Gsalpha-selective G protein antagonists.

  title={Gsalpha-selective G protein antagonists.},
  author={Martin Hohenegger and Maria Waldhoer and Wolfgang Beindl and Barbara B{\"o}ing and Annett Kreimeyer and Peter Nickel and Christian Nanoff and Michael Freissmuth},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  volume={95 1},
Suramin acts as a G protein inhibitor because it inhibits the rate-limiting step in activation of the Galpha subunit, i.e., the exchange of GDP for GTP. Here, we have searched for analogues that are selective for Gsalpha. Two compounds have been identified: NF449 (4,4',4",4'"-[carbonyl-bis[imino-5,1,3-benzenetriyl bis-(carbonylimino)]]tetrakis-(benzene-1,3-disulfonate) and NF503 (4, 4'-[carbonylbis[imino-3,1-phenylene-(2, 5-benzimidazolylene)carbonylimino]]bis-benzenesulfonate). These compounds… CONTINUE READING


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