Bombesin and substance P analogues differentially regulate G-protein coupling to the bombesin receptor. Direct evidence for biased agonism.

@article{Mackinnon2001BombesinAS,
  title={Bombesin and substance P analogues differentially regulate G-protein coupling to the bombesin receptor. Direct evidence for biased agonism.},
  author={Alison Mackinnon and Christopher M. Waters and Duncan J. Jodrell and Christopher Haslett and Tariq Sethi},
  journal={The Journal of biological chemistry},
  year={2001},
  volume={276 30},
  pages={28083-91}
}
Substance P analogues including [d-Arg1,d-Phe5,d-Trp7,9,Leu11]substance P (SpD) act as "broad spectrum neuropeptide antagonists" and are potential anticancer agents that inhibit the growth of small cell lung cancer cells in vitro and in vivo. However, their mechanism of action is controversial and not fully understood. Although these compounds block bombesin-induced mitogenesis and signal transduction, they also have agonist activity. The mechanism underlying this agonist activity was examined… CONTINUE READING

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