Chemical inhibition of prometastatic lysyl-tRNA synthetase-laminin receptor interaction

Nat Chem Biol. 2014 Jan;10(1):29-34. doi: 10.1038/nchembio.1381. Epub 2013 Nov 10.

Abstract

Lysyl-tRNA synthetase (KRS), a protein synthesis enzyme in the cytosol, relocates to the plasma membrane after a laminin signal and stabilizes a 67-kDa laminin receptor (67LR) that is implicated in cancer metastasis; however, its potential as an antimetastatic therapeutic target has not been explored. We found that the small compound BC-K-YH16899, which binds KRS, impinged on the interaction of KRS with 67LR and suppressed metastasis in three different mouse models. The compound inhibited the KRS-67LR interaction in two ways. First, it directly blocked the association between KRS and 67LR. Second, it suppressed the dynamic movement of the N-terminal extension of KRS and reduced membrane localization of KRS. However, it did not affect the catalytic activity of KRS. Our results suggest that specific modulation of a cancer-related KRS-67LR interaction may offer a way to control metastasis while avoiding the toxicities associated with inhibition of the normal functions of KRS.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Cell Membrane / metabolism
  • Lysine-tRNA Ligase / antagonists & inhibitors
  • Lysine-tRNA Ligase / metabolism*
  • Neoplasm Metastasis*
  • Protein Transport
  • Receptors, Laminin / antagonists & inhibitors
  • Receptors, Laminin / metabolism*

Substances

  • Receptors, Laminin
  • Lysine-tRNA Ligase

Associated data

  • PubChem-Substance/164194142
  • PubChem-Substance/164194143
  • PubChem-Substance/164194144
  • PubChem-Substance/164194145
  • PubChem-Substance/164194146