Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases.

@article{Shang2012RationalDO,
  title={Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases.},
  author={Xun Zhong Shang and Fillipo Marchioni and Nisha S Sipes and Chris Richard Evelyn and Moran Jerabek-Willemsen and Stefan Duhr and William Seibel and Matthew D. Wortman and Yi Xiong Zheng},
  journal={Chemistry & biology},
  year={2012},
  volume={19 6},
  pages={
          699-710
        }
}
Rho GTPases have been implicated in diverse cellular functions and are potential therapeutic targets. By virtual screening, we have identified a Rho-specific inhibitor, Rhosin. Rhosin contains two aromatic rings tethered by a linker, and it binds to the surface area sandwiching Trp58 of RhoA with a submicromolar Kd and effectively inhibits GEF-catalyzed RhoA activation. In cells, Rhosin specifically inhibited RhoA activity and RhoA-mediated cellular function without affecting Cdc42 or Rac1… CONTINUE READING
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References

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SHOWING 1-10 OF 42 REFERENCES

Clostridium difficile toxins: more than mere inhibitors of Rho proteins.

  • The international journal of biochemistry & cell biology
  • 2008
VIEW 4 EXCERPTS
HIGHLY INFLUENTIAL

GEF means go: turning on RHO GTPases with guanine nucleotide-exchange factors

  • Nature Reviews Molecular Cell Biology
  • 2005
VIEW 13 EXCERPTS
HIGHLY INFLUENTIAL

Rational design and characterization of a Rac GTPase-specific small molecule inhibitor.

  • Proceedings of the National Academy of Sciences of the United States of America
  • 2004
VIEW 5 EXCERPTS
HIGHLY INFLUENTIAL