Design, synthesis and structure-activity relationship of novel Relacin analogs as inhibitors of Rel proteins.

@article{Wexselblatt2013DesignSA,
  title={Design, synthesis and structure-activity relationship of novel Relacin analogs as inhibitors of Rel proteins.},
  author={Ezequiel Wexselblatt and Ilana Kaspy and Gad Glaser and Joshua Katzhendler and Eylon Yavin},
  journal={European journal of medicinal chemistry},
  year={2013},
  volume={70},
  pages={
          497-504
        }
}
Rel proteins in bacteria synthesize the signal molecules (p)ppGpp that trigger the Stringent Response, responsible for bacterial survival. Inhibiting the activity of such enzymes prevents the Stringent Response, resulting in the inactivation of long-term bacterial survival strategies, leading to bacterial cell death. Herein, we describe a series of deoxyguanosine-based analogs of the Relacin molecule that inhibit in vitro the synthetic activity of Rel proteins from Gram positive and Gram… CONTINUE READING

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