Mapping the active site in vasoactive intestinal peptide to a core of four amino acids: neuroprotective drug design.

@article{Gozes1999MappingTA,
  title={Mapping the active site in vasoactive intestinal peptide to a core of four amino acids: neuroprotective drug design.},
  author={Illana Gozes and Orly Perl and Eliezer Giladi and Anne Davidson and Osnat Ashur-Fabian and Sara Rubinraut and Mati Fridkin},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={1999},
  volume={96 7},
  pages={4143-8}
}
The understanding of the molecular mechanisms leading to peptide action entails the identification of a core active site. The major 28-aa neuropeptide, vasoactive intestinal peptide (VIP), provides neuroprotection. A lipophilic derivative with a stearyl moiety at the N-terminal and norleucine residue replacing the Met-17 was 100-fold more potent than VIP in promoting neuronal survival, acting at femtomolar-picomolar concentration. To identify the active site in VIP, over 50 related fragments… CONTINUE READING
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Gozes et al

  • A. Fisher, R. Brandeis, +7 authors 325– 331. 4148 Pharmacology
  • Proc. Natl. Acad. Sci. USA 96
  • 1999

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