Structure and inhibition analysis of the mouse SAD-B C-terminal fragment

Biosci Biotechnol Biochem. 2016 Oct;80(10):1939-46. doi: 10.1080/09168451.2016.1191331. Epub 2016 Jun 2.

Abstract

The SAD (synapses of amphids defective) kinases, including SAD-A and SAD-B, play important roles in the regulation of neuronal development, cell cycle, and energy metabolism. Our recent study of mouse SAD-A identified a unique autoinhibitory sequence (AIS), which binds at the junction of the kinase domain (KD) and the ubiquitin-associated (UBA) domain and exerts autoregulation in cooperation with UBA. Here, we report the crystal structure of the mouse SAD-B C-terminal fragment including the AIS and the kinase-associated domain 1 (KA1) at 2.8 Å resolution. The KA1 domain is structurally conserved, while the isolated AIS sequence is highly flexible and solvent-accessible. Our biochemical studies indicated that the SAD-B AIS exerts the same autoinhibitory role as that in SAD-A. We believe that the flexible isolated AIS sequence is readily available for interaction with KD-UBA and thus inhibits SAD-B activity.

Keywords: autoinhibitory sequence (AIS); crystal structure; kinase associated domain 1 (KA1); synapses of amphids defective (SAD).

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Conserved Sequence
  • Mice
  • Models, Molecular
  • Peptide Fragments / chemistry*
  • Protein Domains
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Protein Serine-Threonine Kinases / chemistry*
  • Protein Serine-Threonine Kinases / metabolism

Substances

  • Peptide Fragments
  • Brsk1 protein, mouse
  • Protein Serine-Threonine Kinases