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