domain in complex with its obligate partner, CycK. I solved three distinct crysta...

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Authors: Dixon-Clarke, S

• Type of award: DPhil
• Level of award: Doctoral
• Awarding institution: University of Oxford
• Language: English
• Keywords: Rebastinib; CDK12; Cancer; Cyclin-dependent kinase; THZ531; CDK16 (PCTAIRE1/PCTK1); Kinase; Transcriptional CDKs
• Subjects: Medical sciences; X-ray crystallography; Mass spectrometry; Protein chemistry; Oncology