Anticancer activity of BIM-46174, a new inhibitor of the heterotrimeric Galpha/Gbetagamma protein complex.

@article{Prvost2006AnticancerAO,
  title={Anticancer activity of BIM-46174, a new inhibitor of the heterotrimeric Galpha/Gbetagamma protein complex.},
  author={Gr{\'e}goire Pierre Pr{\'e}vost and Marie O Lonchampt and Susan L. Holbeck and Samir Attoub and Daniel Zaharevitz and Mike Alley and John W. Wright and Marie Christine Brezak and H{\'e}l{\`e}ne Coulomb and Ann Savola and Marion Huchet and Sophie Chaumeron and Quang-De Nguyen and Patricia Forgez and Erik A. Bruyneel and Mark Bracke and Eric Ferrandis and Pierre Roubert and Dani{\`e}le Demarquay and Christian P Gespach and Philip G. Kasprzyk},
  journal={Cancer research},
  year={2006},
  volume={66 18},
  pages={9227-34}
}
A large number of hormones and local agonists activating guanine-binding protein-coupled receptors (GPCR) play a major role in cancer progression. Here, we characterize the new imidazo-pyrazine derivative BIM-46174, which acts as a selective inhibitor of heterotrimeric G-protein complex. BIM-46174 prevents the heterotrimeric G-protein signaling linked to several GPCRs mediating (a) cyclic AMP generation (Galphas), (b) calcium release (Galphaq), and (c) cancer cell invasion by Wnt-2 frizzled… CONTINUE READING

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