Discovery of a new phosphotyrosine mimetic for PTP1B using breakaway tethering.

@article{Erlanson2003DiscoveryOA,
  title={Discovery of a new phosphotyrosine mimetic for PTP1B using breakaway tethering.},
  author={Daniel A. Erlanson and Robert S. McDowell and Molly Min He and Mike Randal and Robert Lee Simmons and Jenny Kung and Andrew Bryan Waight and Stig K. Hansen},
  journal={Journal of the American Chemical Society},
  year={2003},
  volume={125 19},
  pages={
          5602-3
        }
}
Protein tyrosine phosphatases play important roles in many signaling cascades involved in human disease. The identification of druglike inhibitors for these targets is a major challenge, and the discovery of suitable phosphotyrosine (pY) mimetics remains one of the key difficulties. Here we describe an extension of tethering technology, "breakaway tethering", which is ideally suited for discovering such new chemical entities. The approach involves first irreversibly modifying a protein with an… CONTINUE READING
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