Rational design, synthesis and biological evaluation of modular fluorogenic substrates with high affinity and selectivity for PTP1B.

@article{Sanchini2014RationalDS,
  title={Rational design, synthesis and biological evaluation of modular fluorogenic substrates with high affinity and selectivity for PTP1B.},
  author={Silvano Sanchini and Francesca Perruccio and Grazia Piizzi},
  journal={Chembiochem : a European journal of chemical biology},
  year={2014},
  volume={15 7},
  pages={961-76}
}
Protein-tyrosine phosphatase 1B (PTP1B) is a key regulatory enzyme in several signal transduction pathways, and its upregulation has been associated with type-2 diabetes, obesity and cancer. Selective determination of the functional significance of PTP1B remains a major challenge because the activity of this crucial enzyme is currently evaluated through the use of fluorescent probes that lack selectivity and are limited to biochemical assays. Here we describe the rational design, synthesis and… CONTINUE READING
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