This grad topic will focus on a structural survey of eukaryotic protein kinase function and regulation. The course will involve literature reading plus a few lectures.

Topics and papers will be selected from the following themes biased heavily on atomic resolution (X-ray crystallographic and NMR) snapshots of protein kinases in action:

1. Structure and catalytic mechanism of the protein kinase domain

  • conserved subdomains

  • the regulatory and catalytic spines

2. Modes of catalytic regulation

  • the activation segment

  • dimerization induced allostery

  • pseudo-substrate regulation

  • higher order inter and intramolecular mechanisms

3. Modes of substrate recognition

  • Serine versus Threonine versus Tyrosine specificity

  • peptide based substrate targeting mechanisms

  • domain based substrate targeting mechanisms

4. Mechanism of action of disease causing mutations and small molecule intervention strategies

Coordinators: Dr. Frank Sicheri
Dates: TBA
Place: TBA
Enrollment: Class size is limited to 10 students